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(11bS)-9,10-dimethoxy-3-(3-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
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(11bS)-9,10-dimethoxy-3-phenyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
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(1R)-1-(4-bromophenyl)-2-(2,5-difluorophenyl)ethanamine
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(1R)-1-[4-(3-chloropyridin-4-yl)phenyl]-2-(2,5-difluorophenyl)ethanamine
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(1R)-2-(2,5-difluorophenyl)-1-(4-pyridin-4-ylphenyl)ethanamine
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(1R)-2-([(3R,4R)-4-amino-1-[1-(4-ethynylphenyl)ethyl]pyrrolidin-3-yl]carbonyl)cyclopentanecarbonitrile
-
(1R)-2-([(3R,4R)-4-amino-1-[2-methyl-4-(1H-1,2,4-triazol-1-yl)benzyl]pyrrolidin-3-yl]carbonyl)cyclopentanecarbonitrile
-
(1R)-2-([(3R,4R)-4-amino-1-[3-methyl-4-(1H-1,2,4-triazol-1-yl)benzyl]pyrrolidin-3-yl]carbonyl)cyclopentanecarbonitrile
-
(1R)-2-[[(3R,4R)-4-amino-1-(3,4-dihydro-2H-chromen-4-yl)pyrrolidin-3-yl]carbonyl]cyclopentanecarbonitrile
-
(1R)-2-[[(3R,4R)-4-amino-1-[1-[4-(1H-1,2,4-triazol-1-yl)phenyl]ethyl]pyrrolidin-3-yl]carbonyl]cyclopentanecarbonitrile
(1R,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
-
-
(1R,3S)-2-([(3R,4R)-4-amino-1-[4-(5-methyl-1,3,4-oxadiazol-2-yl)benzyl]pyrrolidin-3-yl]carbonyl)-3-fluorocyclopentanecarbonitrile
-
(1R,3S)-2-[(2S)-2-amino-2-cyclopentylacetyl]-3-ethynylcyclopentanecarbonitrile
(1S)-1-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-2-[(3S)-3-fluoropyrrolidin-1-yl]-2-oxoethanaminium
-
(1S)-1-cyclohexyl-2-(3,3-difluoropyrrolidin-1-yl)-2-oxoethanamine
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(1S)-1-cyclohexyl-2-(3-fluoropyrrolidin-1-yl)-2-oxoethanamine
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(1S)-1-cyclohexyl-2-oxo-2-(3,3,4,4-tetrafluoropyrrolidin-1-yl)ethanamine
-
-
(1S,2R)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
-
-
(1S,2R,5S)-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-2-(2,4,5-trifluorophenyl)cyclohexanamine
(1S,2S)-1-(4'-fluorobiphenyl-4-yl)-3-[(3S)-3-fluoropyrrolidin-1-yl]-3-oxo-1-(1H-tetrazol-1-yl)propan-2-amine
-
(1S,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopropyl-3-[(3S)-3-fluoropyrrolidin-1-yl]-3-oxopropan-2-aminium
-
-
(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
-
-
(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
(1S,3S,5S)-2-[(2S)-2-amino-2-[(1R,3S,5S)-3-hydroxytricyclo[3.3.1.13,7]dec-1-yl]acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
-
(2-(4-((2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl)-2-oxoethyl)amino)-4-methyl-1-piperidinyl)-4-pyridine carboxylic acid
i. e. ABT-279, a very potent, selective, effective, and well-tolerated inhibitor useful for the treatment of diabetes
(2-(4-((2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl)-2-oxoethyl)amino)-4-methyl-1-piperidinyl)-4-pyridinecarboxylic acid
(2R)-1-(2,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2,4-difluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-(2,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2,5-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(2-phenyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl)butan-2-amine
-
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(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(3-pyridin-4-yl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)butan-2-amine
-
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(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
-
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(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
(2R)-1-(2,5-difluorophenyl)-4-[(4R)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
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(2R)-1-(2,5-difluorophenyl)-4-[(4S)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[1-(2-methylpropyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[1-(4-fluorobenzyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[1-ethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[2-(4-fluorophenyl)-1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-(2,5-difluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-(2-methylpropyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorobenzyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-ethyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-[3-methyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
-
-
(2R)-1-(2-chloro-4,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2-fluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
(2R)-1-(2-methylphenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-(3,4-dichlorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-(3,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(3,4-difluorophenyl)-4-(3-ethyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxobutan-2-amine
-
-
(2R)-1-(3,4-difluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-(3,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
(2R)-1-(3-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(3-fluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-(3-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(4-chloro-2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(4-chlorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-(4-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(4-fluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-(4-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(4-iodophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-(4-nitrophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-(5-chloro-2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-cyclohexyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-1-oxopropan-2-aminium
-
-
(2R)-1-[8-(trifluoromethyl)bis[1,2,4]triazolo[4,3-a:3',4'-c]pyrazin-3-yl]-3-(2,4,5-trifluorophenyl)propan-2-amine
-
-
(2R)-1-[9-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4',3':1,2]pyrido[3,4-d]pyrimidin-3-yl]-3-(2,4,5-trifluorophenyl)propan-2-amine
-
-
(2R)-1-[N-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)glycyl]pyrrolidine-2-carbonitrile
-
-
(2R)-4-(1,4-diazepan-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-(2-benzoylpyrazolidin-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-(2-cyclopropyl-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-(3-cyclopropyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-(3-ethyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-(3-methyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-(4-acetyl-1,4-diazepan-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-(4-benzyl-1,4-diazepan-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-(4-ethyl-1,4-diazepan-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-(5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-1-(2,4,5-trifluorophenyl)-4-[1,4,4-trimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
-
-
(2R)-4-oxo-1-(pentafluorophenyl)-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-4-oxo-1-phenyl-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-4-oxo-1-pyridin-2-yl-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-4-oxo-1-pyridin-3-yl-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-4-oxo-1-pyridin-4-yl-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-4-oxo-4-(1,3-thiazolidin-3-yl)-1-(3,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-oxo-4-(1,3-thiazolidin-3-yl)-1-[2-(trifluoromethyl)phenyl]butan-2-amine
-
(2R)-4-oxo-4-(1,3-thiazolidin-3-yl)-1-[3-(trifluoromethyl)phenyl]butan-2-amine
-
(2R)-4-oxo-4-(1,3-thiazolidin-3-yl)-1-[4-(trifluoromethyl)phenyl]butan-2-amine
-
(2R)-4-oxo-4-(2-phenyl-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-(4-pyrazin-2-yl-1,4-diazepan-1-yl)-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-oxo-4-(4-pyrimidin-2-yl-1,4-diazepan-1-yl)-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-oxo-4-pyrazolidin-1-yl-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8R)-2-(trifluoromethyl)-8-[4-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8R)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8R)-8-(1H-1,2,4-triazol-1-ylmethyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8R)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8R)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8R)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8S)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8S)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8S)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[(8S)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[2-(phenylcarbonyl)-1,2-diazepan-1-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
competitive
(2R)-4-oxo-4-[2-(phenylcarbonyl)tetrahydropyridazin-1(2H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
the inhibitor displays a greater than 1400fold selectivity over all the enzymes tested including DPP-8 and DPP-9
(2R)-4-oxo-4-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,6-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,6-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[2-(trifluoromethyl)phenyl]butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[3-(trifluoromethyl)phenyl]butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[4-(trifluoromethyl)phenyl]butan-2-amine
-
-
(2R)-4-oxo-4-[4-(phenylcarbonyl)-1,4-diazepan-1-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-oxo-4-[4-(pyridin-3-ylcarbonyl)-1,4-diazepan-1-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-oxo-4-[8-(1H-pyrazol-1-ylmethyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(2R)-2-benzylpiperazin-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4R)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(4S)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(5R)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(5S)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(6R)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(6S)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-(4-fluorobenzyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-(cyclopropylmethyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-methyl-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-[(1-fluorocyclopropyl)methyl]-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8R)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-methyl-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[(8S)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
(2R)-4-[2-[(4-methylphenyl)sulfonyl]pyrazolidin-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[3-(difluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[4-(1,3-benzodioxol-5-ylcarbonyl)-1,4-diazepan-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine hydrochloride
-
(2R)-4-[4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[4-(methylsulfonyl)-1,4-diazepan-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-[4-[(4-methylphenyl)sulfonyl]-1,4-diazepan-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-[4-[(4-methylpiperazin-1-yl)carbonyl]-1,4-diazepan-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-[4-[(4-nitrophenyl)sulfonyl]-1,4-diazepan-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-[5,5-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[8,8-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[8-(1H-imidazol-1-ylmethyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[8-(4-fluorobenzyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[8-methyl-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R,3R)-1-(2,5-difluorophenyl)-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]butan-2-amine
-
-
(2R,3R)-3-(2,4,5-trifluorophenyl)-1,2,3,4-tetrahydropyrido[1,2-a]benzimidazol-2-amine
-
potent, selectiveDPP-4 inhibitor
(2R,3R)-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
(2R,3S)-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N1,N1-dimethyl-4-oxobutane-1,3-diamine
-
(2R,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
-
-
(2R,3S,11bS)-3-(3,4-dimethylphenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2R,3S,11bS)-3-(3-chlorophenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2R,3S,11bS)-9,10-dimethoxy-3-(3-methoxyphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2R,3S,11bS)-9,10-dimethoxy-3-(3-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2R,3S,11bS)-9,10-dimethoxy-3-(4-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2R,3S,11bS)-9,10-dimethoxy-3-phenyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2R,3S,11bS)-9,10-dimethoxy-3-pyridin-2-yl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2R,3S,5R)-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-2-(2,4,5-trifluorophenyl)tetrahydro-2H-pyran-3-amine
-
-
(2R,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
(2R,4R)-2-(dihydroxyboranyl)-4-hydroxypyrrolidin-1-yl (4S)-4-hydroxy-L-prolinate
-
best selectivity for dipeptidyl peptidase IV over dipeptidyl peptidases DPP8 and DPP9
(2R,4R)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
-
-
(2R,4R)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
-
-
(2R,4S)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
-
-
(2R,4S)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
-
-
(2R,5S)-1-[N-[1-(5-cyanopyridin-2-yl)-4-methylpiperidin-4-yl]glycyl]pyrrolidine-2,5-dicarbonitrile
-
(2R,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)-N-phenylpyrrolidine-2-carboxamide
-
(2R,5S)-N-(4-bromophenyl)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidine-2-carboxamide
-
(2S)-1-(((2S,5R)-5-[(1,3-benzodioxol-4-yloxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(((2S,5R)-5-[(1-naphthyloxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(((2S,5R)-5-[(2,4-dichlorophenoxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(((2S,5R)-5-[(2,6-dichlorophenoxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(((2S,5R)-5-[(2-chloro-4-cyanophenoxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(((2S,5R)-5-[(2-chlorophenoxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(((2S,5R)-5-[(2-methylphenoxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(((2S,5R)-5-[(4-bromophenoxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(((2S,5R)-5-[(4-cyanophenoxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(((2S,5R)-5-[(4-methoxyphenoxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(((2S,5R)-5-[(4-methylphenoxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(((2S,5R)-5-[(benzyloxy)methyl]pyrrolidin-2-yl)carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-(3-furyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2S)-1-(5-morpholin-4-yl-5-oxo-L-norvalyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-(5-oxo-5-piperidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-(5-oxo-5-pyrrolidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-([(2S,4S)-4-[(2E)-but-2-en-1-yl]pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
(2S)-1-([(2S,4S)-4-[(3-chloro-4-cyanophenyl)amino]pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-([(2S,5R)-5-(([2-chloro-5-(dihydroxymethyl)pyridin-3-yl]oxy)methyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(2S,5R)-5-(([dihydroxy(phenyl)-'4-sulfanyl]amino)methyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(2S,5R)-5-(anilinomethyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(2S,5R)-5-(morpholin-4-ylmethyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(2S,5R)-5-(phenoxymethyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(2S,5R)-5-([(2-chloropyridin-3-yl)oxy]methyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(2S,5R)-5-([(4-bromophenyl)amino]methyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(2S,5R)-5-([(6-bromo-1,3-benzodioxol-5-yl)oxy]methyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(2S,5R)-5-([2,4-dichloro-5-(dihydroxyamino)phenoxy]methyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(2S,5R)-5-([2-bromo-4-(methylsulfonodithioyl)phenoxy]methyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(2S,5R)-5-([2-chloro-4-(methylsulfonodithioyl)phenoxy]methyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(3R,4R)-4-amino-1-[4-(1,2,3-thiadiazol-4-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(3R,4R)-4-amino-1-[4-(1-methyl-1H-pyrazol-4-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(3R,4R)-4-amino-1-[4-(1H-1,2,4-triazol-1-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(3R,4R)-4-amino-1-[4-(1H-pyrazol-5-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(3R,4R)-4-amino-1-[4-(2H-1,2,3-triazol-2-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(3R,4R)-4-amino-1-[4-(3-methyl-1H-1,2,4-triazol-1-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([(3R,4R)-4-amino-1-[4-(5-methyl-1,3,4-oxadiazol-2-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([[(1R,3S,5S)-3-hydroxytricyclo[3.3.1.13,7]dec-1-yl]amino]acetyl)pyrrolidine-2-carbonitrile
-
(2S)-1-([[2-methyl-4-oxo-4-(pyrrolidin-1-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile
(2S)-1-cyclopentyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2S)-1-L-prolylpyrrolidine-2-carbonitrile
(2S)-1-[(1-adamantylamino)acetyl]pyrrolidine-2-carbonitrile
-
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-1-oxo-3-phenylpropan-2-amine
-
-
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-1-oxohexan-2-amine
-
-
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-3,3-dimethyl-1-oxobutan-2-amine
-
-
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-3-(4-chlorophenyl)-1-oxopropan-2-amine
-
-
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-3-methyl-1-oxobutan-2-amine
-
-
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-4-methyl-3-(1-methylethyl)-1-oxopentan-2-amine
-
-
(2S)-1-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-1-oxopropan-2-aminium
-
-
(2S)-1-[(2R)-2-amino-2-cyclopentylacetyl]pyrrolidine-2-carbonitrile
-
(2S)-1-[(2S)-2-amino-2-cyclopentylacetyl]pyrrolidine-2-carbonitrile
(2S)-1-[(2S)-2-amino-3,3-dimethylbutanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S)-2-amino-4-(1,3-dihydro-2H-isoindol-2-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S)-2-amino-6-(1,3-dihydro-2H-isoindol-2-yl)-6-oxohexanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[(2S,3R)-2-amino-3-ethyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]pentanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S,3S)-2-amino-3-methylpentanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
-
(2S)-1-[(4R)-4-tricyclo[3.3.1.13,7]dec-2-yl-L-prolyl]pyrrolidine-2-carbonitrile
(2S)-1-[(4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-5,5-dimethyl-L-prolyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(4S)-4-(azocan-1-ylcarbonyl)-L-prolyl]pyrrolidine-2-carbonitrile
(2S)-1-[(cyclopentylamino)acetyl]pyrrolidine-2-carbonitrile
-
(2S)-1-[(tert-butylamino)acetyl]pyrrolidine-2-carbonitrile
-
(2S)-1-[([2-[(5-nitropyridin-2-yl)amino]ethyl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
(2S)-1-[3-([2-[(5-nitropyridin-2-yl)amino]ethyl]amino)propanoyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[3-methyl-5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[3-methyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[3-methyl-5-[(2R)-2-methylpyrrolidin-1-yl]-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-(1,3-thiazolidin-3-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-(4-pyridin-4-ylpiperazin-1-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-oxo-5-[4-(trifluoroacetyl)piperazin-1-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[(2R)-2-(methoxyamino)pyrrolidin-1-yl]-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[2-(4-fluorophenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-6-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[5-[6,7-dimethoxy-1-(1-methylethyl)-3,4-dihydroisoquinolin-2(1H)-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[N-[3-(1,3-dihydro-2H-isoindol-2-yl)-1,1-dimethyl-3-oxopropyl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[N-[4-(1,3-dihydro-2H-isoindol-2-yl)-2-methyl-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(1R,3S,5R,7R)-tricyclo[3.3.1.13,7]dec-2-ylamino]acetyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(1R,5R)-tricyclo[3.3.1.13,7]dec-2-ylamino]acetyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-(2-ethyl-4-hydroxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-(2-hydroxyethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-(2-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,4,6-trimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-(3-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethoxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-(4-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-cyclohexylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4R)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-(azepan-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-(azetidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-(hydroxymethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-allylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-isobutylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S)-4-propylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S,5S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S,5S)-4-(azetidin-1-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile
(2S)-1-[[(3R,4R)-4-amino-1-(3-cyano-4-fluorobenzyl)pyrrolidin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
-
(2S)-1-[[(3R,4R)-4-amino-1-(4-cyano-3-methylbenzyl)pyrrolidin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(3R,4R)-4-amino-1-(4-cyanobenzyl)pyrrolidin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
-
(2S)-1-[[(3R,4R)-4-amino-1-(quinolin-3-ylmethyl)pyrrolidin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
-
(2S)-2-(1-adamantyl)-2-amino-N-(1-cyanoethyl)acetamide
-
-
(2S)-2-(1-adamantyl)-2-amino-N-(cyanomethyl)-N-cyclopropylacetamide
-
-
(2S)-2-(1-adamantyl)-2-amino-N-(cyanomethyl)-N-ethylacetamide
-
-
(2S)-2-(1-adamantyl)-2-amino-N-(cyanomethyl)-N-methylacetamide
-
-
(2S)-2-(1-adamantyl)-2-amino-N-(cyanomethyl)-N-propylacetamide
-
-
(2S)-2-(1-adamantyl)-N-allyl-2-amino-N-(cyanomethyl)acetamide
-
-
(2S)-2-(4-[[(1-[(3S)-3-amino-4-[2,5-difluoro-4-(trifluoromethyl)phenyl]butanoyl]-L-prolyl)amino]methyl]phenoxy)-3-methylbutanoic acid
-
(2S)-2-(4-[[(1-[(3S)-3-amino-4-[2-fluoro-4-(trifluoromethyl)phenyl]butanoyl]-L-prolyl)amino]methyl]phenoxy)-3-methylbutanoic acid
-
(2S)-2-(4-[[(1-[(3S)-3-amino-4-[2-fluoro-5-(trifluoromethoxy)phenyl]butanoyl]-L-prolyl)amino]methyl]phenoxy)-3-methylbutanoic acid
-
(2S)-2-(4-[[(1-[(3S)-3-amino-4-[2-fluoro-5-(trifluoromethyl)phenyl]butanoyl]-L-prolyl)amino]methyl]phenoxy)-3-methylbutanoic acid
-
(2S)-2-(4-[[([(4R)-3-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-1,3-thiazolidin-4-yl]carbonyl)amino]methyl]phenyl)-3-methylbutanoic acid
-
(2S)-2-amino-N-(1-cyanoethyl)-3,3-dimethylbutanamide
-
-
(2S)-2-amino-N-(1-cyanoethyl)-N,3,3-trimethylbutanamide
-
-
(2S)-2-amino-N-(cyanomethyl)-2-(3,5-dihydroxy-1-adamantyl)-N-methylacetamide
-
-
(2S)-2-amino-N-(cyanomethyl)-2-(3-hydroxy-1-adamantyl)-N-methylacetamide
-
-
(2S)-2-amino-N-(cyanomethyl)-N,3,3-trimethylbutanamide
-
-
(2S)-2-amino-N-(cyanomethyl)-N,3-dimethylbutanamide
-
-
(2S)-2-amino-N-(cyanomethyl)-N-cyclobutyl-3,3-dimethylbutanamide
-
-
(2S)-2-amino-N-(cyanomethyl)-N-cyclopropyl-3,3-dimethylbutanamide
-
-
(2S)-2-amino-N-(cyanomethyl)-N-ethyl-2-(3-hydroxy-1-adamantyl)acetamide
-
-
(2S)-2-amino-N-(cyanomethyl)-N-ethyl-3,3-dimethylbutanamide
-
-
(2S)-2-[2-[([1-[(2S)-2-amino-2-cyclohexylacetyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
-
(2S)-2-[4-[([1-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
-
-
(2S)-2-[4-[([1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
-
(2S)-2-[4-[([1-[(3S)-3-amino-4-(2,5-difluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
-
(2S)-2-[4-[([1-[(3S)-3-amino-4-(2-chloro-4-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
-
(2S)-2-[4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
-
(2S)-2-[4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]propanoic acid
-
(2S)-2-[4-[([1-[(3S)-3-amino-4-(3,4-difluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
-
(2S)-2-[4-[([1-[(3S)-3-amino-4-(5-chloro-2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
-
(2S)-2-[4-[([1-[(3S)-3-amino-4-(5-fluoro-2-methylphenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
-
(2S)-2-[4-[([1-[(3S)-3-amino-4-(pentafluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
-
(2S)-2-[4-[([1-[(3S)-3-amino-4-phenylbutanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
-
(2S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxopropan-2-amine
-
(2S)-3-methyl-1-oxo-1-pyrrolidin-1-ylbutan-2-amine
-
-
(2S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoropropan-2-aminium
-
-
(2S)-5-(1,3-dihydro-2H-isoindol-2-yl)-1,5-dioxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine
-
-
(2S)-N-allyl-2-amino-N-(cyanomethyl)-3,3-dimethylbutanamide
-
-
(2S)-{((3-Hydroxyadamantan-1-yl)amino) acetyl}pyrrolidin-2-carbonitrile
-
vldagliptin is rapidly and well absorbed with an estimated absolute bioavailability of 85%. Two possible sites of absorption are identified, and the absorption rates are slower than the elimination rate, indicating a flip-flop phenomenon after oral dosing
(2S,3R)-1-cyclopentylidene-1-fluoro-3-(3-[4-[(trifluoromethyl)sulfonyl]phenyl]-1,2,4-oxadiazol-5-yl)butan-2-aminium
-
-
(2S,3R)-1-cyclopentylidene-1-fluoro-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]butan-2-aminium
-
-
(2S,3R)-1-cyclopentylidene-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-fluorobutan-2-aminium
-
-
(2S,3R)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-3-methyl-1-oxopentan-2-amine
-
-
(2S,3R)-3-(3-[2-chloro-4-[(methylsulfonyl)amino]phenyl]-1,2,4-oxadiazol-5-yl)-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-(4-bromo-2-chlorophenyl)-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(ethylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R)-3-[3-[2-chloro-4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
-
-
(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
(2S,3S)-1-oxo-1-pyrrolidin-1-yl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]butan-2-amine
-
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-(4-pyridin-4-ylphenyl)butan-2-amine
-
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-phenylbutan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[2'-(trifluoromethyl)biphenyl-4-yl]butan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[3'-(1H-1,2,4-triazol-3-yl)biphenyl-4-yl]butan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[3'-(1H-tetrazol-1-yl)biphenyl-4-yl]butan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[3'-(1H-tetrazol-5-yl)biphenyl-4-yl]butan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4'-(trifluoromethyl)biphenyl-4-yl]butan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4-(trifluoromethyl)phenyl]butan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(2'-methoxybiphenyl-4-yl)-1-oxobutan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(2'-methylbiphenyl-4-yl)-1-oxobutan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4'-methoxybiphenyl-4-yl)-1-oxobutan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4'-methylbiphenyl-4-yl)-1-oxobutan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-methoxyphenyl)-1-oxobutan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl](methyl)amino]cyclohexyl)-1-oxobutan-2-aminium
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl]amino]cyclohexyl)-1-oxobutan-2-aminium
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[3'-(1,3,4-oxadiazol-2-yl)biphenyl-4-yl]-1-oxobutan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[3'-(methylsulfonyl)biphenyl-4-yl]-1-oxobutan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4'-(methylsulfonyl)biphenyl-4-yl]-1-oxobutan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4-(methylthio)phenyl]-1-oxobutan-2-amine
-
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4-fluoro-2-(trifluoromethyl)phenyl]-1-oxobutan-2-amine
-
(2S,3S)-2-amino-1-((1S,5S)-2-azabicyclo[3.1.0]hexan-2-yl)-3-methylpentan-1-one
-
-
(2S,3S)-2-amino-3-methyl-1-(thiazolidin-3-yl)pentan-1-one
-
-
(2S,3S)-3-(2',4'-difluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(2',5'-difluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(2'-chlorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(2'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(2,4-difluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(2-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(2-fluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(3',4'-difluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(3',5'-difluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(3,4-difluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(3,5-difluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(3-chloro-4-fluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(3-chlorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(3-fluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-4-pyrrolidin-1-ylbutan-2-amine
-
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-5-pyrrolidin-1-ylpentan-2-amine
-
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
(2S,3S)-3-(4-bromophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
(2S,3S)-3-(4-chloro-2-fluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(4-fluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
(2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
(2S,3S)-3-(4-[[(4-fluorophenyl)carbonyl](methyl)amino]phenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
(2S,3S)-3-amino-2-(2',4'-difluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
-
(2S,3S)-3-amino-2-(2',5'-difluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
-
(2S,3S)-3-amino-2-(3',4'-difluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
-
(2S,3S)-3-amino-2-(3'-ethynylbiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3R)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutan-1-ol
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanamide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanoic acid
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N',N'-dimethyl-4-oxobutanehydrazide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N-(1-methylethyl)-4-oxobutanamide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N-(2-hydroxyethyl)-4-oxobutanamide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N-methoxy-N-methyl-4-oxobutanamide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N-methyl-4-oxobutanamide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-morpholin-4-yl-4-oxobutanamide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxo-4-(1,3-thiazolidin-3-yl)butanamide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxo-4-piperidin-1-ylbutanamide
-
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxo-4-pyrrolidin-1-ylbutanamide
-
(2S,3S)-3-amino-4-(1,1-dioxido-1,3-thiazolidin-3-yl)-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxobutanamide
-
(2S,3S)-3-amino-4-(3,3-difluoroazetidin-1-yl)-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxobutanamide
-
(2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxobutanamide
-
(2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide
-
a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
(2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]pyridin-6-ylphenyl)butanamide
-
-
(2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(trans-4-[1,2,4]triazolo[1,5-a]pyridin-6-ylcyclohexyl)butanamide
-
-
(2S,3S)-3-amino-4-(3-fluoroazetidin-1-yl)-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxobutanamide
-
(2S,3S)-3-amino-4-aziridin-1-yl-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxobutanamide
-
(2S,3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-2-[3'-(methylsulfonyl)biphenyl-4-yl]-4-oxobutanamide
-
(2S,3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-(4-pyridin-3-ylphenyl)butanamide
-
(2S,3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-(4-pyridin-4-ylphenyl)butanamide
-
(2S,3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-[3'-(2H-tetrazol-2-yl)biphenyl-4-yl]butanamide
-
(2S,3S)-3-amino-N,N-diethyl-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanamide
-
(2S,3S)-3-amino-N-(3,4-dihydro-2H-tetrazol-2-yl)-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanamide
-
(2S,3S)-3-amino-N-cyclopropyl-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanamide
-
(2S,3S)-3-amino-N-ethyl-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanamide
-
(2S,3S)-3-amino-N-ethyl-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N-methyl-4-oxobutanamide
-
(2S,3S)-3-biphenyl-4-yl-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-methyl-1-oxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine
-
(2S,3S)-3-methyl-1-oxo-1-pyrrolidin-1-ylpentan-2-amine
-
-
(2S,3S)-3-[3'-(5-cyclopropyl-2,3-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
-
-
(2S,3S)-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
-
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
-
-
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
-
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
-
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-5-hydroxy-1-oxopentan-2-aminium
-
-
(2S,3S)-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
-
-
(2S,3S)-3-[4-(3-chloropyridin-4-yl)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
-
(2S,3S)-3-[4-(acetylamino)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
(2S,3S)-3-[4-[(cyclopropylcarbonyl)(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
(2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
(2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
(2S,3S)-3-[4-[acetyl(methyl)amino]phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
(2S,3S)-3-[4-[acetyl(methyl)amino]phenyl]-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
-
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-3-[4-[(phenylsulfonyl)amino]phenyl]butan-2-aminium
-
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[methyl[(4-methylphenyl)carbonyl]amino]phenyl)-1,4-dioxobutan-2-aminium
-
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[methyl[(4-methylphenyl)sulfonyl]amino]phenyl)-1,4-dioxobutan-2-aminium
-
(2S,3S)-4-(dimethylamino)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
(2S,3S)-4-(dimethylamino)-3-(4-[[(3-fluorophenyl)carbonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
(2S,3S)-4-(dimethylamino)-3-(4-[[(4-fluorophenyl)carbonyl](methyl)amino]phenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
-
(2S,3S)-4-azetidin-1-yl-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-amine
-
(2S,3S)-4-cyclopropyl-3-[3-[2-fluoro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
-
-
(2S,3S)-9,10-dimethoxy-3-(3-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-3-(1,1-dioxido-1,2-thiazinan-2-yl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-3-(2,5-dimethylphenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-3-(3,4-dimethylphenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-3-(3-chlorophenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-3-(3-cyclopropylphenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-3-(3-ethylphenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-3-butyl-9,10-dimethoxy-1,2,3,4,6,7-hexahydro-11bH-pyrido[2,1-a]isoquinoline-2,11b-diamine
-
-
(2S,3S,11bS)-3-butyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-3-[3-(fluoromethyl)phenyl]-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-3-[4-(fluoromethyl)pyridin-2-yl]-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-9,10-dimethoxy-3-(3-methoxyphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-9,10-dimethoxy-3-(3-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-9,10-dimethoxy-3-(4-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-9,10-dimethoxy-3-(4-methylpyridin-2-yl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-9,10-dimethoxy-3-phenyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-9,10-dimethoxy-3-pyridin-2-yl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,11bS)-9,10-dimethoxy-3-[3-(propan-2-yl)phenyl]-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-ethyl-N,N-dimethylpyrrolidine-3-carboxamide
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N,2-dimethylpyrrolidine-3-carboxamide
(2S,4R)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
-
-
(2S,4R)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-((2S)-2-amino-3-methylpentanoyl)-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-(N-1-adamantylglycyl)-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-(N-2-adamantylglycyl)-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-(N-cyclobutylglycyl)-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-(N-cyclooctylglycyl)-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-(N-cyclopentylglycyl)-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-(N-cyclopropylglycyl)-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-(N-[2-[(5-chloropyridin-2-yl)amino]ethyl]-glycyl)-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-(O-benzyl-L-threonyl)-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-L-alloisoleucyl-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[(2S)-2-amino-2-cyclohexylacetyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile
(2S,4S)-1-[N-(tert-butyl)glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[N-[(2E)-1,1-dimethyl-3-phenylprop-2-en-1-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[N-[1-(1-benzofuran-2-yl)-1-methylethyl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[N-[2-(3,4-dimethoxyphenyl)ethyl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[N-[2-(diethylamino)-1,1-dimethylethyl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[N-[4-(3,6-dihydropyridin-1(2H)-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
(2S,4S)-1-[N-[4-(7-azabicyclo[2.2.1]hept-7-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
(2S,4S)-1-[N-[4-(azepan-1-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
(2S,4S)-1-[O-(tert-butyl)-L-threonyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[[(3S)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(N-isopropylglycyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(N-methyl-L-isoleucyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[(2R)-2-methylpyrrolidin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[4-(methylsulfonyl)piperazin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
(2S,4S)-4-fluoro-1-(N-[2-[(4-cyanobenzyl)amino]-1,1-dimethylethyl]glycyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(N-[2-[(5-cyanopyridin-2-yl)-amino]ethyl]glycyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(N-[4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
(2S,4S)-4-fluoro-1-(O-methyl-L-threonyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-([[2-methyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile
(2S,4S)-4-fluoro-1-L-valyl-pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[(3S)-1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-fluoropyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
(2S,4S)-4-fluoro-1-[([4-[(3S)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
(2S,4S)-4-fluoro-1-[N-(1-methyl-1-pyridin-2-ylethyl)glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-(2-hydroxy-1,1-dimethylethyl)glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-(2-methoxy-1,1-dimethylethyl)glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-(3-hydroxy-1-adamantyl)-glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-(3-isopropoxypropyl)glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-(3-methoxy-1-adamantyl)-glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-(5-hydroxy-2-adamantyl)-glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[1-(2-furyl)-1-methylethyl]-glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[1-(hydroxymethyl)cyclopentyl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[1-methyl-1-(2-thienyl)-ethyl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-(pyridin-2-ylamino)ethyl]-glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(4-methylpiperazin-1-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(morpholin-4-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(4-oxopiperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(piperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile
(2S,4S)-4-fluoro-1-[[(3S)-7-hydroxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[[(3S)-7-methoxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-N-ethyl-5-methylpyrrolidine-2-carboxamide
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-prop-2-yn-1-ylpyrrolidine-2-carboxamide
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-propylpyrrolidine-2-carboxamide
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-N,5-dimethylpyrrolidine-2-carboxamide
(2S,4S,5S)-N-(cyanomethyl)-N-cyclopropyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidine-2-carboxamide
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
(2S,4S,5S)-N-allyl-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
(2S,4S,5S)-N4-benzyl-N2-(cyanomethyl)-N2-ethyl-5-methylpyrrolidine-2,4-dicarboxamide
(2S,5R)-1-[(2R)-2-amino-2-cyclohexylacetyl]-5-ethynylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[(2R)-2-amino-2-cyclopentylacetyl]-5-ethynylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[(2R)-2-amino-2-cyclopentylacetyl]-5-methylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[(2R)-2-amino-2-cyclopentylacetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[(2R)-2-amino-2-cyclopentylacetyl]-5-vinylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[(2R)-2-amino-4-methylpentanoyl]-5-ethynylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[(2R)-2-amino-4-methylpentanoyl]-5-methylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[(2S)-2-amino-2-cyclopentylacetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
(2S,5R)-1-[(cyclohexylamino)acetyl]-5-ethynylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[(cyclopentylamino)acetyl]-5-ethynylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[(cyclopentylamino)acetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[(tert-butylamino)acetyl]-5-ethynylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[N-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)glycyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
-
(2S,5R)-1-[[(cis-1-ethyl-4-hydroxycyclohexyl)amino]acetyl]-5-ethynylpyrrolidine-2-carbonitrile
-
(2S,5S)-1-[(cyclopentylamino)acetyl]-5-methylpyrrolidine-2-carbonitrile
-
(3'S,5'S)-5'-(1,3-thiazolidin-3-ylcarbonyl)-1,3'-bipyrrolidine
(3,3-difluoro-pyrrolidin-1-yl)-[(2S,4R)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin)-2-yl]-methanone
-
(3,3-difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl)-piperazin-1-yl)-pyrrolidin-2-yl]-methanone
PF-00734200, potent, selective, orally active dipeptidyl peptidase IV inhibitor
(3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]phenyl)methanol
-
-
(3R)-1-[(1R)-1-(dihydroxyboranyl)ethyl]-2-oxopyrrolidin-3-aminium
-
-
(3R)-1-[6-[(3R,4R)-3-amino-4-(2,4,5-trifluorophenyl)piperidin-1-yl]pyrimidin-4-yl]pyrrolidin-3-ol
-
(3R)-3-amino-1-(2-cyclopropyl-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-(2-phenyl-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-(3-cyclopropyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-(3-ethyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-(5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-diaminophosphinyl-2-piperidinone
-
IC50: 46 nM
(3R)-3-amino-1-[(2S)-2-([[2-(trifluoromethyl)pyrimidin-4-yl]oxy]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(3R)-3-amino-1-[(2S)-2-([[4-(trifluoromethyl)pyrimidin-2-yl]amino]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(3R)-3-amino-1-[(2S)-2-([[6-(trifluoromethyl)pyridin-3-yl]amino]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(3R)-3-amino-1-[(2S)-2-[(cyclopropylmethoxy)methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(3R)-3-amino-1-[(2S)-2-[(pyrimidin-2-ylamino)methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(3R)-3-amino-1-[(2S)-2-[[(5-fluoropyridin-2-yl)amino]methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(3R)-3-amino-1-[(2S)-2-[[(5-fluoropyrimidin-2-yl)amino]methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(3R)-3-amino-1-[(4R)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(4R)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(4R)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(4R)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(4S)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(4S)-1-methyl-4-propyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(4S)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(4S)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(5R)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(5S)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(6R)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(6S)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-2-(trifluoromethyl)-8-[4-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-8-(1H-1,2,4-triazol-1-ylmethyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-8-(4-fluorobenzyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-8-(cyclopropylmethyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-8-(prop-2-en-1-yl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-8-methyl-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8R)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8S)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8S)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8S)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8S)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8S)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8S)-8-(prop-2-en-1-yl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8S)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8S)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8S)-8-methyl-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[(8S)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[2,3-bis(trifluoromethyl)-4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl]-4-(2,5-difluorophenyl)butan-1-one
-
(3R)-3-amino-1-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[2-cyclopropyl-3-(trifluoromethyl)-4,7-dihydrofuro[2,3-c]pyridin-6(5H)-yl]-4-(2,5-difluorophenyl)butan-1-one
-
(3R)-3-amino-1-[3-(difluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
(3R)-3-amino-4-(2,5-difluorophenyl)-1-(2-phenyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl)butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-(3-methyl-1,2,4-oxadiazol-5-yl)butan-1-one
-
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[(4R)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[(4S)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[(8R)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[1-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[1-(4-fluorobenzyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[1-(4-fluorophenyl)-3-methyl-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[1-ethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[1-methyl-3-(2,2,2-trifluoroethyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[1-methyl-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[1-methyl-3-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-2,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-(4-fluorophenyl)-1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-(4-fluorophenyl)-3-(trifluoromethyl)-4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-(4-fluorophenyl)-6,7-dihydro[1,3]thiazolo[4,5-c]pyridin-5(4H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-(trifluoromethyl)-6,7-dihydro[1,3]thiazolo[4,5-c]pyridin-5(4H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-methyl-3-(2,2,2-trifluoroethyl)-2,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-methyl-3-(trifluoromethyl)-2,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-methyl-3-(trifluoromethyl)-2,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-methyl-3-(trifluoromethyl)-4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-[4-(methylsulfanyl)phenyl]-3-(trifluoromethyl)-4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-[4-(methylsulfonyl)phenyl]-3-(trifluoromethyl)-4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-[4-(methylsulfonyl)phenyl]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridin-5(4H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[2-[4-(trifluoromethyl)phenyl]-6,7-dihydro[1,3]thiazolo[4,5-c]pyridin-5(4H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(2,2,2-trifluoroethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(2,5-difluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(4-fluorobenzyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(4-fluorophenyl)-1-methyl-1,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(4-fluorophenyl)-2-methyl-2,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(4-fluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(hydroxymethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(pyridin-4-yl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(trifluoromethyl)-2-[4-(trifluoromethyl)phenyl]-4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(trifluoromethyl)-4,5-dihydro[1,2]oxazolo[3,4-c]pyridin-6(7H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-(trifluoromethyl)-6,7-dihydro[1,2]oxazolo[4,3-c]pyridin-5(4H)-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-ethyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-methyl-2-(4-fluorophenyl)-2,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl]butan-1-one
-
(3R)-3-amino-4-(2,5-difluorophenyl)-1-[3-methyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-1-one
-
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,3-dimethyl-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-(2-hydroxyethyl)-3-methyl-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-cyclopropyl-3-methyl-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-tert-butyl-3-methyl-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-[2-(benzyloxy)ethyl]-3-methyl-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-[(2-methylpropan-2-yl)oxymethyl]piperazin-2-one
i.e. evogliptin
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-1-cyclopropyl-3-methyl-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-1-ethyl-3-methyl-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-1-(2-oxopropyl)-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
-
(3R)-4-[(3S)-3-amino-4-(2-oxopiperidin-1-yl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
-
(3R)-4-[(3S)-3-amino-4-(2-oxopiperidin-1-yl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
-
(3R,4R)-1-(1,3-benzothiazol-2-ylcarbonyl)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
-
(3R,4R)-1-(1,3-benzothiazol-6-ylcarbonyl)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
-
(3R,4R)-1-(2-methyl-3-oxo-2,3-dihydro[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-(2-methyl-4-oxo-3,4-dihydropyrido[3,2-d]pyrimidin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-(2-methyl-4-oxo-4H-pyrimido[1,2-b]pyridazin-7-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
pharmacokinetic properties
(3R,4R)-1-(2-naphthoyl)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
-
(3R,4R)-1-(2-oxo-2H-pyrimido[1,2-b]pyridazin-7-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
pharmacokinetic properties
(3R,4R)-1-(3,4-difluorobenzyl)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
-
(3R,4R)-1-(3-ethyl[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-(3-methyl[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
-
(3R,4R)-1-(3-methyl[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
pharmacokinetic properties
(3R,4R)-1-(4-cyanopyridin-2-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-(4-cyclopropylpyrido[3,2-d]pyrimidin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-(6-phenylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
(3R,4R)-1-(6-piperidin-1-ylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
(3R,4R)-1-(6-pyrrolidin-1-ylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
(3R,4R)-1-(isoquinolin-3-ylcarbonyl)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
-
(3R,4R)-1-isoquinolin-1-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-phenyl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-pteridin-7-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-pyrazino[2,3-b]pyrazin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-pyridin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-pyridin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-pyridin-4-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-pyrido[2,3-b]pyrazin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-pyrido[2,3-b]pyrazin-6-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-quinolin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-quinoxalin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-[(5-chloro-1-benzofuran-2-yl)carbonyl]-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
-
(3R,4R)-1-[1,2,4]triazolo[4,3-a]pyrimidin-7-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
pharmacokinetic properties
(3R,4R)-1-[1,2,4]triazolo[4,3-b]pyridazin-6-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-[1-methyl-1-(4-nitrophenyl)ethyl]-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
-
(3R,4R)-1-[2-(trifluoromethyl)imidazo[1,2-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-[2-(trifluoromethyl)[1,2,4]triazolo[1,5-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-[3-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-[3-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-[3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-[4-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-[4-[3-(methylsulfonyl)phenyl]-1,3,5-triazin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
(3R,4R)-1-[5-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-[6-(3,3-difluoropyrrolidin-1-yl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
(3R,4R)-1-[6-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3R,4R)-1-[6-[2-(trifluoromethyl)-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
(3R,4R)-1-[6-[3-(methylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
(3R,4R)-3-amino-N-phenyl-4-(2,4,5-trifluorophenyl)piperidine-1-carboxamide
-
(3R,4R)-3-butyl-1-(3,4,5-trimethoxyphenyl)piperidin-4-amine
-
-
(3R,4R)-3-butyl-1-(3,4-dimethoxyphenyl)piperidin-4-amine
-
-
(3R,4R)-3-butyl-1-(4-methylphenyl)piperidin-4-amine
-
-
(3R,4R)-3-butyl-1-(4-phenoxyphenyl)piperidin-4-amine
-
-
(3R,4R)-3-butyl-1-(6-methoxybiphenyl-3-yl)piperidin-4-amine
-
-
(3R,4R)-3-butyl-1-naphthalen-2-ylpiperidin-4-amine
-
-
(3R,4R)-3-butyl-1-phenylpiperidin-4-amine
-
-
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-(quinolin-3-ylcarbonyl)pyrrolidin-3-amine
-
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-(quinolin-3-ylmethyl)pyrrolidin-3-amine
-
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-(quinolin-6-ylcarbonyl)pyrrolidin-3-amine
-
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-[4-(1,2,3-thiadiazol-4-yl)benzyl]pyrrolidin-3-amine
-
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-[4-(1H-1,2,4-triazol-1-yl)benzoyl]pyrrolidin-3-amine
-
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-[4-(1H-1,2,4-triazol-1-yl)benzyl]pyrrolidin-3-amine
-
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-[4-(1H-tetrazol-1-yl)benzoyl]pyrrolidin-3-amine
-
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-[4-(1H-tetrazol-1-yl)benzyl]pyrrolidin-3-amine
-
(3R,4S)-1-(6-phenylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
(3R,4S)-1-(6-pyridin-3-ylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-acetyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine
-
(3R,4S)-1-benzyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine
-
(3R,4S)-1-[4-[3-(methylsulfonyl)phenyl]-1,3,5-triazin-2-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
(3R,4S)-1-[6-(2-chlorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(2-fluorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(2-methoxyphenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(3-chlorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(3-chlorophenyl)pyrimidin-4-yl]-4-phenylpyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(3-fluorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(3-methoxyphenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(3-nitrophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(3-thienyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
(3R,4S)-1-[6-(4-chlorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(4-fluorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(4-methoxyphenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(4-methoxyphenyl)pyrimidin-4-yl]-4-phenylpyrrolidin-3-amine
-
-
(3R,4S)-1-[6-(6-methoxypyridin-3-yl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-[3-(methylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
(3R,4S)-1-[6-[3-(morpholin-4-ylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
(3R,4S)-1-[6-[3-(trifluoromethoxy)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-[3-(trifluoromethyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[6-[3-fluoro-5-(methylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-(3-fluorobenzyl)pyrrolidine-1-carboxamide
-
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-(3-methoxybenzyl)-N-methylpyrrolidine-1-carboxamide
-
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-ethyl-N-methylpyrrolidine-1-carboxamide
-
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-ethylpyrrolidine-1-carboxamide
-
(3R,4S)-4-(2,4-dichlorophenyl)-1-(6-phenylpyridin-2-yl)pyrrolidin-3-amine
-
(3R,4S)-4-(2,4-dichlorophenyl)-1-phenylpyrrolidin-3-amine
-
(3R,4S)-4-(2,4-dichlorophenyl)-1-pyridin-2-ylpyrrolidin-3-amine
-
(3R,4S)-4-(2,4-dichlorophenyl)-1-pyrimidin-2-ylpyrrolidin-3-amine
-
(3R,4S)-4-(2,4-dichlorophenyl)-1-[(4-methylphenyl)sulfonyl]pyrrolidin-3-amine
-
(3R,4S)-4-(2,4-dichlorophenyl)-1-[2-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
-
(3R,4S)-4-(2,4-dichlorophenyl)-1-[4-(3-thienyl)pyrimidin-2-yl]pyrrolidin-3-amine
-
(3R,4S)-4-(2,4-dichlorophenyl)-1-[5-(4-methoxyphenyl)pyrimidin-2-yl]pyrrolidin-3-amine
-
(3R,4S)-4-(2,4-dichlorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
-
(3R,4S)-4-(2-chloro-4,5-difluorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
-
(3R,4S)-4-(2-chloro-4-fluorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
-
(3R,4S)-4-phenyl-1-(6-phenylpyrimidin-4-yl)pyrrolidin-3-amine
-
-
(3R,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6-dimethyl-1,4-diazepan-2-one
-
-
(3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-7-(trifluoromethyl)-1,4-diazepan-2-one
-
-
(3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-(2-fluorobenzyl)-3-methyl-1,4-diazepan-2-one
-
-
(3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-ethyl-3-methyl-1,4-diazepan-2-one
-
-
(3R,S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
-
(3S)-1-oxo-5-phenyl-1-(1,3-thiazolidin-3-yl)pentan-3-amine
-
(3S)-1-[(1R)-1-(dihydroxyboranyl)ethyl]-2-oxopyrrolidin-3-aminium
-
-
(3S)-1-[6-[(3R,4R)-3-amino-4-(2,4,5-trifluorophenyl)piperidin-1-yl]pyrimidin-4-yl]pyrrolidin-3-ol
-
-
(3S)-3-amino-1-diaminophosphinyl-2-perhydroazepinone
-
IC50: 130 nM
(3S)-3-amino-1-diaminophosphinyl-2-piperidinone
-
IC50: 94 nM
(3S)-3-amino-1-diaminophosphinyl-2-pyrrolidinone
-
IC50: 11 nM
(3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-1-(3-methyl-1,2,4-oxadiazol-5-yl)-4-oxobutan-1-one
-
-
(3S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6,6-trimethyl-1,4-diazepan-2-one
-
-
(3S)-N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-fluoro-3-methylbutanamide
-
-
(3S,4R)-3-butyl-1-(3,4,5-trimethoxyphenyl)piperidin-4-amine
-
-
(3S,4R)-3-butyl-1-(3,4-dichlorophenyl)piperidin-4-amine
-
-
(3S,4R)-3-butyl-1-(3,4-dimethoxyphenyl)piperidin-4-amine
-
-
(3S,4R)-3-butyl-1-(4-methylphenyl)piperidin-4-amine
-
-
(3S,4R)-3-butyl-1-(4-phenoxyphenyl)piperidin-4-amine
-
-
(3S,4R)-3-butyl-1-(6-methoxybiphenyl-3-yl)piperidin-4-amine
-
-
(3S,4R)-3-butyl-1-(diphenylmethyl)piperidin-4-amine
-
-
(3S,4R)-3-butyl-1-cyclohexylpiperidin-4-amine
-
-
(3S,4R)-3-butyl-1-naphthalen-2-ylpiperidin-4-amine
-
-
(3S,4R)-3-butyl-1-[3-methoxy-5-(trifluoromethyl)phenyl]piperidin-4-amine
-
-
(3S,4R)-3-butyl-1-[4-chloro-3-(trifluoromethyl)phenyl]piperidin-4-amine
-
-
(3S,4S)-1-pyrazin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3S,4S)-1-pyridazin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3S,4S)-1-pyrimidin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3S,4S)-1-pyrimidin-4-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
-
-
(3S,4S)-5-(dimethylamino)-2-[(3S)-3-fluoropyrrolidin-1-yl]-5-oxo-4-(4-[1,2,4]triazolo[1,5-a]pyridin-6-ylphenyl)pent-1-en-3-aminium
-
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl 4-cyanobenzoate
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl benzoate
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-diethylpyrrolidine-3-carboxamide
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-dimethylpyrrolidine-3-carboxamide
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N-methylpyrrolidine-3-carboxamide
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethylpyrrolidine-3-carboxamide
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-methylpyrrolidine-3-carboxamide
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-propylpyrrolidine-3-carboxamide
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidine-3-carboxamide
(3S,5S)-N-(2-phenylethyl)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide
-
-
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
(3S,5S)-N-(4-methoxyphenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
(3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
(3S,5S)-N-benzyl-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide
-
-
(3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
(3S,5S)-N-phenyl-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide
-
-
(3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6-dimethyl-1,4-diazepan-2-one
-
-
(3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-ethyl-6-methyl-1,4-diazepan-2-one
-
-
(3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-6-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
-
(3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6-dimethyl-1,4-diazepan-2-one
-
-
(3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-ethyl-6-methyl-1,4-diazepan-2-one
-
-
(3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-6-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
-
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,7-dimethyl-1,4-diazepan-2-one
-
-
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2-fluorobenzyl)-7-methyl-1,4-diazepan-2-one
-
-
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
-
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(2-methylbenzyl)-1,4-diazepan-2-one
-
-
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(pyridin-2-ylmethyl)-1,4-diazepan-2-one
-
-
(3S,7S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,7-dimethyl-1,4-diazepan-2-one
-
-
(4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]phenyl)ethynamine
(4-[[([(4R)-3-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-1,3-thiazolidin-4-yl]carbonyl)amino]methyl]phenyl)acetic acid
-
(4-[[([(4R)-3-[(3R)-3-amino-4-phenylbutanoyl]-1,3-thiazolidin-4-yl]carbonyl)amino]methyl]phenyl)acetic acid
-
(4R)-3-([1-[1-(2-phenoxyethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(4-cyanobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(4-fluorobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(4-nitrobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-([2-ethyl-1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(2'-cyanobiphenyl-4-yl)methyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(4-chlorophenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(4-methoxyphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[(1-[1-[(4-methylphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[[1-(1-benzylpiperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[[1-(1-[3-[2-(aminooxy)cyclopropyl]propyl]piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R)-3-[[1-(piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
-
-
(4R,5R)-5-amino-1-(2-phenylethyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
(4R,5R)-5-amino-1-(2-pyridin-4-ylethyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
(4R,5R)-5-amino-1-(3-phenylpropyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
(4R,5R)-5-amino-1-(morpholin-4-ylmethyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
(4R,5R)-5-amino-1-benzyl-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
(4R,5R)-5-amino-1-benzyl-4-(2-chlorophenyl)piperidin-2-one
-
(4R,5R)-5-amino-1-[(2S)-2-phenylpropyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
(4R,5R)-5-amino-1-[2-(1,3-benzodioxol-5-yl)ethyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
(4R,5R)-5-amino-1-[2-[3-(methylsulfonyl)phenyl]ethyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
(4R,5R)-5-amino-1-[2-[4-(methylsulfonyl)phenyl]ethyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
(4R,5R)-5-amino-4-(2-chlorophenyl)-1-(cyclohexylmethyl)piperidin-2-one
-
(4R,5R)-5-amino-4-(2-chlorophenyl)-1-phenylpiperidin-2-one
-
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxo-N-phenylpentanamide
-
-
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-N-cyclopentyl-5-oxopentanamide
-
-
(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-[(3R)-3-aminopiperidin-1-yl]-3-(2-chlorobenzyl)-5-methyl-4-oxo-4,5-dihydro-3H-imidazo[4,5-c]quinoline-8-carboxylate
-
compound shows significantly high oral absorption and potent dipeptidyl peptidase IV inhibition in vivo and decreased Zucker fatty rats glucose levels in the oral glucose tolerance test
(6-methylpyridin-2-yl)methyl (3R,4S)-3-amino-4-(2,4-dichlorophenyl)pyrrolidine-1-carboxylate
-
(7R,8R)-2-methyl-7-(2,4,5-trifluorophenyl)-6,7,8,9-tetrahydropyrido[3',2':4,5]imidazo[1,2-a]pyridin-8-amine
-
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid (1H-benzoimidazol-2-ylmethyl)amide
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid (4-morpholin-4-ylphenyl)amide
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid (4-sulfamoyl phenyl)amide
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid 4-amino benzyl amide
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid 4-ethoxycarbonyl phenyl ester
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid 4-methoxycarbonyl benzyl ester
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid 4-methoxycarbonyl methyl phenyl ester
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid amide
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid benzyl amide
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid benzyl ester
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid phenyl amide
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid phenyl ester
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid(pyridin-2-ylmethyl)amide
-
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-4-sulfamoyl benzyl amide
-
(R)-3-amino-1-((R)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(R)-3-amino-1-((S)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(R)-3-amino-4-(2,5-difluorophenyl)-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)butan-1-one
-
-
(R)-4-([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino) benzoic acid ethyl ester
-
(R)-4-([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)benzenesulfonic acid
-
(R)-4-([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)benzoic acid
-
(R)-4-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]benzoic acid
-
(R)-4-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]benzoic acid methyl ester
-
(R)-[2-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid
-
(R)-[2-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid ethyl ester
-
(R)-[3-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]phenoxy]acetic acid
-
(R)-[3-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]phenoxy]acetic acid ethyl ester
-
(R)-[3-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid
-
(R)-[3-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid ethyl ester
-
(R)-[4-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]phenoxy]acetic acid
-
(R)-[4-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]phenoxy]acetic acid ethyl ester
-
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]-(R)-isopropyl acetic acid
-
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]-(R)-isopropyl acetic acid ethyl ester
-
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]-(S)-isopropyl acetic acid
-
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]-(S)-isopropyl acetic acid ethyl ester
-
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid
-
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid ethyl ester
-
(S)-1-(2-(2-(2-oxo-3-(3,4,5-trimethoxyphenyl)imidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(2-oxo-3-p-tolylimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(2-oxo-3-phenylimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-(2-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-(3,4-dimethoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-(3,5-dimethoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-(3-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-(3-methoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-(4-chlorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-(4-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-(4-methoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-butyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-cyclohexyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-isopropyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
(S)-1-(2-(2-(3-tert-butyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
-
-
1-(1-methyl-6-phenyl-1H-benzimidazol-7-yl)methanamine
-
1-(2-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(2-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]phenyl)ethanone
-
-
1-(3,4-dichlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(3,4-dimethoxyphenyl)-3-(3,4-dimethylphenyl)piperidin-4-amine
-
-
1-(3,4-dimethoxyphenyl)-3-(3-methoxyphenyl)piperidin-4-amine
-
-
1-(3,4-dimethoxyphenyl)-3-(3-methylphenyl)piperidin-4-amine
-
-
1-(3,4-dimethoxyphenyl)-3-(4-methylphenyl)piperidin-4-amine
-
-
1-(3,4-dimethoxyphenyl)-3-pyridin-2-ylpiperidin-4-amine
-
-
1-(3-benzyl-4-oxido-3H-imidazo[4,5-b]pyridin-2-yl)piperidin-3-aminium
-
-
1-(3-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(3-methyl-1,2,4-thiadiazol-5-yl)-4-[[(2S,3S,5S)-2-methyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]carbonyl]piperazine
-
-
1-(3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]phenyl)ethanone
-
-
1-(4-bromophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(4-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
1-(4-ethynylpyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(4-fluorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(4-methoxyphenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,4-diazepane
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(4-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]phenyl)ethanone
-
-
1-(5-chloropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(5-nitropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(6-chloro-2-isobutyl-4-phenyl-3,4-dihydroquinolin-3-yl)methanamine
-
-
1-(diphenylmethyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-(L-cyclohexylalanyl)piperidine
1-(L-cyclohexylalanyl)pyrrolidine
1-(L-isoleucyl)-1,2,5,6-tetrahydropyridine
1-(L-isoleucyl)-3(R,S)-azidopyrrolidine
1-(L-isoleucyl)-3(R,S)-chloropyrrolidine
1-(L-isoleucyl)-3(R,S)-hydroxypyrrolidine
1-(L-isoleucyl)-3-pyrroline
1-(L-isoleucyl)hexamethyleneimine
1-(L-isoleucyl)piperidine
1-(L-isoleucyl)pyrrolidine
1-(L-phenylalanyl)pyrrolidine
1-([(5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-2-yl]methyl)-3-phenylurea
-
1-benzyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-cyclohexyl-2-oxo-2-(1,3-thiazolidin-3-yl)ethanaminium 2,2,2-trifluoro-1-oxoethanide
-
1-methyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
1-phenyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-pyridin-2-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-pyridin-4-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-4,4-dimethyl-1-oxopentan-2-amine
-
-
1-[(2R)-2-[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]cyclopentyl]-2-(tricyclo[3.3.1.13,7]dec-1-ylamino)ethanone
-
-
1-[(2R)-4,4-difluoro-2-[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]cyclopentyl]-2-(tricyclo[3.3.1.13,7]dec-1-ylamino)ethanone
-
-
1-[(2R,4R)-4-fluoro-2-[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]cyclopentyl]-2-(tricyclo[3.3.1.13,7]dec-1-ylamino)ethanone
-
-
1-[(2S)-2-amino-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butyl]piperidin-2-one
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-methylpiperidin-2-one
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-5-methylpiperidin-2-one
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]azepan-2-one
-
-
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
-
-
1-[(3R)-3-amino-4-phenylbutanoyl]-N-[5-chloro-2-[2-(cyclopropylamino)-2-oxoethoxy]benzyl]-L-prolinamide
-
-
1-[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]indane-5-carbonitrile
-
1-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
-
1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-N-benzyl-L-prolinamide
-
1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-N-[4-(1H-1,2,3-triazol-4-yl)butyl]-L-prolinamide
-
1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-N-[4-(2,3-dihydro-1H-tetrazol-5-yl)butyl]-L-prolinamide
-
1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-N-[4-(trifluoromethyl)benzyl]-L-prolinamide
-
1-[(3S,4S)-4-amino-1-[4-(3,3-difluoropyrrolidin-1-yl)-1,3,5-triazin-2-yl]pyrrolidin-3-yl]-4,4-difluoropiperidin-2-one
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)phenyl]piperazine
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
1-[(4R)-4-[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]tetrahydrothiophen-3-yl]-2-(tricyclo[3.3.1.13,7]dec-1-ylamino)ethanone
-
-
1-[([2-[(5-iodopyridin-2-yl)amino]-ethyl]amino)-acetyl]-2-cyano(S)-pyrrolidine
-
competitive
1-[1-(2-chlorobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
-
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
1-[1-(2-cyanobenzyl)-5-methyl-4-oxo-4,5-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
-
-
1-[1-(2-cyanobenzyl)-6-methyl-7-oxo-3a,6,7,7a-tetrahydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
-
-
1-[1-(3-cyanobenzyl)-6-methyl-7-oxo-6,7-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
-
-
1-[1-benzyl-6-(2-chlorophenyl)-1H-benzimidazol-7-yl]methanamine
-
1-[1-methyl-6-(2-methylphenyl)-1H-benzimidazol-7-yl]methanamine
-
1-[1-[3-(cyanomethyl)benzyl]-6-methyl-7-oxo-6,7-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
-
-
1-[2-amino-3-(4-iodophenyl)propanoyl]pyrrolidine--2-carbonitrile
-
1-[3-[2-[2-cyano-(S)-pyrrolidin-1-yl]-2-oxoethylamino]-1-oxopropyl]-4-[benzothiazol-2-yl]piperazine
-
-
1-[4,9-dioxo-1-[2-(trifluoromethyl)benzyl]-4,9-dihydro-1H-naphtho[2,3-d]imidazol-2-yl]piperidin-3-aminium
-
-
1-[5-benzyl-1-(3-cyanobenzyl)-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
-
1-[5-bromo-6-(2-chlorophenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
-
1-[5-methyl-4,6-dioxo-1-[2-(trifluoromethoxy)benzyl]-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
-
1-[5-methyl-4,6-dioxo-1-[2-(trifluoromethyl)benzyl]-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
-
1-[6-(2,4-dichlorophenyl)-1-ethyl-1H-benzimidazol-7-yl]methanamine
-
1-[6-(2,4-dichlorophenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
-
1-[6-(2,4-dichlorophenyl)-1H-benzimidazol-7-yl]methanamine
-
1-[6-(2,4-difluorophenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
-
1-[6-(2-chloro-5-fluorophenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
-
1-[6-(2-chlorophenyl)-1,2-dimethyl-1H-benzimidazol-7-yl]methanamine
-
1-[6-(2-chlorophenyl)-1-methyl-1H-1,2,3-benzotriazol-7-yl]methanamine
-
1-[6-(2-chlorophenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
-
1-[6-(2-chlorophenyl)-1-methyl-2-pyridin-3-yl-1H-benzimidazol-7-yl]methanamine
-
1-[6-(2-chlorophenyl)-2-ethyl-1-methyl-1H-benzimidazol-7-yl]methanamine
-
1-[6-(2-chlorophenyl)-2-methoxy-1-methyl-1H-benzimidazol-7-yl]methanamine
-
1-[6-(2-methoxyphenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
-
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
1-[7-fluoro-6-methoxy-1-[2-(trifluoromethyl)benzyl]-1H-benzimidazol-2-yl]piperidin-3-aminium
-
-
1-[amino(cyclohexyl)acetyl]pyrrolidine-2-carbonitrile
-
-
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine
1-[[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-2-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[1,5-a]pyrazin-8-yl]methyl]cyclopropanol
-
-
2,2-bis(4-chlorophenyl)-N-[2-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-2-methylpropyl]acetamide
-
-
2-(2-[4-(4-chloro-phenyl)-piperazin-1-yl]-2-oxoethylsulfanyl)-4-hydroxy-6-phenyl-pyrimidine-5-carbonitrile
-
single dose of 10 mg/kg of the compound significantly reduces glucose excursion during oral glucose tolerance test in streptozotocin-induced diabetic rat model
2-(3-aminopiperidin-1-yl)-1-but-2-yn-1-yl-4-cyano-N-(naphthalen-1-ylmethyl)-1H-imidazole-5-carboxamide
-
-
2-(3-aminopiperidin-1-yl)-1-but-2-yn-1-yl-N-(naphthalen-1-ylmethyl)-1H-imidazole-5-carboxamide
-
-
2-(3-aminopiperidin-1-yl)-1-but-2-yn-1-yl-N-methyl-N-(naphthalen-1-ylmethyl)-1H-imidazole-5-carboxamide
-
-
2-(3-aminopiperidin-1-yl)-1-but-2-yn-1-yl-N-methyl-N-[(3-methylisoquinolin-1-yl)methyl]-1H-imidazole-5-carboxamide
-
-
2-(3-aminopiperidin-1-yl)-1-but-2-yn-1-yl-N-[(3-methylisoquinolin-1-yl)methyl]-1H-imidazole-5-carboxamide
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-(10,11-dihydrodibenzo[b,f][1,4]oxazepin-11-ylmethyl)-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-(2-oxo-2-phenylethyl)-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-(naphthalen-1-ylmethyl)-3,5-dihydro-4H-imidazo[4,5-c]pyridin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-(naphthalen-1-ylmethyl)-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(11R)-10,11-dihydrodibenzo[b,f][1,4]oxazepin-11-ylmethyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(11S)-10,11-dihydrodibenzo[b,f][1,4]oxazepin-11-ylmethyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(3-methylisoquinolin-1-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-c]pyridin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(3-methylisoquinolin-1-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(6-methyl-1,3-benzoxazol-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-7-methoxy-5-(naphthalen-1-ylmethyl)-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-7-methoxy-5-[(3-methylisoquinolin-1-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-7-methyl-5-(naphthalen-1-ylmethyl)-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-7-methyl-5-[(3-methylisoquinolin-1-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-7-methyl-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-(3-aminopiperidin-1-yl)-4-bromo-1-but-2-yn-1-yl-N-(naphthalen-1-ylmethyl)-1H-imidazole-5-carboxamide
-
-
2-(3-aminopiperidin-1-yl)-4-bromo-1-but-2-yn-1-yl-N-[(3-methylisoquinolin-1-yl)methyl]-1H-imidazole-5-carboxamide
-
-
2-(3-but-2-yn-1-yl-4-oxo-2-piperazin-1-yl-3,4-dihydro-5H-imidazo[4,5-d]pyridazin-5-yl)benzonitrile
-
-
2-(4-[(3R,5S)-5-[(3,3,4,4-tetrafluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
-
2-(4-[(3R,5S)-5-[(3,3-difluoroazetidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
-
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)-1,3-benzoxazole
-
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrazine
-
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyridine-3-carbonitrile
-
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
-
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)[1,3]oxazolo[5,4-b]pyridine
-
2-(4-[(3R,5S)-5-[(3-fluoroazetidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
-
2-(N-tert-butylglycyl-L-prolyl)-5-(1-methylcyclohexyl)-1,3,4-oxadiazole
-
-
2-(N-tert-butylglycyl-L-prolyl)-5-(2,4,6-trimethylphenyl)-1,3,4-oxadiazole
-
-
2-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methoxy)pyridine-4-carbonitrile
-
-
2-([(3S,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]carbonyl)isoindoline
-
-
2-([2-(4-aminopiperidin-1-yl)-2-oxoethyl]sulfanyl)-4-hydroxy-6-phenylpyrimidine-5-carbonitrile
-
single dose of 10 mg/kg of the compound significantly reduces glucose excursion during oral glucose tolerance test in streptozotocin-induced diabetic rat model
2-([2-[(1R,3S)-3-aminocyclohexyl]-5-benzyl-4-oxo-4,5-dihydro-3H-imidazo[4,5-c]pyridin-3-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-5-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,7-dimethoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,8-dichloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-bromo-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-fluoro-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3S)-3-aminopiperidin-1-yl]-6-fluoro-7-morpholin-4-yl-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]methyl)benzonitrile
2-([8-(3-aminopiperidin-1-yl)-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl]methyl)benzonitrile
2-([8-[(3R)-3-aminopiperidin-1-yl]-3-methyl-7-(3-methylbut-2-en-1-yl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-1-yl]methyl)benzonitrile
most potent inhibitor tested, exhibits moderate antihyperglycemic activity as compared to the standard antidiabetic drug Linagliptin in ther oral glucose tolerance test. The compound effectively improves the pathological state of diet-induced obesity mice. IC50 value with isoforms DPP-8 and DPP-9 is above 0.1 mM
2-cyanopyrrolidines
-
-
-
2-ethoxy-4-[2-(methylsulfanyl)ethyl]-1,3,2-oxazaphospholidine 2-sulfide
-
2-methyl-2-[(2-[(2S)-2-[(5-methyl-1,2,4-oxadiazol-3-yl)carbonyl]pyrrolidin-1-yl]-2-oxoethyl)amino]propanoic acid
-
-
2-tert-butyl-5-(N-tert-butylglycyl-L-prolyl)-1,3,4-oxadiazole
-
-
2-tert-butyl-5-[N-(2-hydroxy-1,1-dimethylethyl)glycyl-(4S)-4-fluoro-L-prolyl]-1,3,4-oxadiazole
2-tert-butyl-5-[N-(2-hydroxy-1,1-dimethylethyl)glycyl-L-prolyl]-1,3,4-oxadiazole
-
-
2-tert-butyl-5-[N-[2-(4-fluorophenyl)-1,1-dimethylethyl]glycyl-(4S)-4-fluoro-L-prolyl]-1,3,4-oxadiazole
-
-
2-[(2-aminoethyl)(methyl)amino]-3-but-2-yn-1-yl-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-[(2R)-2-amino-4-oxo-4-(1,3-thiazolidin-3-yl)butyl]benzonitrile
-
2-[(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-methylpyrrolidin-3-yl]-N,N-dimethylacetamide
2-[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]-1-[(2R)-2-[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]cyclopentyl]ethanone
-
-
2-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-phenylpyrazolidine-1-carboxamide
-
-
2-[(3R)-3-aminopiperidin-1-yl]-3-but-2-yn-1-yl-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-[(3R)-4-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-3-benzylpiperazin-1-yl]-N-[3-[(methylsulfonyl)amino]phenyl]acetamide
-
-
2-[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylacetamide
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
2-[(7-but-2-yn-1-yl-2-methoxy-6-oxo-8-piperazin-1-yl-6,7-dihydro-1H-purin-1-yl)methyl]benzonitrile
-
-
2-[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
2-[(8S)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
2-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)amino]pyridine-3-carbonitrile
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-fluorobenzyl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-methoxyethyl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4,5-dimethyl-1,3-thiazol-2-yl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(pyrimidin-2-yl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(tricyclo[3.3.1.13,7]dec-1-yl)acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclohexylacetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[2-(thiophen-2-yl)ethyl]acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[3-(propan-2-yloxy)propyl]acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[4-(trifluoromethyl)phenyl]acetamide
-
-
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
2-[4-[(2S)-2-amino-3-phenylpropyl]-3-benzylpiperazin-1-yl]-N-[3-[(methylsulfonyl)amino]phenyl]acetamide
-
-
2-[4-[(3R,5S)-5-(azetidin-1-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
-
2-[4-[(3R,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
-
2-[4-[(3R,5S)-5-[[(3R)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
-
2-[4-[(3R,5S)-5-[[(3R,4R)-3,4-difluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
-
2-[4-[(3R,5S)-5-[[(3R,4S)-3,4-difluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
-
2-[4-[(3R,5S)-5-[[(3S)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
-
2-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
2-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzonitrile
-
-
2-[7-(aminomethyl)-1-methyl-1H-benzimidazol-6-yl]benzamide
-
2-[7-(aminomethyl)-1-methyl-1H-benzimidazol-6-yl]phenol
-
2-[7-(aminomethyl)-6-(2-chlorophenyl)-1H-benzimidazol-1-yl]ethanol
-
2-[N-tert-butylglycyl-(4S)-4-fluoro-L-prolyl]-5-(1,1-dimethylpropyl)-1,3,4-oxadiazole
-
-
2-[N-tert-butylglycyl-(4S)-4-fluoro-L-prolyl]-5-cyclohexyl-1,3,4-oxadiazole
-
-
2-[[(2S)-2-aminopropyl](methyl)amino]-3-but-2-yn-1-yl-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
2-[[(3S)-3-[[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]carbonyl]-1,2,3,4-tetrahydroisoquinolin-7-yl]oxy]acetamide
-
-
2-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
-
2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]-5-(trifluoromethyl)isoindoline
-
-
2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
-
2-[[(3S,5S)-5-[[(3R)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]carbonyl]isoindoline
-
-
2-[[(3S,5S)-5-[[(3S)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]carbonyl]isoindoline
-
-
2-[[2-(3-aminopiperidin-1-yl)-4-oxoquinazolin-3(4H)-yl]methyl]benzonitrile
-
-
2-[[2-(3-aminopiperidin-1-yl)-5,6-dimethyl-4,7-dioxo-4,5,6,7-tetrahydro-1H-imidazo[4,5-d]pyridazin-1-yl]methyl]benzonitrile
-
-
2-[[2-(3-aminopiperidin-1-yl)-5-methyl-4,6-dioxo-5,6-dihydropyrrolo[3,4-d]imidazol-1(4H)-yl]methyl]benzonitrile
-
-
3,4-dichloroisocoumarine
-
1.0 mM, 97% inhibition
3-((2S,4S)-4-anilino-2-pyrrolidinylcarbonyl)-1,3-thiazolidine
3-(1-amino-2-oxo-2-pyrrolidin-1-ylethyl)tricyclo[3.3.1.13,7]decan-1-ol
-
-
3-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-yl)-1,2,4-oxadiazolidin-5-one
-
3-(aminomethyl)-2-isobutyl-4-phenylisoquinolin-1(2H)-one
-
-
3-(aminomethyl)-4-(2,4-dichlorophenyl)-7,8-dimethoxy-5H-indeno[1,2-b]pyridin-2-amine
-
-
3-(aminomethyl)-4-(2,4-dichlorophenyl)quinolin-2-amine
-
-
3-(N-tert-butylglycyl-L-prolyl)-5-(2-methylcyclohexyl)-1,2,4-oxadiazole
-
-
3-([2-[(2S)-2-cyano-4,4-difluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[3-(trifluoromethyl)phenyl]cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[4-(trifluoromethyl)phenyl]cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(2,4-di-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-methoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,5-di-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-phenylcyclopropyl]butanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]-amino)-3-methyl-N-[trans-2-(4-methyl-1,3-thiazol-5-yl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-(pyridin-2-yl)butanamide
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
-
15 nM DPP-IV inhibitor with high selectivity over DPP-II, DPP8 and FAP
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-ethoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-fluorophenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-methoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(4-methoxyphenyl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-phenylcyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(pyridin-3-yl)cyclopropyl]butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-cyclopentyl-3-methylbutanamide
3-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)benzoic acid
-
3-bromo-4-([(2R,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-2-yl]methoxy)benzoic acid
-
3-but-2-yn-1-yl-2-(1,4-diazepan-1-yl)-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
3-but-2-yn-1-yl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
-
-
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
3-butyl-1-(5,6,7,8-tetrahydronaphthalen-1-yl)piperidin-4-amine
-
-
3-butyl-1-(diphenylmethyl)piperidin-4-amine
-
-
3-butyl-1-naphthalen-1-ylpiperidin-4-amine
-
-
3-butyl-1-[3-methoxy-5-(trifluoromethyl)phenyl]piperidin-4-amine
-
-
3-butyl-1-[4-chloro-3-(trifluoromethyl)phenyl]piperidin-4-amine
-
-
3-butyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
-
-
3-chloro-4-([(2R,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-2-yl]methoxy)benzoic acid
-
3-L-prolyl-1,3-thiazolidine
3-N-[(2S,3S)-2-amino-3-methylpentanoyl]-1,3-thiazolidine
-
in genetically susceptible animals, inhibition of DPP IV increases arterial blood pressure via Y1 receptors when elevated blood pressure is reduced with antihypertensive drugs provided that the sympathetic nervous system is functional
3-[(2R)-2-amino-4-oxo-4-(1,3-thiazolidin-3-yl)butyl]benzonitrile
-
3-[(2S)-pyrrolidin-2-ylcarbonyl]-1,3-thiazolidine
3-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-1,3-oxazinan-2-one
-
-
3-[(2S,4S)-4-(2-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(2-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(3,4-dicyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(3,4-methylenedioxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(3-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(3-chloro-4-methoxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(4-aminophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(4-chlorophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(4-methanesulfonylphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(4-nitrophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(5-cyano-2-pyridyl)amino-2-pyrolidinylcarbonyl]-1,3-thiazolidine
3-[(2S,4S)-4-(p-anisidino)-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
3-[(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylpropanamide
3-[1-amino-2-(2H-isoindol-2-yl)-2-oxoethyl]tricyclo[3.3.1.13,7]decan-1-ol
-
-
3-[1-amino-2-(4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethyl]tricyclo[3.3.1.13,7]decan-1-ol
-
-
3-[1-amino-2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]tricyclo[3.3.1.13,7]decan-1-ol
-
-
3-[1-amino-2-[(1R,5S)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]tricyclo[3.3.1.13,7]decan-1-ol
-
-
3-[1-amino-2-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]-5,7-dimethyltricyclo[3.3.1.13,7]decan-1-ol
-
-
3-[1-amino-2-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]tricyclo[3.3.1.13,7]decan-1-ol
-
-
3-[2-[(4R,5R)-5-amino-2-oxo-4-(2,4,5-trifluorophenyl)piperidin-1-yl]ethyl]benzoic acid
-
3-[6-[(3R,4R)-3-amino-4-(2,4,5-trifluorophenyl)piperidin-1-yl]pyrimidin-4-yl]phenyl methanesulfonate
-
-
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]-N,N-dimethylbenzamide
-
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzonitrile
-
-
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]phenol
-
-
3-[6-[(3R,4S)-3-amino-4-phenylpyrrolidin-1-yl]pyrimidin-4-yl]benzonitrile
-
-
3H-imidazo[4,5-c]quinolin-4(5H)-one
-
inhibitor with potent dipeptidyl peptidase IV inhibitory activity that shows poor oral absorption can be improved by esterification of the carboxylic acid moiety
4'-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]biphenyl-3-carboxamide
-
-
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-carboxamide
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-carboxylic acid
-
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-sulfonamide
-
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-4-carboxylic acid
-
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
4-(2-aminoethyl)-benzenesulfonyl fluoride
-
-
4-(2-aminoethyl)benzenesulfonyl fluoride
-
i.e. AEBSF
4-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-yl)-1,3-dihydro-2H-imidazol-2-one
-
4-(4-nitrophenyl)-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
4-([(2R,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-2-yl]methoxy)-3-methoxybenzoic acid
-
4-([1-[(2-oxo-2-thiophen-3-ylethyl)amino]cyclopentyl]methoxy)benzamide
-
-
4-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)benzamide
-
4-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)benzenesulfonamide
-
4-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)benzoic acid
-
4-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]sulfonyl)benzoic acid
-
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
4-bromo-3-([(2R,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-2-yl]methoxy)benzoic acid
-
4-chloro-3-([(2R,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-2-yl]methoxy)benzoic acid
-
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
4-hydroxymercuribenzoate
-
-
4-nitrobenzyl[(5S)-5-amino-6-oxo-6-(1-pyrrolidinyl)hexyl]carbamate
-
-
4-phenyl-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
4-[(1-[[2-oxo-2-(3-thienyl)ethyl]amino]cyclopentyl)methoxy]benzamide
-
4-[(2R)-2-amino-4-oxo-4-(1,3-thiazolidin-3-yl)butyl]benzonitrile
-
4-[(2S)-2-amino-3-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-3-oxopropyl]phenol
-
-
4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-(4-methylphenyl)-1,4-diazepane-1-carboxamide
-
4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-phenyl-1,4-diazepane-1-carboxamide
-
4-[(3R)-3-[(2-oxo-2-phenylethyl)amino]butyl]benzamide
-
4-[(3R)-3-[[2-(2-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide
-
4-[(3R)-3-[[2-(3,4-difluorophenyl)-2-oxoethyl]amino]butyl]benzamide
-
4-[(3R)-3-[[2-(4-chlorophenyl)-2-oxoethyl]amino]butyl]benzamide
-
4-[(3R)-3-[[2-(4-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide
4-[(3R)-3-[[2-oxo-2-(3-thienyl)ethyl]amino]butyl]benzamide
-
4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]morpholine
4-[([1-[(2S)-2-amino-2-cyclohexylacetyl]-L-prolyl]amino)methyl]benzoic acid
-
4-[2-(methylsulfanyl)ethyl]-2-phenoxy-1,3,2-oxazaphospholidine 2-sulfide
-
4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]benzene-1,2-dicarbonitrile
4-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
-
4-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzonitrile
-
-
4-[[(2R)-2-[[2-oxo-2-(3-thienyl)ethyl]amino]propyl]oxy]benzamide
-
4-[[(2R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-2-yl]methoxy]-3-(1-methylethyl)benzoic acid
-
-
4-[[(3R,4R)-3-amino-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]methyl]benzonitrile
-
4-[[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]methyl]-2,6-diethylbenzonitrile
-
4-[[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]methyl]-2,6-dimethylbenzonitrile
-
4-[[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]methyl]-2-methylbenzonitrile
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
4-[[2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-4-oxo-3,4-dihydro-5H-imidazo[4,5-d]pyridazin-5-yl]methyl]naphthalene-1-carbonitrile
-
-
5,6-dichloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
-
5-(3-aminopiperidin-1-yl)-4-but-2-yn-1-yl-N-(naphthalen-1-ylmethyl)-4H-1,2,4-triazole-3-carboxamide
-
-
5-(3-aminopiperidin-1-yl)-4-but-2-yn-1-yl-N-[(3-methylisoquinolin-1-yl)methyl]-4H-1,2,4-triazole-3-carboxamide
-
-
5-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-4-yl)-1,2,4-triazolidin-3-one
-
5-(aminomethyl)-6-(1,3-benzodioxol-5-yl)-2-phenylpyrimidin-4-amine
-
-
5-(aminomethyl)-6-(2,4-dichlorophenyl)-2-(3,5-dimethoxyphenyl)pyrimidin-4-amine
-
-
5-(aminomethyl)-6-(2,4-dichlorophenyl)-2-phenylpyrimidin-4-amine
-
-
5-(aminomethyl)-6-(2,4-dichlorophenyl)-N2-(2-methoxyethyl)-N2-methylpyrimidine-2,4-diamine
-
-
5-(aminomethyl)-6-(2,4-dichlrophenyl)-2-(3,5-dimethoxyphenyl)pyrimidin-4-amine
base compound for inhibitor design, form hydrogen bonds with residues Arg125, Glu205, Glu206, Tyr547, Ser630, Tyr662 and His740
5-(aminomethyl)-6-(4-chlorophenyl)-2-phenylpyrimidin-4-amine
-
-
5-(aminomethyl)-6-[2-chloro-4-(trifluoromethyl)phenyl]-2-(3,5-dimethoxyphenyl)pyrimidin-4-amine
proposed inhibitor, displays three hydrogen bonds with Ser209, two with Glu205 and His740 each, and one with each of the amino acids Arg358 and Tyr662. Compounds is predicted to have good oral absorption and bioavailability
5-([2-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]amino)tricyclo[3.3.1.13,7]decane-1,3-diol
-
-
5-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)pyridine-2-carboxylic acid
-
5-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)pyridine-3-carboxylic acid
-
5-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)tetrahydrofuran-2-carboxylic acid
-
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
5-chloro-2-([(2R,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-2-yl]methoxy)benzoic acid
-
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
5-chloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
5-chloro-6-([(2R,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-2-yl]methoxy)nicotinic acid
-
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
5-fluoro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
-
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
5-methyl-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
-
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
5-tert-butyl-3-[N-(2-hydroxy-1,1-dimethylethyl)glycyl-(4S)-4-fluoro-L-prolyl]-1,2,4-oxadiazole
-
-
5-tert-butyl-3-[N-(2-hydroxy-1,1-dimethylethyl)glycyl-L-prolyl]-1,2,4-oxadiazole
-
-
5-tert-butyl-3-[N-tert-butylglycyl-(4S)-4-fluoro-L-prolyl]-1,2,4-oxadiazole
-
-
5-[1-amino-2-(3-azabicyclo[3.1.0]hex-3-yl)-2-oxoethyl]tricyclo[3.3.1.13,7]decane-1,3-diol
-
-
5-[1-amino-2-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]tricyclo[3.3.1.13,7]decane-1,3-diol
-
-
5-[[(3R,4R)-3-amino-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]methyl]-2-fluorobenzonitrile
-
6-(aminomethyl)-1,3-dimethyl-7-(1-methylpiperazinium)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione
compound exhibits low exposure, high clearance, high selectivity for dipeptidyl peptidase IV over dipeptidyleptidase DPP8
6-(aminomethyl)-1,3-dimethyl-7-(morpholin-4-yl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione
compound exhibits excellent exposure, low clearance, high selectivity for dipeptidyl peptidase IV over dipeptidyleptidase DPP8
6-(aminomethyl)-5-(2,4-dichlorophenyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine
-
-
6-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methoxy)pyridine-3-carbonitrile
-
-
6-([(3S,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-3-yl]amino)pyridine-3-carbonitrile
6-([2-((2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl)amino)ethyl]amino)pyridine-3-carbonitrile
6-[(2-([2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]amino)ethyl)amino]pyridine-3-carbonitrile
6-[(3R,4R)-3-amino-4-(2,4,5-trifluorophenyl)piperidin-1-yl]-N,N-diethylpyrimidin-4-amine
-
6-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)(methyl)amino]pyridine-3-carbonitrile
-
-
6-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)amino]pyridine-3-carbonitrile
-
-
6-[4-([2-[(2R,5S)-2,5-dicyanopyrrolidin-1-yl]-2-oxoethyl]amino)-4-methylpiperidin-1-yl]pyridine-3-carboxylic acid
-
6-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
6-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]nicotinonitrile
-
6-[[2-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)ethyl]amino]nicotinonitrile
-
-
6-[[2-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)ethyl]amino]nicotinamide
-
-
6-[[4-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)cyclohexyl]oxy]nicotinonitrile
-
6-[[4-([2-[(2S,5R)-2-cyano-5-ethynylpyrrolidin-1-yl]-2-oxoethyl]amino)cyclohexyl]oxy]pyridine-3-carbonitrile
-
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
6-{[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)ethyl]amino}pyridine-3-carbonitrile
-
-
7-(aminomethyl)-6-(2-chlorophenyl)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
-
7-(aminomethyl)-6-(2-chlorophenyl)-1-methyl-1H-benzimidazole-5-carbonitrile
-
7-(aminomethyl)-6-(2-chlorophenyl)-1-methyl-1H-benzimidazole-5-carboxamide
-
7-amino-6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione
compound exhibits good exposure, moderate clearance, high selctivity for dipeptidyl peptidase IV over dipeptidyleptidase DPP8
7-amino-6-(aminomethyl)-5-(2-fluoro-6-methoxyphenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione
compound exhibits good exposure, moderate clearance, high selectivity for dipeptidyl peptidase IV over dipeptidyleptidase DPP8
7-benzyl-3-methyl-8-piperazin-1-yl-3,7-dihydro-1H-purine-2,6-dione
-
-
7-but-2-ynyl-9-(6-methoxy-pyridin-3-yl)-6-piperazin-1-yl-7,9-dihydro-purin-8-one
-
a competitive and selective inhibitor of dipeptidyl peptidase IV with an antihyperglycemic activity
7-but-2-ynyl-9-(6-methoxy-pyridin-3-yl)-6-piperazin-1-yl-7,9-dihydro-purin-8-one trifluoroacetate
-
-
7-[(2-butyl-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-6-yl)amino]-N-[(3R)-1-[3-[(2-cyanophenyl)methyl]-1-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl]piperidin-3-yl]heptanamide
fluorescent probe based on inhibitor alogliptin
7-[(2E)-but-2-en-1-yl]-8-(3,3-dimethylpiperazin-1-yl)-3-methyl-1-(2-oxo-2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
-
-
7-[(3R)-3-amino-1-oxo-4-(2,5-difluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine
-
inhibition of DPP-IV does not alter the circulating levels of insulin-like growth factor 1 (biomarker for the physiological relevance of DPP-IV activity) in the growing pig
7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-tert-butyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxamide
7-[(3R,4R)-3-amino-4-(2,4,5-trifluorophenyl)piperidin-1-yl]-2H-pyrimido[1,2-b]pyridazin-2-one
-
-
7-[(3R,4R)-3-amino-4-(2-methoxyphenyl)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
-
-
7-[(3R,4S)-3-amino-4-(2-methoxyphenyl)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
-
-
7-[(3R,4S)-3-amino-4-(3,4-dichlorophenyl)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
-
-
7-[(3R,4S)-3-amino-4-(4-fluorophenyl)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
-
-
7-[(3R,4S)-3-amino-4-phenylpyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
-
-
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione
a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. Potential for once-daily treatment of type 2 diabetics
8-(3-aminopiperidin-1-yl)-7-but-2-yn-1-yl-3-methyl-1-(naphthalen-1-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
-
-
8-(3-aminopiperidin-1-yl)-7-but-2-yn-1-yl-3-methyl-1-[(3-methylisoquinolin-1-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
-
-
8-[(3R)-3-aminopiperidin-1-yl]-1-[(1,3-benzothiazol-2-yl)methyl]-3-methyl-7-(3-methylbut-2-en-1-yl)-3,7-dihydro-1H-purine-2,6-dione
IC50 value with isoforms DPP-8 and DPP-9 is above 0.1 mM
8-[(3R)-3-aminopiperidin-1-yl]-3-methyl-7-(3-methylbut-2-en-1-yl)-1-(2-oxo-2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
-
-
8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
AB192
-
i.e. bis(4-acetamidophenyl) 1-((S)-prolyl)pyrrolidine-2(R,S)-phosphonate hydrochloride
Ala-Ala
-
hydrolysis of Gly-Pro-4-nitroanilide
Ala-Ala-Leu-Glu-Gln-Thr-Glu-Arg
-
inhibitory peptide from hydrolysate of Hypophthalmichthys molitrix muscle
Ala-PSI[CS-N]-pyrrolidide
-
-
Ala-PSI[CS-N]-thiazolidide
-
-
alpha-amino boronic acid analogues of pyrrolidides
-
-
-
alpha-amino boronic acid analogues of thiazolidides
-
-
-
antipain
-
0.2 mM, 17% inhibition
atorvastatin
-
competitive
benzyl 4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepane-1-carboxylate
-
benzyl 6-([5-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-(4S)-4-amino-5-oxopentanoyl]amino)hexanoate
-
-
benzyl [(5S)-5-amino-6-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-6-oxohexyl]carbamate
-
-
benzyloxycarbonyl-Pro-prolinal
-
-
bis(4-acetamidophenyl) 1-((S)-prolyl)pyrrolidine-2(R,S)-phosphonate
bis(4-acetamidophenyl) 1-(S)-prolylpyrrolidine-2(R,S)-phosphonate
bis(4-[(ethoxycarbonyl)-methylaminocarbonyl]-phenyl) 1-((S)-prolyl)pyrrolidine-2-(R,S)-phosphonate
bis-(4-nitrophenylphosphate)
Bl-1356
-
ondero or linagliptin, competitive, reversible, and long-lasting inhibition
BMS-477118
-
saxagliptin, the proprietary name is Onglyza, covalently bound and reversible inhibitor
Ca2+
-
mixed type inhibition, Ca2+ ions preferentially bind to the betA-propeller domain
carmegliptin
-
potent and long-acting dipeptidyl peptidase IV inhibitor
cis-(2S)-1-([(2S)-5-(2-hydroxyethyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
cis-(2S)-1-([(2S)-5-ethylpyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
cis-(2S)-1-([(2S)-5-methylpyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
cis-(2S)-1-([(2S)-5-phenylpyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
cis-(2S)-1-([(2S)-5-prop-2-yn-1-ylpyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
cis-(2S)-1-([(2S)-5-propylpyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
cyclohexylglycine thiazolidide
-
-
des-fluoro-sitagliptin
-
sitagliptin analogue, reversible inhibition
diaryl phosphonates
-
-
-
diethyldicarbonate
-
modification of 4 His residues per subunit using diethyldicarbonate results in 30% inactivation
diisopropyl fluorophosphate
diisopropylfluorophosphate
dipeptide-derived diphenyl phosphonate esters
-
mechanism-based inhibitors. Formation of a fairly weak initial complex, followed by a slow irreversible inactivation. Due to their stability and the irreversible nature of the inhibition, the diphenyl phosphonate ester promise to be useful tools in the continuing investigation of the physiological function of the dipeptidyl peptidase IV
-
diphenyl [1-(N-(15-oxo-19-[(4R)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]-4,7,10-trioxa-14-azanonadec-1-yl)-L-glutaminyl)pyrrolidin-2-yl]phosphonate
-
irreversible inhibitor
di{4-[(erythrocarbonyl)methylaminoacrbonyl]-phenyl} 1-((S)-prolyl)pyrrolidine-2(R,S)-phosphonate
irreversible
DP IV-I3
-
selective DP IV inhibitor, 87% inhibition at 0.01 mM
DP-893
-
reversible inhibition
epsilon-(4-nitrobenzyloxycarbonyl)-L-Lys thiazolidide
-
-
ethyl (3R,4S)-3-amino-4-(2,4-dichlorophenyl)pyrrolidine-1-carboxylate
-
ethyl 4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-carboxylate
-
ethyl 4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-4-carboxylate
-
ethyl 4-[(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxopentanoyl]piperazine-1-carboxylate
-
-
ethyl 4-[3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanoyl]piperazine-1-carboxylate
ethyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
ethyl [(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]carbamate
-
-
ethyl-2-(4-(((S)-1-((S)-2-amino-(4-fluorophenyl)propanoyl)pyrrolidine-2-carboxamido)-methyl)phenoxy)acetate
compound exhibits high selectivities against dipeptidyl peptidases FAP, DPP 7, DPP 8, and DPP 9, with inhibition rates <50% at 20 microg/ml
ethyl-2-(4-(((S)-1-((S)-2-amino-3-(2-fluorophenyl)propanoyl)pyrrolidine-2-carboxamido)-methyl)phenoxy)acetate
compound exhibits high selectivities against dipeptidyl peptidases FAP, DPP 7, DPP 8, and DPP 9, with inhibition rates <50% at 20 microg/ml
Fe2+
-
1 mM, 13% inhibition
Gly-Ala
-
hydrolysis of Gly-Pro-4-nitroanilide
Gly-Pro
-
competitive inhibition
glypican-3
-
Simpson-Golabi-Behmel syndrome is an X-linked condition shown to be the result of deletions of the glypican-3 gene. Glypican-3, binds to and inhibits the dipeptidyl peptidase activity of CD26. Inhibition of CD26 reduces the rate of cell proliferation. A number of physical findings observed in SGBS patients may be a consequence of a direct interaction of GPC3 with CD26
-
GSK-823093C
-
denagliptin
H-(S)-alaninyl-(R)-boro-proline
H-(S)-Glu-(R)-boro-alanine
H-(S)-glutaminyl-(R)-boro-alanine
H-(S)-glutamyl-(R)-boro-proline
H-(S)-valinyl-(R)-boro-alanine
H-(S)-valinyl-(R)-boro-proline
H-Glu-(NHO-Bz)-Pyr
-
DppIV-specific inhibitor
H-glycyl-(R)-boro-proline
hemorphin-4 peptide
-
12% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence YPWT, competitive
hemorphin-5 peptide
-
18% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence YPWTQ, competitive
-
hemorphin-7 peptide
-
30% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence YPWTQRF, selective and competitive
human HIV-1 Ala2-Tat(1-9) peptide
-
amino acid sequence MAPVDPNIE
human HIV-1 Arg2-Tat(1-9) peptide
-
amino acid sequence MRPVDPNIE
human HIV-1 Asn2-Tat(1-9) peptide
-
amino acid sequence MNPVDPNIE
human HIV-1 Asp2-Tat(1-9) peptide
-
amino acid sequence MDPVDPNIE, moderate inhibitor
human HIV-1 Cys2-Tat(1-9) peptide
-
amino acid sequence MCPVDPNIE
human HIV-1 Gln2-Tat(1-9) peptide
-
amino acid sequence MQPVDPNIE
human HIV-1 Glu2-Tat(1-9) peptide
-
amino acid sequence MEPVDPNIE, moderate inhibitor
human HIV-1 Gly2-Tat(1-9) peptide
-
amino acid sequence MGPVDPNIE
human HIV-1 Gly3-Tat(1-9) peptide
-
amino acid sequence MDGVDPNIE, parabolic mixed type inhibition
-
human HIV-1 His2-Tat(1-9) peptide
-
amino acid sequence MHPVDPNIE, strong inhibitor
human HIV-1 Ile2-Tat(1-9) peptide
-
amino acid sequence MIPVDPNIE
human HIV-1 Ile3-Tat(1-9) peptide
-
amino acid sequence MDIVDPNIE, parabolic mixed type inhibition
-
human HIV-1 Leu2-Tat(1-9) peptide
-
amino acid sequence MLPVDPNIE
human HIV-1 Lys2-Tat(1-9) peptide
-
human HIV-1 Met2-Tat(1-9) peptide
-
amino acid sequence MMPVDPNIE
human HIV-1 Phe2-Tat(1-9) peptide
-
amino acid sequence MFPVDPNIE, strong inhibitor
human HIV-1 Pro2-Tat(1-9) peptide
-
amino acid sequence MPPVDPNIE
human HIV-1 Ser2-Tat(1-9) peptide
-
amino acid sequence MSPVDPNIE
human HIV-1 Tat protein
-
viral protein, inhibits the enzyme activity and cell proliferation
-
human HIV-1 Tat(1-9) peptide
-
human HIV-1 Thr2-Tat(1-9) peptide
-
amino acid sequence MTPVDPNIE, weak inhibitor
human HIV-1 Trp1-Tat(1-9) peptide
-
amino acid sequence WDPVDPNIE, parabolic mixed type inhibition
-
human HIV-1 Trp2-Tat(1-9) peptide
-
human HIV-1 Tyr2-Tat(1-9) peptide
-
amino acid sequence MYPVDPNIE, strong inhibitor
human HIV-1 Val2-Tat(1-9) peptide
-
amino acid sequence MVPVDPNIE
Ile cyanothiazolidide
-
-
Ile-Pro-Ile
i.e. diprotin A, inhibition mechanism, binds covalently to Ser630
Ile-PSI[CS-N]-pyrrolidide
-
-
Ile-PSI[CS-N]-thiazolidide
-
-
interleukin-2 peptide Met-IL-2(1-12)
-
amino acid sequence MAPTSSSTKKTQL, linear mixed type inhibition
-
interleukin-2 peptide Met-IL-2(1-9)
-
amino acid sequence MAPTSSSTKK, weak inhibitor
interleukin-2 peptide Met-TRp1-IL-2(1-8)
-
amino acid sequence MWPTSSSTK, competitive inhibition
-
iodoacetamide
0.01 mM, 19% inhibition
isoleucyl-(2)-cyanopyrrolidine
-
-
isoleucyl-thiazolidine
-
-
K-579
-
reversibile and long-lasting inhibition
L-1-chloro-3-[4-tosylamido]-7-amino-2-heptanone
-
-
L-Ile-L-Pro-L-Ile
-
the dipeptidyl peptidase IV inhibitor switches the enzyme from hydrolase to synthase functional mode to generate endomorphin 2
L-isoleucinepyrrolidine
-
IC50: 0.022 mM
L-threo-Ile-thiazolidide
-
-
LAF237
-
i.e. (S)-1-[(3-hydroxy-1-adamantyl)ammo]acetyl-2-cyanopyrrolidine
LC-150444
-
reversible inhibition
LC15-0444
-
selective and competitive inhibitor of dipeptidyl peptidase IV, more than 80% inhibition of DPP IV activity from baseline is sustained for more than 24 h in all dose groups (200, 400 or 600 mg of LC15-0444 once daily for 10 days)
Leu-Ala
-
hydrolysis of Gly-Pro-4-nitroanilide
Leu-Pro
-
hydrolysis of Gly-Pro-4-nitroanilide
LVV-hemorphin-7 peptide
-
9% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence LVVYPWTQRF, the additional leucine residue reduces the inhibitory potential
LY-2463665
-
reversible inhibition
Lys-2-cyano-pyrrolidides
-
-
Lys-Ala-Val-Gly-Glu-Pro-Pro-Leu-Phe
-
inhibitory peptide from hydrolysate of Hypophthalmichthys molitrix muscle, exhibits the dual inhibition against both DPP-IV and angiotensin-converting enzyme
Lys[benzyloxycarbonyl(NO2)]-thiazolidide
-
-
Met-(4-benzoyl-phenylalanine)-DPVDPNIE
-
-
Met-(4-nitrophenyl-alanine)-DPVDPNIE
-
strong inhibitor
Met-(beta-(1-naphthyl)-alanine)-DPVDPNIE
-
strong inhibitor
Met-(beta-(2-naphthyl)-alanine)-DPVDPNIE
-
strong inhibitor
Met-(beta-(3-benzothienyl)-alanine)-DPVDPNIE
-
strong inhibitor
Met-(beta-(3-biphenyl)-alanine)-DPVDPNIE
-
-
Met-(beta-(4-pyridyl)-alanine)-DPVDPNIE
-
-
Met-GCSF(1-9) peptide
-
GCSF is the granulocyte colony stimulating factor, weak inhibitor
Met-Trp-Pro
-
competitive inhibition
Met-Trp-Val
-
linear-mixed type inhibition
Met-Trp1-G-CSF(1-8) peptide
-
amino acid sequence MWPLGPASS, G-CSF is the granulocyte colony stimulating factor, linear mixed type inhibition
methionyl-2(S)-cyanopyrrolidine
-
irreversible noncompetitive inhibitor of DP-IV
methyl (2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanoate
-
methyl (4-[[([(4R)-3-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-1,3-thiazolidin-4-yl]carbonyl)amino]methyl]phenyl)acetate
-
methyl 4-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]benzenesulfinate
-
methyl 4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]benzoate
-
MK-0431
-
sitagliptin, potent, selective DPP IV inhibitor, the proprietary name is Januvia, reversible and long-lasting inhibition
MK0431
-
sitagliptin, treatment of NOD mice with daily 4 g/kg MK0431 before and after islet transplantation results in prolongation of islet graft survival
N,N-diallyl-3-(bicyclo[3.2.0]hept-6-ylsulfonyl)-1H-1,2,4-triazole-1-carboxamide
-
-
N-(1,3-benzothiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(3-chloro-4-fluorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-yl)-1,1,1-trifluoromethanesulfonamide
-
N-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-yl)methanesulfonamide
-
N-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-4-yl)methanesulfonamide
-
N-(4-chlorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
N-(4-cyanophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(4-nitrobenzyloxycarbonyl)-L-Ile thiazolidide
-
-
N-(5-bromo-1,3-thiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-ethylhydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-hydroperoxyhydrazinyl)piperidin-1-yl]acetamide
-
-
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
potent inhibitor of DPP IV
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
-
-
N-(H-Phe-Pro-)-O-(4-nitrobenzoyl)hydroxylamine hydrochloride
-
irreversible
N-([(2R,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-2-yl]methyl)benzamide
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1,1,1-trifluoro-N-methylmethanesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1,1,1-trifluoromethanesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1-(trifluoromethyl)cyclopropanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2,2-trifluoroethanesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluoro-N-methylpropanamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluorocyclopropanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluoropropanamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-dimethylpropanamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluoro-2-methylpropanamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3,3,3-trifluoropropanamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N,2,2-trimethylpropanamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N-cyclopropyl-1,1,1-trifluoromethanesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N-methylcyclopropanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclobutanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclopentanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)methanesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-2-carboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-3-carboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-4-carboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3,4,6-trifluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-(methylsulfonyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(5-chlorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2,5-dichlorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-chlorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzenesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
-
-
N-([(3S,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]methyl)-3-[(4-methyl-1,3-thiazol-2-yl)sulfamoyl]benzamide
-
-
N-acetyl-(S)-valinyl-(R)-boro-proline
N-Ala-Pro-O-(4-nitrobenzoyl)hydroxylamine
-
-
N-bromosuccinimide
-
almost completely inactivates with the modification of only one Trp residue per subunit, protective action of the substrate and inhibitors such as Ala-Pro-Ala and Pro-Pro
N-isoleucyl-3-fluoro-pyrrolidine
reversible
N-terminal nonapeptide of HIV-1 Tat protein
-
wild-type is a strong inhibitor, mutant exchange variants Ile5 and Leu6 show highly reduced inhibitory activity, replacement of Asp2 with Gly or Lys lead to enhanced inhibitory potency compared to the wild-type peptide, study of structure-function relationship
-
N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]-3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanamide
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-2-methylbutanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylpentanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]butanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]pentanamide
-
-
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]propane-1-sulfonamide
-
-
N-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butyl]-6-(trifluoromethyl)-3,4-dihydropyrrolo[1,2-a]pyrazine-2(1H)-carboxamide
-
good enzyme inhibitory activity and excellent selectivity for isoform DPP4 over dipeptidyl peptidase family homologues DPP8 and DPP9. Compound shows efficacy similar to that of sitagliptin in the oral glucose tolerance test
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
N-[2-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-2-methylpropyl]-1-methylcyclohexanecarboxamide
-
-
N-[2-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-2-methylpropyl]-2,2-dimethylpropanamide
-
-
N-[2-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-2-oxoethyl]-N-methyl-5-oxoprolinamide
-
-
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-1H-1,2,3-benzotriazole-5-carboxamide
-
-
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-1H-benzimidazole-5-carboxamide
-
-
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-2,3-dihydro-1-benzofuran-5-carboxamide
-
-
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-N-(4-cyanobenzyl)benzamide
-
-
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-N-isobutylbenzamide
-
-
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-N-methylbenzenesulfonamide
-
-
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]benzamide
-
-
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]benzenesulfonamide
-
-
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]pyridine-2-carboxamide
-
-
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]thiophene-2-carboxamide
-
-
N-[3-[(2-[4-[(2S)-2-amino-3-phenylpropyl]-3-benzylpiperazin-1-yl]ethyl)amino]phenyl]methanesulfonamide
-
-
N-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]methyl]-1,3-thiazole-4-carboxamide
-
-
N3-[2-[(2S)-2-cyanopyrrolidin-1-yl]-1,1-dimethyl-2-oxoethyl]-N-(2-pyridin-2-ylethyl)-b-alaninamide
-
in vivo efficacy in rat models after oral administration
nateglinide
-
prevents the degradation of glucagon-like peptide-1 in a time and concentration-dependent manner
Nepsilon-nitrobenzyloxycarbonyl-Lys-azetidide
-
-
Nepsilon-nitrobenzyloxycarbonyl-Lys-piperidide
-
-
Nepsilon-nitrobenzyloxycarbonyl-Lys-Pro
Nepsilon-nitrobenzyloxycarbonyl-Lys-Pyrr-CN
-
-
Nepsilon-nitrobenzyloxycarbonyl-Lys-pyrrolidide
Nepsilon-nitrobenzyloxycarbonyl-Lys-thiazolide
-
specific
Nepsilon-nitrobenzyloxycarbonyl-Lys-thiazolidide
Ngamma-(2,2,5,7,8-pentamethylchroman-6-sulfonyl)-L-Arg-cyanopyrrolidine
-
-
P-[(3S)-3-amino-2-oxopyrrolidin-1-yl]phosphonic diamide
-
-
P32/P98
-
isoleucine thiazolidide DPPIV, reversible inhibition
peptides
-
diacylhydroxylamine derivatives of Xaa-Pro or Xaa-Ala peptides. Different oligopeptides with N-terminal Xaa-Pro-sequences
Phe-Pro
-
hydrolysis of Gly-Pro-4-nitroanilide
phenylmethylsulfonyl fluoride
PHX-1149
-
dutogliptin tartrate, reversible inhibition
Pro-Gly
-
hydrolysis of Gly-Pro-4-nitroanilide
Pro-Ile
-
hydrolysis of Gly-Pro-4-nitroanilide
Pro-Leu
-
hydrolysis of Gly-Pro-4-nitroanilide
Pro-Met
-
hydrolysis of Gly-Pro-4-nitroanilide
Pro-Phe
-
hydrolysis of Gly-Pro-4-nitroanilide
Pro-Pro-PSI[P(OPh-4Ac)2
-
2 diastereomers
Pro-Pro-PSI[P(OPh-4Cl)2]
-
2 diastereomers
Pro-Pro-[OPh-4 Cl]2
-
irreversible
Pro-PSI[CH2-N]-pyrrolidide
-
-
pyrrolidine-carbonitrile derivatives
-
-
-
R-1438
-
aminomethylpyridine derivate
R-1579
-
carmegliptin, reversible inhibition
SYR-322
-
2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, also called alogliptin or TAK-322, reversible inhibition
Syrrx106124
-
acutely lowers blood glucose and enhances glucose-stimulated insulin secretion in wild-type mice and in mice with targeted disruption of single incretin receptors
tert-butyl 2-(1-acetylpiperidin-4-yl)-2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,3-dichlorobenzoyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(dimethylcarbamoyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(pyridin-3-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
-
-
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-[(4-methylcyclohexyl)carbonyl]piperidin-4-yl]hydrazinecarboxylate
-
-
threo-Ile thiazolidide
-
-
thromboxane A2 receptor peptide TXA2-R(1-9)
-
TP8211
-
acutely lowers blood glucose and enhances glucose-stimulated insulin secretion in wild-type mice and in mice with targeted disruption of single incretin receptors
-
trans-(2S)-1-([(2S)-5-(2-hydroxyethyl)pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
trans-(2S)-1-([(2S)-5-ethylpyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
trans-(2S)-1-([(2S)-5-prop-2-yn-1-ylpyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
Trp2,Ile3-Tat(1-9) peptide
-
amino acid sequence MWIVDPNIE, competitive inhibition
-
Tyr-Pro
-
hydrolysis of Gly-Pro-4-nitroanilide
Val-PSI[CS-N]-pyrrolidide
-
-
Val-PSI[CS-N]-thiazolidide
-
-
Val-PSI[PO(OCH3)-N]-pyrrolidide
-
2 diastereomers
VV-hemorphin-5 peptide
-
10% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence VVYPWTQ
VV-hemorphin-6 peptide
-
15% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence VVYPWTQR
VV-hemorphin-7 peptide
-
27% inhibition at 0.03 mM, endogenous blood-derived peptide belonging to the family of atypical opioidic peptides released from sequentially hydrolyzed hemoglobin, amino acid sequence VVYPWTQRF
W2-interleukin-2 peptide Met-IL-2(1-9)
-
amino acid sequence MWPTSSSTKK
W2-Met-GCSF(1-9) peptide
-
GCSF is the granulocyte colony stimulating factor
ZnCl2
-
2 mM, complete inhibition
[(2R)-1-(4-oxo-4-phenylbutanoyl)pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-(N-acetyl-N-methylglycyl)pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-(N-acetylglycyl)pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)acetyl]pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[(2-oxopyridin-1(2H)-yl)acetyl]pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[N-(2,2-dimethylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[N-(cyclohexylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[N-(cyclopentylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[N-methyl-N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[N-methyl-N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
-
-
[(2R)-1-[N-[(2,5-dichlorophenyl)carbonyl]glycyl]pyrrolidin-2-yl]boronic acid
-
-
[(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro-1,2,4[triazolo]4,3-alpha]pyrazin-7(8H)-yl]-1-(2,5-difluorophenyl)butan-2-amine hydrochloride
-
selective DP IV inhibitor
[(2R,4R)-1-(L-arginyl)-4-hydroxypyrrolidin-2-yl]boronic acid
-
most potent inhibitor tested
[(2S)-1-([[2-(4-fluorophenyl)-1,1-dimethylethyl]amino]acetyl)pyrrolidin-2-yl](1,2,4-oxadiazol-3-yl)methanone
-
-
[(2S)-1-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]pyrrolidin-2-yl]methanol
-
-
[(2S)-1-[(3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanoyl]pyrrolidin-2-yl]methanol
-
-
[(2S)-1-[(tert-butylamino)acetyl]pyrrolidin-2-yl][5-(4-fluorophenyl)-1,2,4-oxadiazol-3-yl]methanone
-
-
[(2S)-1-[[(2-hydroxy-1,1-dimethylethyl)amino]acetyl]pyrrolidin-2-yl](5-methyl-1,2,4-oxadiazol-3-yl)methanone
-
-
[(2S)-1-[[(2-hydroxy-1,1-dimethylethyl)amino]acetyl]pyrrolidin-2-yl](5-methyl-1,3,4-oxadiazol-2-yl)methanone
-
-
[(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-2-oxo-1,4-diazepan-1-yl]acetic acid
-
-
[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]acetic acid
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
[(R)-amino[(3S)-3-amino-2-oxoazepan-1-yl]phosphoryl]sulfamic acid
-
-
[(R)-amino[(3S)-3-amino-2-oxopiperidin-1-yl]phosphoryl]sulfamic acid
-
-
[2-[([1-[(2S)-2-amino-2-cyclohexylacetyl]-L-prolyl]amino)methyl]phenyl]acetic acid
-
[2-[([1-[(3S)-3-amino-4-phenylbutanoyl]-L-prolyl]amino)methyl]phenyl]acetic acid
-
[2-[7-(aminomethyl)-1-methyl-1H-benzimidazol-6-yl]phenyl]methanol
-
[3-[([1-[(2S)-2-amino-2-cyclohexylacetyl]-L-prolyl]amino)methyl]phenyl]acetic acid
-
[3-[([1-[(3S)-3-amino-4-phenylbutanoyl]-L-prolyl]amino)methyl]phenyl]acetic acid
-
[4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]acetic acid
-
[4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenyl]acetic acid
-
[4-[([1-[(3S)-3-amino-4-(3,4-difluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenyl]acetic acid
-
[4-[([1-[(3S)-3-amino-4-phenylbutanoyl]-L-prolyl]amino)methyl]phenyl]acetic acid
-
[7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-3-yl]methanol
-
-
(1R)-2-[[(3R,4R)-4-amino-1-[1-[4-(1H-1,2,4-triazol-1-yl)phenyl]ethyl]pyrrolidin-3-yl]carbonyl]cyclopentanecarbonitrile
-
(1R)-2-[[(3R,4R)-4-amino-1-[1-[4-(1H-1,2,4-triazol-1-yl)phenyl]ethyl]pyrrolidin-3-yl]carbonyl]cyclopentanecarbonitrile
-
-
(1R,3S)-2-[(2S)-2-amino-2-cyclopentylacetyl]-3-ethynylcyclopentanecarbonitrile
-
-
(1R,3S)-2-[(2S)-2-amino-2-cyclopentylacetyl]-3-ethynylcyclopentanecarbonitrile
-
(1S,2R,5S)-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-2-(2,4,5-trifluorophenyl)cyclohexanamine
-
the inhibitor has similar potency to sitagliptin and excellent pharmacokinetic properties
(1S,2R,5S)-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-2-(2,4,5-trifluorophenyl)cyclohexanamine
-
-
(1S,2R,5S)-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-2-(2,4,5-trifluorophenyl)cyclohexanamine
-
the inhibitor has similar potency to sitagliptin and excellent pharmacokinetic properties
(1S,2R,5S)-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-2-(2,4,5-trifluorophenyl)cyclohexanamine
-
the inhibitor has similar potency to sitagliptin and excellent pharmacokinetic properties
(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
-
-
(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
-
66% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 30% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2-(4-((2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl)-2-oxoethyl)amino)-4-methyl-1-piperidinyl)-4-pyridinecarboxylic acid
-
i. e. ABT-279, a very potent, selective, effective, and well-tolerated inhibitor useful for the treatment of diabetes
(2-(4-((2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl)-2-oxoethyl)amino)-4-methyl-1-piperidinyl)-4-pyridinecarboxylic acid
-
i. e. ABT-279, a very potent, selective, effective, and well-tolerated inhibitor useful for the treatment of diabetes
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(3,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-1-(3,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
sitagliptin
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R)-4-[1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
-
(2R,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2R,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2R,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2R,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2S)-1-([(2S,4S)-4-[(2E)-but-2-en-1-yl]pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-([(2S,4S)-4-[(2E)-but-2-en-1-yl]pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-([[2-methyl-4-oxo-4-(pyrrolidin-1-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-([[2-methyl-4-oxo-4-(pyrrolidin-1-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile
-
-
(2S)-1-L-prolylpyrrolidine-2-carbonitrile
-
IC50: 2.9 nmol/L
(2S)-1-L-prolylpyrrolidine-2-carbonitrile
-
IC50: 2.9 nmol/L
(2S)-1-[(2S)-2-amino-2-cyclopentylacetyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S)-2-amino-2-cyclopentylacetyl]pyrrolidine-2-carbonitrile
-
(2S)-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
-
(2S)-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(4R)-4-tricyclo[3.3.1.13,7]dec-2-yl-L-prolyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(4R)-4-tricyclo[3.3.1.13,7]dec-2-yl-L-prolyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(4S)-4-(azocan-1-ylcarbonyl)-L-prolyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[(4S)-4-(azocan-1-ylcarbonyl)-L-prolyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[N-[4-(1,3-dihydro-2H-isoindol-2-yl)-2-methyl-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[N-[4-(1,3-dihydro-2H-isoindol-2-yl)-2-methyl-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-ethyl-4-hydroxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-ethyl-4-hydroxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-hydroxyethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-hydroxyethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(2-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,4,6-trimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,4,6-trimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(3-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethoxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethoxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-(4-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-cyclohexylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-cyclohexylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4R)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
in vivo plasma DPP-IV inhibition in Wistar rats
(2S)-1-[[(2S,4S)-4-(azepan-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(azepan-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(azetidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(azetidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(hydroxymethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(hydroxymethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-allylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-allylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-isobutylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-isobutylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-propylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S)-4-propylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-4-(azetidin-1-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-4-(azetidin-1-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile
-
-
(2S)-1-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile
-
84% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 73% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
-
(2S,3S)-3-(4-bromophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
(2S,3S)-3-(4-bromophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-ethyl-N,N-dimethylpyrrolidine-3-carboxamide
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-ethyl-N,N-dimethylpyrrolidine-3-carboxamide
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N,2-dimethylpyrrolidine-3-carboxamide
-
-
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N,2-dimethylpyrrolidine-3-carboxamide
-
-
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile
-
potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile
-
potent, selective, and orally bioavailable dipeptide-derived inhibitor of dipeptidyl peptidase IV, 82% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 70% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-1-[N-[4-(3,6-dihydropyridin-1(2H)-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[N-[4-(3,6-dihydropyridin-1(2H)-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
85% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 70% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-1-[N-[4-(7-azabicyclo[2.2.1]hept-7-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[N-[4-(7-azabicyclo[2.2.1]hept-7-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[N-[4-(azepan-1-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-1-[N-[4-(azepan-1-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[(2R)-2-methylpyrrolidin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[(2R)-2-methylpyrrolidin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
-
75% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 48% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[4-(methylsulfonyl)piperazin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[4-(methylsulfonyl)piperazin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
-
64% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 7% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-4-fluoro-1-(N-[4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-(N-[4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-([[2-methyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-([[2-methyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile
-
77% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 56% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-fluoropyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-fluoropyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
63% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 15% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-4-fluoro-1-[([4-[(3S)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[([4-[(3S)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(4-methylpiperazin-1-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(4-methylpiperazin-1-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(morpholin-4-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(morpholin-4-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
89% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 59% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(4-oxopiperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(4-oxopiperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(piperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
-
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(piperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile
-
86% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 74% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(2S,4S,5S)-N-(cyanomethyl)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-N-ethyl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-N-ethyl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-prop-2-yn-1-ylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-prop-2-yn-1-ylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-propylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-propylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-N,5-dimethylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-N,5-dimethylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-cyclopropyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-cyclopropyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-allyl-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N-allyl-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
-
-
(2S,4S,5S)-N4-benzyl-N2-(cyanomethyl)-N2-ethyl-5-methylpyrrolidine-2,4-dicarboxamide
-
-
(2S,4S,5S)-N4-benzyl-N2-(cyanomethyl)-N2-ethyl-5-methylpyrrolidine-2,4-dicarboxamide
-
-
(2S,5R)-1-[(2S)-2-amino-2-cyclopentylacetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
-
-
(2S,5R)-1-[(2S)-2-amino-2-cyclopentylacetyl]-5-prop-1-yn-1-ylpyrrolidine-2-carbonitrile
-
(3'S,5'S)-5'-(1,3-thiazolidin-3-ylcarbonyl)-1,3'-bipyrrolidine
-
-
(3'S,5'S)-5'-(1,3-thiazolidin-3-ylcarbonyl)-1,3'-bipyrrolidine
-
-
(3R)-3-amino-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
-
(3R)-3-amino-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
(3R)-3-amino-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
30% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 20% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
competitive, reversible inhibitor. Pharmacokinetic parameters
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
competitive, reversible inhibitor
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
-
competitive, reversible inhibitor. Pharmacokinetic parameters
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
pharmacokinetic parameters
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
-
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
pharmacokinetic parameters
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
-
pharmacokinetic parameters
(3R,4S)-1-(6-phenylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
(3R,4S)-1-(6-phenylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3R,4S)-1-[4-[3-(methylsulfonyl)phenyl]-1,3,5-triazin-2-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
efficacious in vivo, lowering blood glucose in ZDF rats that were allowed to feed freely on a mixed meal
(3R,4S)-1-[4-[3-(methylsulfonyl)phenyl]-1,3,5-triazin-2-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
-
-
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl 4-cyanobenzoate
-
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl 4-cyanobenzoate
-
-
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl benzoate
-
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl benzoate
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-diethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-diethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-dimethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-dimethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N-methylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N-methylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-methylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-methylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-propylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-propylpyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidine-3-carboxamide
-
-
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidine-3-carboxamide
-
-
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(3S,5S)-N-(4-methoxyphenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
(3S,5S)-N-(4-methoxyphenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
(3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
(3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
-
(4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]phenyl)ethynamine
-
-
(4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]phenyl)ethynamine
-
-
(4R,5R)-5-amino-1-[2-[3-(methylsulfonyl)phenyl]ethyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
(4R,5R)-5-amino-1-[2-[3-(methylsulfonyl)phenyl]ethyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
-
1,10-phenanthroline
-
1.0 mM, 14 mM 40°C, partial
1,10-phenanthroline
10 mM, 34% inhibition
1,10-phenanthroline
-
slight
1-(2-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(2-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(3,4-dichlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(3,4-dichlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(3-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(3-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-bromophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-bromophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
-
1-(4-ethynylpyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-ethynylpyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-fluorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-fluorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-methoxyphenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-methoxyphenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,4-diazepane
-
-
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,4-diazepane
-
-
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(5-chloropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(5-chloropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(5-nitropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(5-nitropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(diphenylmethyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(diphenylmethyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-(L-alanyl)pyrrolidine
-
reversible
1-(L-alanyl)pyrrolidine
-
reversible
1-(L-cyclohexylalanyl)piperidine
-
reversible
1-(L-cyclohexylalanyl)piperidine
-
reversible
1-(L-cyclohexylalanyl)pyrrolidine
-
reversible
1-(L-cyclohexylalanyl)pyrrolidine
-
reversible
1-(L-isoleucyl)-1,2,5,6-tetrahydropyridine
-
reversible
1-(L-isoleucyl)-1,2,5,6-tetrahydropyridine
-
reversible
1-(L-isoleucyl)-3(R,S)-azidopyrrolidine
-
reversible
1-(L-isoleucyl)-3(R,S)-azidopyrrolidine
-
reversible
1-(L-isoleucyl)-3(R,S)-chloropyrrolidine
-
reversible
1-(L-isoleucyl)-3(R,S)-chloropyrrolidine
-
reversible
1-(L-isoleucyl)-3(R,S)-hydroxypyrrolidine
-
reversible
1-(L-isoleucyl)-3(R,S)-hydroxypyrrolidine
-
reversible
1-(L-isoleucyl)-3-pyrroline
-
reversible
1-(L-isoleucyl)-3-pyrroline
-
reversible
1-(L-isoleucyl)hexamethyleneimine
-
reversible
1-(L-isoleucyl)hexamethyleneimine
-
reversible
1-(L-isoleucyl)piperidine
-
reversible
1-(L-isoleucyl)piperidine
-
reversible
1-(L-isoleucyl)pyrrolidine
-
reversible
1-(L-isoleucyl)pyrrolidine
-
reversible
1-(L-lysyl)piperidine
-
reversible
1-(L-lysyl)piperidine
-
reversible
1-(L-lysyl)pyrrolidine
-
reversible
1-(L-lysyl)pyrrolidine
-
reversible
1-(L-phenylalanyl)pyrrolidine
-
reversible
1-(L-phenylalanyl)pyrrolidine
-
reversible
1-(L-prolyl)pyrrolidine
-
reversible
1-(L-prolyl)pyrrolidine
-
reversible
1-(L-tyrosyl)pyrrolidine
-
reversible
1-(L-tyrosyl)pyrrolidine
-
reversible
1-(L-valyl)pyrrolidine
-
reversible
1-(L-valyl)pyrrolidine
-
reversible
1-benzyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-benzyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-methyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-methyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
-
1-phenyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-phenyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-pyridin-2-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-pyridin-2-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-pyridin-4-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-pyridin-4-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)phenyl]piperazine
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)phenyl]piperazine
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
-
-
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
-
-
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
-
-
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
-
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
potent and selective DPPIV inhibitor, but it showed a significant loss of activity in the presence of plasma
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
-
-
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
-
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine
-
vildagliptin, reversible inhibitor
1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine
-
vildagliptin, reversible inhibitor, vildagliptin inhibits DPP4 activity by about 50% at a dosage of 0.3 mg/kg body weight
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-bromo-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-bromo-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
Syrrx106124
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
-
-
2-([6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]methyl)benzonitrile
-
2-([6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]methyl)benzonitrile
-
SYR322, alogliptin
2-([8-(3-aminopiperidin-1-yl)-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl]methyl)benzonitrile
-
-
2-([8-(3-aminopiperidin-1-yl)-1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl]methyl)benzonitrile
-
2-tert-butyl-5-[N-(2-hydroxy-1,1-dimethylethyl)glycyl-(4S)-4-fluoro-L-prolyl]-1,3,4-oxadiazole
-
pharmacokinetic data
2-tert-butyl-5-[N-(2-hydroxy-1,1-dimethylethyl)glycyl-(4S)-4-fluoro-L-prolyl]-1,3,4-oxadiazole
-
the inhibitor shows good potency against DPPIV, and good selectivity against DPPII, DPPVIII, and elastase
2-tert-butyl-5-[N-(2-hydroxy-1,1-dimethylethyl)glycyl-(4S)-4-fluoro-L-prolyl]-1,3,4-oxadiazole
-
pharmacokinetic data
2-[(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-methylpyrrolidin-3-yl]-N,N-dimethylacetamide
-
-
2-[(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-methylpyrrolidin-3-yl]-N,N-dimethylacetamide
-
-
2-[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylacetamide
-
-
2-[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylacetamide
-
-
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
-
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
-
-
2-[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
-
2-[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
-
-
2-[(8S)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
-
2-[(8S)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
-
-
2-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
-
-
2-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
-
-
3,4-dichloroisocoumarin
-
-
3,4-dichloroisocoumarin
0.1 mM, 18% inhibition
3-((2S,4S)-4-anilino-2-pyrrolidinylcarbonyl)-1,3-thiazolidine
-
IC50: 147 nmol/L
3-((2S,4S)-4-anilino-2-pyrrolidinylcarbonyl)-1,3-thiazolidine
-
IC50: 190 nmol/L
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
-
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
in vivo efficacy in rat models after oral administration. The inhibitor has potential for further development as antidiabetic agent
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-(pyridin-2-yl)butanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-(pyridin-2-yl)butanamide
-
87% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 31% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
-
86% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 18% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose; 88% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 41% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-cyclopentyl-3-methylbutanamide
-
-
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-cyclopentyl-3-methylbutanamide
-
81% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 60% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
-
selective and competitive dipeptidyl peptidase-IV inhibitor
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
-
selective and competitive dipeptidyl peptidase-IV inhibitor
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
-
selective and competitive dipeptidyl peptidase-IV inhibitor
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
-
i.e. E3024, pharmacokinetic profile
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
-
i.e. E3024, selective, and competitive
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
-
i.e. E3024, selective, and competitive
3-L-prolyl-1,3-thiazolidine
-
IC50: 538 nmol/L
3-L-prolyl-1,3-thiazolidine
-
IC50: 607 nmol/L
3-[(2S)-pyrrolidin-2-ylcarbonyl]-1,3-thiazolidine
-
3-[(2S)-pyrrolidin-2-ylcarbonyl]-1,3-thiazolidine
-
-
3-[(2S)-pyrrolidin-2-ylcarbonyl]-1,3-thiazolidine
-
-
3-[(2S,4S)-4-(2-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 18.2 nmol/L
3-[(2S,4S)-4-(2-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 21.8 nmol/L
3-[(2S,4S)-4-(2-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 24.1 nmol/L
3-[(2S,4S)-4-(2-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 41.3 nmol/L
3-[(2S,4S)-4-(3,4-dicyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 8.4 nmol/L
3-[(2S,4S)-4-(3,4-dicyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 10.8 nmol/L
3-[(2S,4S)-4-(3,4-methylenedioxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 29.0 nmol/L
3-[(2S,4S)-4-(3,4-methylenedioxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 34.5 nmol/L
3-[(2S,4S)-4-(3-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 11.1nmol/L
3-[(2S,4S)-4-(3-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 13.0 nmol/L
3-[(2S,4S)-4-(3-chloro-4-methoxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 19.9 nmol/L
3-[(2S,4S)-4-(3-chloro-4-methoxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 14.8 nmol/L
3-[(2S,4S)-4-(4-aminophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 105 nmol/L
3-[(2S,4S)-4-(4-aminophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 125 nmol/L
3-[(2S,4S)-4-(4-chlorophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 45.4 nmol/L
3-[(2S,4S)-4-(4-chlorophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 55.1 nmol/L
3-[(2S,4S)-4-(4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 25.2 nmol/L
3-[(2S,4S)-4-(4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 33.6 nmol/L
3-[(2S,4S)-4-(4-methanesulfonylphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 52.3 nmol/L
3-[(2S,4S)-4-(4-methanesulfonylphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 43.8 nmol/L
3-[(2S,4S)-4-(4-nitrophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 19.2 nmol/L
3-[(2S,4S)-4-(4-nitrophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 21.0 nmol/L
3-[(2S,4S)-4-(5-cyano-2-pyridyl)amino-2-pyrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 25.4 nmol/L
3-[(2S,4S)-4-(5-cyano-2-pyridyl)amino-2-pyrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 30.4 nmol/L
3-[(2S,4S)-4-(p-anisidino)-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 51.5 nmol/L
3-[(2S,4S)-4-(p-anisidino)-2-pyrrolidinylcarbonyl]-1,3-thiazolidine
-
IC50: 54.9 nmol/L
3-[(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylpropanamide
-
-
3-[(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylpropanamide
-
-
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
-
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
-
-
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-carboxamide
-
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-carboxamide
-
-
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
-
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
-
-
4-(4-nitrophenyl)-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
-
-
4-(4-nitrophenyl)-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
-
-
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
-
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
-
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
-
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
-
4-phenyl-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
-
-
4-phenyl-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
-
-
4-[(3R)-3-[[2-(4-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide
-
4-[(3R)-3-[[2-(4-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide
-
-
4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]morpholine
-
-
4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]morpholine
-
-
4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]benzene-1,2-dicarbonitrile
-
-
4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]benzene-1,2-dicarbonitrile
-
-
4-[[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]methyl]-2-methylbenzonitrile
-
4-[[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]methyl]-2-methylbenzonitrile
-
instability in human and dog plasma, but not in rat plasma. Unstable in fresh rat, dog, and human blood
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
-
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
-
-
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-chloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
-
5-chloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
in vivo plasma DPP-IV inhibition in Wistar rats
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
-
6-([(3S,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-3-yl]amino)pyridine-3-carbonitrile
-
IC50: 0.25 nmol/L
6-([(3S,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-3-yl]amino)pyridine-3-carbonitrile
-
IC50: 0.27 nmol/L
6-([2-((2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl)amino)ethyl]amino)pyridine-3-carbonitrile
-
IC50: 1.4 nmol/L
6-([2-((2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl)amino)ethyl]amino)pyridine-3-carbonitrile
-
IC50: 2.3 nmol/L
6-[(2-([2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]amino)ethyl)amino]pyridine-3-carbonitrile
-
IC50: 270 nmol/L
6-[(2-([2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]amino)ethyl)amino]pyridine-3-carbonitrile
-
IC50: 500 nmol/L
6-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
-
-
6-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
-
-
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
-
i.e. KR-62436, IC50: 0.00014 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
-
i.e. KR-62436, IC50: 0.00078 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
-
i.e. KR-62436, IC50: 0.00049 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1
7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-tert-butyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxamide
-
7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-tert-butyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxamide
-
-
8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
-
inhibition of plasma DPP-4 activity after oral administration
8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
-
linagliptin
8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
-
inhibition of plasma DPP-4 activity after oral administration
8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
-
inhibition of plasma DPP-4 activity after oral administration
Ala-Pro
-
hydrolysis of with Gly-Pro-4-nitroanilide
Ala-Pro-Gly
-
-
alogliptin
-
nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase, about 75% inhibition of DPP-4 24 h after treatment with 3 mg/kg alogliptin
alogliptin
-
highly selective dipeptidyl peptidase-4 inhibitor, at single doses up to 800 mg alogliptin the mean peak DPP-4 inhibition ranges from 93% to 99% and mean inhibition at 24 hours after dosing ranges from 74% to 97%
alogliptin
-
synonyms are alogliptin benzoate, SYR-085, SYR-322, SYR-619, SYR-11792, SYR-110085A, SYR-111791, or TAK-322, highly potent and selective dipeptidyl peptidase-IV inhibitor for the treatment of type 2 diabetes, non-covalent inhibitor of DPP-IV with selectivity of more than 10000fold over other proteases including tryptase, DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase and prolyl endopeptidase
alogliptin
-
nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase
alogliptin
-
competitive and reversible inhibitor
alogliptin
-
nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase, about 15% inhibition of DPP-4 24 h after treatment with 3 mg/kg alogliptin
alogliptin
-
i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, formerly SYR-322, potent and highly selective dipeptidyl peptidase-4 inhibitor, after 2 days alogliptin (0.002%, 0.01%, or 0.03%) dose-dependently inhibits DPP-4 activity by 28-82%
alogliptin
-
i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrilemonobenzoate, about 80% inhibition of DPP-4 after 4-week treatment with 45.7 mg/kg/day (0.03%) alogliptin
alogliptin
-
potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV
alogliptin
-
nanomolar inhibitor of DPP-4, i.e. 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]benzonitrile monobenzoate, exhibits 10000fold selectivity for DPP-4 over the closely related serine proteases DPP-2, DPP-8, DPP-9, fibroblast activation protein/seprase, prolyl endopeptidase, and tryptase, complete inhibition of DPP-4 24 h after treatment with 10 mg/kg alogliptin
ASP-8497
-
(2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, selective and competitive inhibitor of DPP-IV, ASP8497 is a DPP-IV inhibitor with long-acting antidiabetic effect that might be a potential agent for type 2 diabetes
ASP-8497
-
(2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, selective and competitive inhibitor of DPP-IV, ASP8497 is a DPP-IV inhibitor with long-acting antidiabetic effect that might be a potential agent for type 2 diabetes
ASP-8497
-
(2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, selective and competitive inhibitor of DPP-IV, ASP8497 is a DPP-IV inhibitor with long-acting antidiabetic effect that might be a potential agent for type 2 diabetes
ASP-8497
-
(2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, selective and competitive inhibitor of DPP-IV, ASP8497 is a DPP-IV inhibitor with long-acting antidiabetic effect that might be a potential agent for type 2 diabetes
ASP8497
-
potent, selective, and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity, i.e. (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate
ASP8497
-
potent, selective, and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity, i.e. (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate
ASP8497
-
i.e. [(2S,4S)-4-fluoro-1-([4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, the combination of 1 mg/kg ASP8497 with antidiabetic drugs can be useful for correcting the postprandial hyperglycemia seen with type 2 diabetes
ASP8497
-
potent, selective, and competitive dipeptidyl peptidase-IV inhibitor with antihyperglycemic activity, i.e. (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate
ASP8497
-
i.e. (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, potent DPP-IV inhibitor and potential agent for the treatment of type 2 diabetes
ASP8497
-
i.e. (2S,4S)-4-fluoro-1-([[4-methyl-1-(methylsulfonyl)-piperidin-4-yl]amino]acetyl)pyrrolidine-2-carbonitrile monofumarate, potent and long-acting inhibitor of plasma DPP-IV activity, inhibitory activity lasts up to 24 h when administered at 5 mg/kg twice a day or 10 mg/kg once a day
bacitracin
-
-
bestatin
-
-
BI 1356
-
-
BI 1356
-
proposed trade name ONDERO, highly potent and selective DPP-4 inhibitor
BI 1356
-
proposed trade name ONDERO, exhibits a prominent concentration-dependent plasma protein binding due to a saturable high affinity binding to the DPP-4 target in plasma
BI 1356
-
competitive inhibitor, i.e. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione, proposed trade name Ondero, BI 1356 is more than 10000fold selective for DPP-4 than DPP-8, DPP-9, aminopeptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin and is 90-fold more selective than for fibroblast activation protein in vitro
BI 1356
-
proposed trade name ONDERO, exhibits a prominent concentration-dependent plasma protein binding due to a saturable high affinity binding to the DPP-4 target in plasma
BI 1356
-
competitive inhibitor, i.e. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione, proposed trade name Ondero, BI 1356 is more than 10000fold selective for DPP-4 than DPP-8, DPP-9, aminopeptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin and is 90-fold more selective than for fibroblast activation protein in vitro
BI 1356
-
proposed trade name ONDERO, highly potent and selective DPP-4 inhibitor
BI 1356
-
proposed trade name ONDERO, exhibits a prominent concentration-dependent plasma protein binding due to a saturable high affinity binding to the DPP-4 target in plasma
BI 1356
-
competitive inhibitor, i.e. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione, proposed trade name Ondero, BI 1356 is more than 10000fold selective for DPP-4 than DPP-8, DPP-9, aminopeptidases N and P, prolyloligopeptidase, trypsin, plasmin, and thrombin and is 90-fold more selective than for fibroblast activation protein in vitro
bis(4-acetamidophenyl) 1-((S)-prolyl)pyrrolidine-2(R,S)-phosphonate
-
i.e. AB192
bis(4-acetamidophenyl) 1-((S)-prolyl)pyrrolidine-2(R,S)-phosphonate
-
i.e. AB192
bis(4-acetamidophenyl) 1-(S)-prolylpyrrolidine-2(R,S)-phosphonate
-
AB-192, irreversible inhibitor
bis(4-acetamidophenyl) 1-(S)-prolylpyrrolidine-2(R,S)-phosphonate
-
AB-192, irreversible inhibitor, AB-192 sufficiently inhibits DPP4 only in the higher dosage range of more than 1mg/kg body weight
bis(4-[(ethoxycarbonyl)-methylaminocarbonyl]-phenyl) 1-((S)-prolyl)pyrrolidine-2-(R,S)-phosphonate
-
i.e. AB207
bis(4-[(ethoxycarbonyl)-methylaminocarbonyl]-phenyl) 1-((S)-prolyl)pyrrolidine-2-(R,S)-phosphonate
-
i.e. AB207
bis-(4-nitrophenylphosphate)
-
-
bis-(4-nitrophenylphosphate)
-
-
Cd2+
-
CdCl2
Co2+
-
-
Cu2+
-
-
Cu2+
-
1.0 mM, 15% inhibition
Cu2+
-
1 mM CuSO4, 15% inhibition
Cu2+
-
1 mM, 17% inhibition
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
1.0 mM, 2 h, 40°C, complete inhibition
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
-
diisopropyl fluorophosphate
-
-
diisopropylfluorophosphate
1 mM, complete inhibition; 1 mM, complete inhibition
diisopropylfluorophosphate
-
1.0 mM, complete inhibition
diisopropylfluorophosphate
-
marked inhibition at 1 mM
Diprotin A
-
specific DPP4 inhibitor
Diprotin A
-
specific inhibitor of DPP4 activity, diprotin A is L-LeuL-Pro-L-Leu, coincubation of a 0.5, 1, 2, 5, and 10fold concentration of diprotin A (relative to the L-Ala-L-Pro-7-amido-4-trifluoromethylcoumarin substrate concentration) results in 52, 71, 77, 86, and 89% reduction in DPP4 activity, respectively
Diprotin A
-
DppIV-specific inhibitor
Diprotin A
-
specific inhibitor of DPPIV enzyme activity, almost complete inhibition at 0.1 mM
Diprotin A
-
specific inhibition
Diprotin A
dipeptidyl peptidase IV in soluble and membrane-bound fractions from the hypothalamus and hippocampus areas is distinguished kinetically as insensitive and sensitive to diprotin A, respectively
Diprotin A
1 mM, 71% inhibition
Diprotin B
-
-
Diprotin B
-
specific inhibition
EDTA
-
1.0 mM, 40°C, 20 h, partial
ethyl 4-[3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanoyl]piperazine-1-carboxylate
-
-
ethyl 4-[3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanoyl]piperazine-1-carboxylate
-
-
ethyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
-
ethyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
-
-
ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
-
ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
-
-
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
-
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
-
-
Gly-L-Pro
-
hydrolysis of Gly-Pro-4-nitroanilide
Gly-L-Pro
-
competitive inhibition of hydrolysis of Gly-L-Pro-4-nitroanilide
Gly-Pro-Ala
-
-
H-(S)-alaninyl-(R)-boro-proline
-
-
H-(S)-alaninyl-(R)-boro-proline
-
-
H-(S)-alaninyl-(R)-boro-proline
-
-
H-(S)-Glu-(R)-boro-alanine
-
-
H-(S)-Glu-(R)-boro-alanine
-
-
H-(S)-Glu-(R)-boro-alanine
-
-
H-(S)-glutaminyl-(R)-boro-alanine
-
-
H-(S)-glutaminyl-(R)-boro-alanine
-
-
H-(S)-glutaminyl-(R)-boro-alanine
-
-
H-(S)-glutamyl-(R)-boro-proline
-
-
H-(S)-glutamyl-(R)-boro-proline
-
-
H-(S)-glutamyl-(R)-boro-proline
-
-
H-(S)-valinyl-(R)-boro-alanine
-
-
H-(S)-valinyl-(R)-boro-alanine
-
-
H-(S)-valinyl-(R)-boro-alanine
-
-
H-(S)-valinyl-(R)-boro-proline
-
-
H-(S)-valinyl-(R)-boro-proline
-
-
H-(S)-valinyl-(R)-boro-proline
-
-
H-glycyl-(R)-boro-proline
-
-
H-glycyl-(R)-boro-proline
-
-
H-glycyl-(R)-boro-proline
-
-
Hg2+
-
HgCl2
Hg2+
1 mM, 70% inhibition
human HIV-1 Lys2-Tat(1-9) peptide
-
amino acid sequence MKPVDPNIE, linear mixed type inhibition
-
human HIV-1 Lys2-Tat(1-9) peptide
-
amino acid sequence MKPVDPNIE
-
human HIV-1 Tat(1-9) peptide
-
amino acid sequence MDPVDPNIE, N-terminal peptide of the viral Tat protein, inhibits the enzyme activity and cell proliferation, parabolic mixed type inhibition
-
human HIV-1 Tat(1-9) peptide
-
amino acid sequence MDPVDPNIE, N-terminal peptide of the viral Tat protein, natural inhibitor, inhibits antigen-, anti-CD-3- and mitogen-induced activation of human T-cells
-
human HIV-1 Trp2-Tat(1-9) peptide
-
amino acid sequence MWPVDPNIE, linear mixed type inhibition
-
human HIV-1 Trp2-Tat(1-9) peptide
-
amino acid sequence MWPVDPNIE, most effective Tat peptide inhibitor derivative
-
Ile-Pro
-
competitive
Ile-pyrrolidide
-
competitive
Ile-pyrrolidide
-
competitive
Ile-thiazolidide
-
competitive
Ile-thiazolidide
-
competitive
iodoacetate
-
1.0 mM, partial
isoleucine thiazolidide
-
-
isoleucine thiazolidide
-
in vivo study
isoleucine thiazolidide
-
i.e. P32/98. Enhancement of incretin with the DPP-4 inhibitor P32/98 has therapeutic effects in hyperinsulinaemia, hyperglycaemia and impaired glucose toleranceIGT in Zucker rats with incipient impaired glucose tolerance and manifest impaired glucose tolerance. Apparently, administration of P32/98 in Zucker rats with incipient impaired glucose tolerance results in more efficient beta-cell function, which is associated with less need for insulin to cope with deterioration of glucose tolerance. P32/98 has a strong effect on dyslipidaemia in manifest impaired glucose tolerance. P32/98 has no side effect on intestinal growth. Daily intake of P32/98 is a promising strategy for treatment of glucose intolerance and has the potential to prevent type 2 diabetes
isoleucine thiazolidide
-
-
LAF-237
-
vildagliptin, potent, selective DPP IV inhibitor, the proprietary name is Galvus, covalently bound and reversible inhibitor
linagliptin
-
Bl-1356, the proprietary name is Ondero
Lys-pyrrolidide
-
-
Lys[Z(NO2)]-pyrrolidide
-
simultaneous application of DP IV and aminopeptidase N inhibitors significantly suppresses DNA synthesis in mitogen- or anti-CD3-stimulated human T cells in vitro when compared to the use of a single DP IV or aminopeptidase N inhibitor. The combined action of DP IV and aminopeptidase N inhibitors markedly increases TGF-beta1 production associated with the observed immunosuppressive effects. In vivo, targeting both DP IV and aminopeptidase N leads to a potent treatment of experimental autoimmune encephalomyelitis an animal model of multiple sclerosis
Lys[Z(NO2)]-pyrrolidide
-
the dipeptidyl peptidase IV inhibitor suppresses proliferation, enhances terminal differentiation and slightly decreases total neutral lipid production in sebocytes
Lys[Z(NO2)]-pyrrolidide
-
-
Lys[Z(NO2)]-pyrrolidide
-
non-specific DPIV inhibitor
Lys[Z(NO2)]-pyrrolidide
-
-
Lys[Z(NO2)]-pyrrolidide
-
non-selective inhibitor of DP IV-like activity; non-specific DPIV inhibitor, 96% inhibition at 0.01 mM
Lys[Z(NO2)]-pyrrolidide
-
inhibition of DPPIV catalytic activity is associated with inhibition of NHE3-mediated NaHCO3 reabsorption in the native renal proximal tubule
Lys[Z(NO2)]-thiazolidide
-
the dipeptidyl peptidase IV inhibitor suppresses proliferation, enhances terminal differentiation and slightly decreases total neutral lipid production in sebocytes
Lys[Z(NO2)]-thiazolidide
-
non-specific DPIV inhibitor
Lys[Z(NO2)]-thiazolidide
-
non-selective inhibitor of DP IV-like activity; non-specific DPIV inhibitor
Mn2+
-
-
Mn2+
-
1.0 mM, 22% inhibition
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
-
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
-
-
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
-
-
N-acetyl-(S)-valinyl-(R)-boro-proline
-
-
N-acetyl-(S)-valinyl-(R)-boro-proline
-
-
N-acetyl-(S)-valinyl-(R)-boro-proline
-
-
N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]-3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanamide
-
-
N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]-3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanamide
-
66% plasma DPP-IV inhibition after 30 min at 3 mg/kg oral dose, 30% plasma DPP-IV inhibition after 8 h at 3 mg/kg oral dose
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
-
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
-
NEM
-
1.0 mM, partial
Nepsilon-nitrobenzyloxycarbonyl-Lys-Pro
-
competitive
Nepsilon-nitrobenzyloxycarbonyl-Lys-Pro
-
competitive
Nepsilon-nitrobenzyloxycarbonyl-Lys-pyrrolidide
-
competitive
Nepsilon-nitrobenzyloxycarbonyl-Lys-pyrrolidide
-
-
Nepsilon-nitrobenzyloxycarbonyl-Lys-pyrrolidide
-
competitive
Nepsilon-nitrobenzyloxycarbonyl-Lys-thiazolidide
-
competitive
Nepsilon-nitrobenzyloxycarbonyl-Lys-thiazolidide
-
-
Nepsilon-nitrobenzyloxycarbonyl-Lys-thiazolidide
-
suppresses mitogen- and alloantigen-induced T-cell proliferation, B-cell differentiation, immunoglobulin secretion and modulates cytokine production
Nepsilon-nitrobenzyloxycarbonyl-Lys-thiazolidide
-
competitive
Ni2+
-
1 mM
NVP DPP728
-
-
NVP DPP728
-
slow-binding inhibitor
NVP DPP728
-
in vivo study
NVP-DPP728
-
i.e. 1-[2-[5-(cyanopyridin-2-yl)amino]ethylamino]acetyl-2-cyano-(S)-pyrrolidide monohydrochloride
NVP-DPP728
-
potent and selective DPP-4 inhibitor
PCMB
-
-
PCMB
-
1.0 mM, 15 min, 40°C, complete inhibition
PF-00734200
-
potent, competitive DPP-IV inhibitor, complete inhibition of DPP-IV for over 24 h after treatment with one single dose of 300 mg PF-00734200
PF-00734200
-
i.e. 3,3-(difluoropyrrolidin-1-yl)-((2S,4S)-4-(4-(pyrimidin-2-yl) piperazin-1-yl)pyrrolidin-2-yl)methanone, inhibitor of dipeptidyl peptidase IV for the treatment of diabetic complications and other disorders
Phe-Pro-PSI[P(OEt)2]
-
diastereomeric mixture, competitive
Phe-Pro-PSI[P(OEt)2]
-
diastereomeric mixture, competitive
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
-
1.0 mM, partial
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
-
slight
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
-
slight
phenylmethylsulfonyl fluoride
-
resistant to inhibition
phenylmethylsulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
-
-
PHX1149
-
pharmacokinetic and pharmacodynamic assessments of the dipeptidyl peptidase-4 inhibitor, double-blind, placebo-controlled, single- and multiple-dose studies in healthy subjects
PHX1149
-
selective DPP4 inhibitor, DPP4 inhibition on day 28 is 53%, 73% and 78% at 24 h after treatment with 100, 200 and 400 mg PHX1149, respectively
PMSF
-
2.5 mM, 78% loss of activity
Pro-Ala
-
hydrolysis of Gly-Pro-4-nitroanilide
Pro-Ala
-
hydrolysis of L-Pro-L-Ala
PSN-9301
-
-
PSN-9301
-
P93/01, reversible inhibition, short acting
saxagliptin
-
-
saxagliptin
-
the oral dipeptidyl peptidase 4 inhibitor is efficious both alone and in association with other oral anti-diabetic agents and may be administered in a single daily dose, the inhibitor has low risk of hypoglycemia and does not affect body weight
saxagliptin
-
highly potent and selective inhibitor of DPP-IV
saxagliptin
-
the proprietary name is Onglyza
saxagliptin
-
BMS-477118, competitive and reversible inhibitor
saxagliptin
-
highly selective dipeptidyl peptidase-IV inhibitor for the treatment of type 2 diabetes, synonyms are BMS-477118, Onglyza, and saxagliptin hydrate, saxagliptin is 400fold and 75fold more potent against DPP-IV than DPP-8 or DPP-9 respectively, DPP-IV is inhibited dose-dependently, with maximal inhibition at 150 mg/day
saxagliptin
-
BMS-477178, (1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]-hexane-3-carbonitrile hydrochloride
SDS
-
1.0% complete inhibition
SDS
35 mM, complete inhibition
sitagliptin
-
the systemic clearance of sitagliptin is driven primarily by renal elimination of intact parent drug
sitagliptin
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
sitagliptin
-
potent, competitive, reversible inhibitor
sitagliptin
-
highly selective orally active dipeptidyl peptidase-4 inhibitor recently approved in the United States for the treatment of type 2 diabetes. Plasma AUC0_1 (area under the plasma concentration-time curve) increases in a dose-proportional manner over the 25-400 mg dose range
sitagliptin
-
dipeptidyl peptidase-4 inhibitor approved in the United States for the treatment of type 2 diabetes. The absolute bioavailability of sitagliptin final market image tablets is approximately 87%. Sitagliptin is Food does not affect the pharmacokinetics of sitagliptin and therefore can be administered without regard to food generally well tolerated when administered orally or intravenously
sitagliptin
-
sitagliptin is a selective DPP-4 inhibitor that enhances intact incretin levels and improves 24-h glycemic control in patients with type 2 diabetes
sitagliptin
-
in a 24-week study, sitagliptin 100 mg once daily added to ongoing pioglitazone therapy is effective and well tolerated in these patients with type 2 diabetes who had not achieved adequate glycemic control with pioglitazone alone
sitagliptin
-
potent and highly specific inhibitor of DPP-4
sitagliptin
-
highly selective DPP-4 inhibitor for the treatment of type 2 diabetes
sitagliptin
-
in a 24-week study, once-daily sitagliptin monotherapy improves glycemic control in the fasting and postprandial states, improves measures of beta-cell function, and is well tolerated in patients with type 2 diabetes
sitagliptin
-
highly effective antihyperglycaemic agent that augments insulin secretion and reduces glucagon secretion via glucose-dependent mechanism
sitagliptin
-
addition of sitagliptin 50 mg b.i.d. to ongoing metformin therapy improves 24-h glycaemic control and beta-cell function, and is generally well tolerated in patients with type 2 diabetes
sitagliptin
-
the addition of sitagliptin compared with glipizide provides similar HbA1c-lowering efficacy over 52 weeks in patients with type 2 diabetes on ongoing metformin therapy. Sitagliptin is generally well tolerated, with a lower risk of hypoglycaemia relative to glipizide and with weight loss compared with weight gain with glipizide
sitagliptin
-
sitagliptin significantly improves glycaemic control and is well tolerated in patients with type 2 diabetes mellitus who have inadequate glycaemic control on exercise and diet
sitagliptin
-
primary route of excretion of is via the kidneys, with a mean value of 87% of the administered dose recovered in urin. Because sitagliptin is eliminated primarily unchanged into urine, it is not expected to be a victim of metabolismbased drug interactions
sitagliptin
-
sitagliptin is one-daily, orally active, potent and selective DPP-4 inhibitor, which reduces both fasting and postprandial glucose levels and improves summary measures of beta-cell function to produce clinically meaningful reductions in HbA1c concentrations. Efficiacy as both a monotherapy and in combination with merformin or pioglitazone, without causing weight gain
sitagliptin
-
does not alter the single-dose pharmacokinetics of rosiglitazone in healthy subjects
sitagliptin
-
the oral dipeptidyl peptidase 4 inhibitor is efficious both alone and in association with other oral anti-diabetic agents and may be administered in a single daily dose, the inhibitor has low risk of hypoglycemia and does not affect body weight
sitagliptin
-
inhibitor for the treatment of type 2 diabetes, is excreted into the urine via active tubular secretion and glomerular filtration in humans. Sitagliptin is transported by human organic anion transporter hOAT3, organic anion transporting polypeptide OATP4C1, and multidrug resistance (MDR) P-glycoprotein, but not by human organic cation transporter 2 hOCT2, hOAT1, oligopeptide transporter hPEPT1, OATP2B1, and the multidrug resistance proteins MRP2 and MRP4
sitagliptin
-
selective inhibitor of DPP-IV, over 80% inhibition of DPP-IV with a single oral dose of 50 mg
sitagliptin
-
the proprietary name is Januvia
sitagliptin
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
sitagliptin
-
MK-0431 or Januvia, competitive and reversible inhibitor
sitagliptin
-
trade name Januvia
sitagliptin
-
MK-0431, trade name Januvia, 100 mg sitagliptin inhibits plasma DPP-4 activity for more than 16 hours after a single administration
sitagliptin
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
sitagliptin
-
MK0431, potent inhibitor, inhibition of DPP-IV with sitagliptin (dose of 4g/kg/day over 7 days) prolongs islet graft retention in a type 1 diabetes mouse model
sitagliptin
-
MK-0431, (2 R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo-[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine phosphate
sitagliptin
-
the systemic clearance of sitagliptin in rats is driven primarily by renal elimination of intact parent drug, with contribution from biliary excretion and metabolism (minor). Active transport mechanisms are probably involved in the renal elimination of sitagliptin
sitagliptin
-
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
SSR-162369
-
-
SSR-162369
-
reversibile and long-lasting inhibition
thromboxane A2 receptor peptide TXA2-R(1-9)
-
N-terminal MWP sequence motif MWPNGSSLG, potent competitive inhibitor, possibly functionally involved in antigen presentation by inhibiting T-cell expressed enzyme
-
thromboxane A2 receptor peptide TXA2-R(1-9)
-
N-terminal MWP sequence motif MWPNGSSLG, strong inhibitor
-
Triton X-100
-
1.0%, 32% inhibition
Triton X-100
16 mM, 22% inhibition
Trp-Pro
-
linear mixed-type
Trp-Pro
-
linear mixed-type
Trp-pyrrolidide
-
competitive
Trp-pyrrolidide
-
competitive
Trp-thiazolidide
-
competitive
Trp-thiazolidide
-
competitive
Val-pyrrolidide
-
-
vildagliptin
-
specific inhibitor of DPPIV
vildagliptin
-
complete inhibition over 4 h after treatment with a single oral dose of 1 mg/kg vildagliptin
vildagliptin
-
i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine
vildagliptin
-
LAF237, 1-[[3-hydroxy-1-adamantyl]amino]acetyl-2-cyano-(S)-pyrrolidine
vildagliptin
-
competitive and reversible inhibitor of DPP-4. It is highly specific for DPP-4 relative to other peptidases. Vildagliptin is rapidly and almost completely absorbed following oral administration and inhibits plasma DPP-4 activity by 90% within 30-60 min. DPP-4 activity remains significantly inhibited for more than 12 h following a single dose
vildagliptin
-
in pre-diabetic subjects, a 12-week treatment with vildagliptin markedly increases postmeal levels of active glucagon-like peptide 1 and gastric inhibitory polypeptide, improves both alpha- and beta-cell function, decreases postprandial hyperhlycemia and decreases A1C levels. Vildagliptin is well tolerated and weight neutral and does not cause hypoglycemia
vildagliptin
-
highly effective antihyperglycaemic agent that augments insulin secretion and reduces glucagon secretion via glucose-dependent mechanism
vildagliptin
-
pharmacokinetic studies in patients with type 2 diabetes
vildagliptin
-
there is no significant difference in exposure to vildagliptin in patients with mild, moderate or severe hepatic impairment
vildagliptin
-
twelve-week monotherapy with the DPP-4 inhibitor vildagliptin improves glycemic control in subjects with type 2 diabetes
vildagliptin
-
suppresses endogenous glucose production and enhances islet function after single-dose administration in type 2 diabetic patients
vildagliptin
-
the oral dipeptidyl peptidase 4 inhibitor is efficious both alone and in association with other oral anti-diabetic agents and may be administered in a single daily dose, the inhibitor has low risk of hypoglycemia and does not affect body weight
vildagliptin
-
highly potent and stable selective inhibitor of DPP-IV, over 90% inhibition of DPP-IV with a single oral dose of 100 mg
vildagliptin
-
NVP-LAF237
vildagliptin
-
the proprietary name is Galvus
vildagliptin
-
i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine
vildagliptin
-
LAF237 or Galvus, competitive and reversible inhibitor
vildagliptin
-
more than 90% inhibition within 30 min of administration of vildagliptin and glyburide, while glyburide alone has no effect on DPP-4 activity
vildagliptin
-
potent, selective DPP-4 inhibitor
vildagliptin
-
trade name Galvus
vildagliptin
-
LAF237, 1-[[3-hydroxy-1-adamantyl]amino]acetyl-2-cyano-(S)-pyrrolidine
vildagliptin
-
LAF237, trade name Galvus, 100 mg vildagliptin inhibits plasma DPP-4 activity for more than 16 hours after a single administration
vildagliptin
-
specific inhibitor of DPPIV
vildagliptin
-
i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine
vildagliptin
-
acutely lowers blood glucose and enhances glucose-stimulated insulin secretion in wild-type mice and in mice with targeted disruption of single incretin receptors
vildagliptin
-
LAF237, 1-[[3-hydroxy-1-adamantyl]amino]acetyl-2-cyano-(S)-pyrrolidine
vildagliptin
-
LAF237, 1-[[(3-hydroxy-1-adamantyl)-amino]acetyl]-2-cyano-(S)-pyrrolidine
vildagliptin
vildagliptin improves glucose tolerance and increases the beta-cell mass by reducing beta-cell apoptosis in Insulin Receptor Substrate-2-Knockout mice fed a high-fat diet, and the reduction of beta-cell apoptosis by vildagliptin is independent of the Insulin Receptor Substrate-2 expression in the cells
vildagliptin
-
liraglutide, a long-acting glucagon-like peptide-1 analog, reduces body weight and food intake in obese candy-fed rats, whereas a dipeptidyl peptidase-IV inhibitor, vildagliptin, does not
vildagliptin
-
i.e. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine
Zn2+
-
1 mM
Zn2+
-
mixed type inhibition
Zn2+
-
1.0 mM, 22% inhibition
[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]acetic acid
-
-
[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]acetic acid
-
-
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
-
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
-
-
additional information
no inhibition by 5 mM EDTA or 0.005 mg/ml leupeptin; no inhibition by 5 mM EDTA or 0.005 mg/ml leupeptin
-
additional information
no inhibition by 5 mM EDTA or 0.005 mg/ml leupeptin; no inhibition by 5 mM EDTA or 0.005 mg/ml leupeptin
-
additional information
-
no inhibition by 5 mM EDTA or 0.005 mg/ml leupeptin; no inhibition by 5 mM EDTA or 0.005 mg/ml leupeptin
-
additional information
-
therapeutical perspectives for dipeptidyl peptidase IV inhibitors
-
additional information
alpha/beta-hydrolase domain and beta-propeller domain both participate in inhibitor binding
-
additional information
-
alpha/beta-hydrolase domain and beta-propeller domain both participate in inhibitor binding
-
additional information
-
conformational flexibility of tyr548 is unique among protein family members and may be utilized in drug design to achieve peptidase selectivity
-
additional information
-
4beta-[4-(hydroxyphenyl)prolyl]prolinenitriles show a potent inhibitory activity with a long duration of action. Metabolic formation of the corresponding phenol glucuronates is found to contribute to their long duration of action
-
additional information
in order to obtain information regarding the design of selective DPP4 inhibitors, a 3D-QSAR study is conducted using DPP4, which were evaluated in vitro for their inhibition of DPP4. A highly predictive CoMFA model based on the fast-docking for DPP4 inhibitors is obtained
-
additional information
-
substituted 3-aminopiperidines are evaluated as DPP-4 inhibitors. The inhibitors show good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9)
-
additional information
-
beta-amino amides containing triazolopiperazine heterocycles are potent, selective, orally active dipeptidyl peptidase IV inhibitors. These compounds display excellent oral bioavailability and good overall pharmacokinetic profiles in preclinical species
-
additional information
-
a three-dimensional pharmacophore model is a useful tool for designing novel DPP-IV inhibitors
-
additional information
-
DPP-IV inhibitors suppress the degradation of a variety of bioactive peptides, including GLP-1
-
additional information
3D-QSAR analysis of several DPP-IV inhibitors, which are aligned by the receptor-based technique
-
additional information
3D-QSAR studies on fluoropyrrolidine amide dipeptidyl peptidase IV inhibitors by comparative molecular field analysis and comparative molecular similarity analysis
-
additional information
-
when assayed against L-Ala-L-Pro-p-nitroanilide or Gly-L-Pro-p-nitroanilide, the activity of DPP9 is not affected by the presence of reducing agents, such as 1 mM dithiothreitol or 18 mM beta-mercaptoethanol
-
additional information
interactions important for binding are the pi-pi stacking interaction of the pyridopyrimidine-dione ring with Tyr547, its H-bond interaction to the backbone NH of Tyr631 and the OH of Ser630, and polar interactions between the basic amine and Glu205, Glu206 and Tyr662, high selectivity for dipeptidyl peptidase IV over dipeptidyleptidase DPP8
-
additional information
development of a multiple linear regressions model for predicting the IC50 of a theoretical molecule. Best model is the penta-parametric with the descriptors molecular weight, molecular volume, molecular density, superficial area and polarizability
-
additional information
-
development of a multiple linear regressions model for predicting the IC50 of a theoretical molecule. Best model is the penta-parametric with the descriptors molecular weight, molecular volume, molecular density, superficial area and polarizability
-
additional information
-
no inhibition by EDTA, E-64, pepstatin A or leupeptin
-
additional information
-
-
-
additional information
-
selective inhibition of DPP-IV does not impair T dependent immune responses to antigenic challenge
-
additional information
not affected by dithiothreitol
-
additional information
-
not affected by dithiothreitol
-
additional information
-
inhibitory mechanism, the N-terminus sequence of hemorphins influence the interaction between hemorphins and the enzyme
-
additional information
conformational flexibility of tyr548 is unique among protein family members and may be utilized in drug design to achieve peptidase selectivity
-
additional information
-
4beta-[4-(hydroxyphenyl)prolyl]prolinenitriles show a potent inhibitory activity with a long duration of action. Metabolic formation of the corresponding phenol glucuronates is found to contribute to their long duration of action
-
additional information
-
in male Zucker diabetic rats, DPP-4 inhibition shows a delay in onset of diabetes and improved glucose tolerance and insulin secretion
-
additional information
-
no inhibition by sulfhydryl-blocking agents and metal chelators, no inhibition by Pro, Pro-Gly, and Pro-Gly-Gly
-
additional information
-
proline substrates, Pro in P1, with R configuration in P2 are inhibitors of the hydrolysis of proline substrates with an S,S configuration in an uncompetitive or mixed inhibition type
-
additional information
-
inhibition kinetics
-
additional information
-
the MWP sequence motif is important for inhibition
-
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0.000013
(11bS)-9,10-dimethoxy-3-(3-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.00022
(11bS)-9,10-dimethoxy-3-phenyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.0013
(1R)-1-(4-bromophenyl)-2-(2,5-difluorophenyl)ethanamine
Homo sapiens
-
-
0.000107
(1R)-1-[4-(3-chloropyridin-4-yl)phenyl]-2-(2,5-difluorophenyl)ethanamine
Homo sapiens
-
-
0.000253
(1R)-2-(2,5-difluorophenyl)-1-(4-pyridin-4-ylphenyl)ethanamine
Homo sapiens
-
-
0.0000055
(1R)-2-([(3R,4R)-4-amino-1-[1-(4-ethynylphenyl)ethyl]pyrrolidin-3-yl]carbonyl)cyclopentanecarbonitrile
Homo sapiens
-
0.0000038
(1R)-2-([(3R,4R)-4-amino-1-[2-methyl-4-(1H-1,2,4-triazol-1-yl)benzyl]pyrrolidin-3-yl]carbonyl)cyclopentanecarbonitrile
Homo sapiens
-
0.000046
(1R)-2-([(3R,4R)-4-amino-1-[3-methyl-4-(1H-1,2,4-triazol-1-yl)benzyl]pyrrolidin-3-yl]carbonyl)cyclopentanecarbonitrile
Homo sapiens
-
0.0000035
(1R)-2-[[(3R,4R)-4-amino-1-(3,4-dihydro-2H-chromen-4-yl)pyrrolidin-3-yl]carbonyl]cyclopentanecarbonitrile
Homo sapiens
-
0.000003
(1R)-2-[[(3R,4R)-4-amino-1-[1-[4-(1H-1,2,4-triazol-1-yl)phenyl]ethyl]pyrrolidin-3-yl]carbonyl]cyclopentanecarbonitrile
Homo sapiens
-
0.00000021
(1R,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
Rattus norvegicus
-
-
0.0000053
(1R,3S)-2-([(3R,4R)-4-amino-1-[4-(5-methyl-1,3,4-oxadiazol-2-yl)benzyl]pyrrolidin-3-yl]carbonyl)-3-fluorocyclopentanecarbonitrile
Homo sapiens
-
0.00032
(1R,4R,6S,10S)-6,10-dihydroxy-4-methyl-2-oxabicyclo[4.3.1]dec-7-ene-8-carboxylic acid
Homo sapiens
-
pH 8.0, 37°C
0.000048
(1S)-1-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-2-[(3S)-3-fluoropyrrolidin-1-yl]-2-oxoethanaminium
Homo sapiens
0% human serum
0.000039 - 0.000073
(1S)-1-cyclohexyl-2-(3,3-difluoropyrrolidin-1-yl)-2-oxoethanamine
0.00017
(1S)-1-cyclohexyl-2-(3-fluoropyrrolidin-1-yl)-2-oxoethanamine
Homo sapiens
-
pH 8.0, 37°C
0.00011
(1S)-1-cyclohexyl-2-oxo-2-(3,3,4,4-tetrafluoropyrrolidin-1-yl)ethanamine
Homo sapiens
-
pH 8.0, 37°C
0.000012
(1S,2R)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-3-cyclopentylidene-1-cyclopropyl-3-fluoropropan-2-aminium
Rattus norvegicus
-
-
0.000021
(1S,2R,5S)-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-2-(2,4,5-trifluorophenyl)cyclohexanamine
Homo sapiens
-
-
0.00000019
(1S,2S)-1-(4'-fluorobiphenyl-4-yl)-3-[(3S)-3-fluoropyrrolidin-1-yl]-3-oxo-1-(1H-tetrazol-1-yl)propan-2-amine
Homo sapiens
-
0.000013
(1S,2S)-1-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopropyl-3-[(3S)-3-fluoropyrrolidin-1-yl]-3-oxopropan-2-aminium
Rattus norvegicus
-
-
0.0000034
(1S,3S,5S)-2-[(2S)-2-amino-2-(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile
Homo sapiens
-
-
0.000023
(2R)-1-(2,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00000059
(2R)-1-(2,4-difluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.000082
(2R)-1-(2,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00018
(2R)-1-(2,5-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00000027 - 0.00027
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
0.00013
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(2-phenyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl)butan-2-amine
Rattus norvegicus
-
-
0.000065
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(3-pyridin-4-yl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)butan-2-amine
Rattus norvegicus
-
-
0.00014
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
Rattus norvegicus
-
-
0.000027
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000065
(2R)-1-(2,5-difluorophenyl)-4-[(4R)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00019
(2R)-1-(2,5-difluorophenyl)-4-[(4S)-1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00022
(2R)-1-(2,5-difluorophenyl)-4-[1-(2-methylpropyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00025
(2R)-1-(2,5-difluorophenyl)-4-[1-(4-fluorobenzyl)-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00018
(2R)-1-(2,5-difluorophenyl)-4-[1-ethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00015
(2R)-1-(2,5-difluorophenyl)-4-[1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00028
(2R)-1-(2,5-difluorophenyl)-4-[2-(4-fluorophenyl)-1-methyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00003
(2R)-1-(2,5-difluorophenyl)-4-[3-(2,5-difluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00026
(2R)-1-(2,5-difluorophenyl)-4-[3-(2-methylpropyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00025
(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorobenzyl)-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00006
(2R)-1-(2,5-difluorophenyl)-4-[3-(4-fluorophenyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00023
(2R)-1-(2,5-difluorophenyl)-4-[3-ethyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.00013
(2R)-1-(2,5-difluorophenyl)-4-[3-methyl-2-(trifluoromethyl)-3,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxobutan-2-amine
Rattus norvegicus
-
-
0.000084
(2R)-1-(2-chloro-4,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000145
(2R)-1-(2-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.00000093
(2R)-1-(2-fluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.000098
(2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
0.00000098
(2R)-1-(2-methylphenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.000002
(2R)-1-(3,4-dichlorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.00158
(2R)-1-(3,4-dichlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.0000017
(2R)-1-(3,4-difluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.000128
(2R)-1-(3,4-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000059
(2R)-1-(3-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000002
(2R)-1-(3-fluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.000135
(2R)-1-(3-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000076
(2R)-1-(4-chloro-2,5-difluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000003
(2R)-1-(4-chlorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.000264
(2R)-1-(4-chlorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.0000031
(2R)-1-(4-fluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.000272
(2R)-1-(4-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000011
(2R)-1-(4-iodophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.0000015
(2R)-1-(4-nitrophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.000021
(2R)-1-(5-chloro-2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000033
(2R)-1-cyclohexyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.021
(2R)-1-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-1-oxopropan-2-aminium
Homo sapiens
-
pH 2
0.00144
(2R)-4-(1,4-diazepan-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.00035
(2R)-4-(2-benzoylpyrazolidin-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.000071
(2R)-4-(2-cyclopropyl-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.00003
(2R)-4-(3-cyclopropyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000037
(2R)-4-(3-ethyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00003
(2R)-4-(3-methyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.0034
(2R)-4-(4-acetyl-1,4-diazepan-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.000387
(2R)-4-(4-benzyl-1,4-diazepan-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.0064
(2R)-4-(4-ethyl-1,4-diazepan-1-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.0001
(2R)-4-(5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.00057
(2R)-4-oxo-1-(2,4,5-trifluorophenyl)-4-[1,4,4-trimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]butan-2-amine
Rattus norvegicus
-
-
0.001018
(2R)-4-oxo-1-(pentafluorophenyl)-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000003
(2R)-4-oxo-1-phenyl-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.00004
(2R)-4-oxo-1-pyridin-2-yl-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.000045
(2R)-4-oxo-1-pyridin-3-yl-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.000051
(2R)-4-oxo-1-pyridin-4-yl-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.00000012
(2R)-4-oxo-4-(1,3-thiazolidin-3-yl)-1-(3,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.0000022
(2R)-4-oxo-4-(1,3-thiazolidin-3-yl)-1-[2-(trifluoromethyl)phenyl]butan-2-amine
Homo sapiens
-
0.0000036
(2R)-4-oxo-4-(1,3-thiazolidin-3-yl)-1-[3-(trifluoromethyl)phenyl]butan-2-amine
Homo sapiens
-
0.0000078
(2R)-4-oxo-4-(1,3-thiazolidin-3-yl)-1-[4-(trifluoromethyl)phenyl]butan-2-amine
Homo sapiens
-
0.000068
(2R)-4-oxo-4-(2-phenyl-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl)-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.000087
(2R)-4-oxo-4-(4-pyrazin-2-yl-1,4-diazepan-1-yl)-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.000423
(2R)-4-oxo-4-(4-pyrimidin-2-yl-1,4-diazepan-1-yl)-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.00385
(2R)-4-oxo-4-pyrazolidin-1-yl-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.000004
(2R)-4-oxo-4-[(8R)-2-(trifluoromethyl)-8-[4-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.00000031
(2R)-4-oxo-4-[(8R)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000005
(2R)-4-oxo-4-[(8R)-8-(1H-1,2,4-triazol-1-ylmethyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.0000057
(2R)-4-oxo-4-[(8R)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000004
(2R)-4-oxo-4-[(8R)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000032
(2R)-4-oxo-4-[(8R)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000438
(2R)-4-oxo-4-[(8S)-3-(trifluoromethyl)-8-[2-(trifluoromethyl)benzyl]-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000123
(2R)-4-oxo-4-[(8S)-8-(2,2,2-trifluoroethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000132
(2R)-4-oxo-4-[(8S)-8-(pyridin-2-ylmethyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000015
(2R)-4-oxo-4-[(8S)-8-prop-2-en-1-yl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00007
(2R)-4-oxo-4-[2-(phenylcarbonyl)-1,2-diazepan-1-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
competitive
0.00005
(2R)-4-oxo-4-[2-(phenylcarbonyl)tetrahydropyridazin-1(2H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
the inhibitor displays a greater than 1400fold selectivity over all the enzymes tested including DPP-8 and DPP-9
0.000059
(2R)-4-oxo-4-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.000805
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000151
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,3,6-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000018
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
0.000087
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,6-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00486
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[2-(trifluoromethyl)phenyl]butan-2-amine
Rattus norvegicus
-
-
0.000366
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[3-(trifluoromethyl)phenyl]butan-2-amine
Rattus norvegicus
-
-
0.000511
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-[4-(trifluoromethyl)phenyl]butan-2-amine
Rattus norvegicus
-
-
0.00051
(2R)-4-oxo-4-[4-(phenylcarbonyl)-1,4-diazepan-1-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.00041
(2R)-4-oxo-4-[4-(pyridin-3-ylcarbonyl)-1,4-diazepan-1-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.000004
(2R)-4-oxo-4-[8-(1H-pyrazol-1-ylmethyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
mixture of diastereomers at position 9
0.000019
(2R)-4-[(2R)-2-benzylpiperazin-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.00005
(2R)-4-[(4R)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00025
(2R)-4-[(4R)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00037
(2R)-4-[(4R)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000058
(2R)-4-[(4R)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.0000084
(2R)-4-[(4R)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00011
(2R)-4-[(4R)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00006
(2R)-4-[(4R)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00038
(2R)-4-[(4S)-1-methyl-4-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00049
(2R)-4-[(4S)-2-cyclopropyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00063
(2R)-4-[(4S)-2-tert-butyl-1,4-dimethyl-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00078
(2R)-4-[(4S)-4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00057
(2R)-4-[(4S)-4-benzyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00034
(2R)-4-[(4S)-4-cyclopropyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00061
(2R)-4-[(4S)-4-ethyl-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000014
(2R)-4-[(5R)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000023
(2R)-4-[(5S)-5-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000042
(2R)-4-[(6R)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000091
(2R)-4-[(6S)-6-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00000046
(2R)-4-[(8R)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000004
(2R)-4-[(8R)-8-(4-fluorobenzyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.00000018
(2R)-4-[(8R)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.00000043
(2R)-4-[(8R)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000007
(2R)-4-[(8R)-8-(cyclopropylmethyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.00000066
(2R)-4-[(8R)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000005
(2R)-4-[(8R)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000025
(2R)-4-[(8R)-8-methyl-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.0000043
(2R)-4-[(8R)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000011 - 0.000018
(2R)-4-[(8R)-8-[(1-fluorocyclopropyl)methyl]-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.0000063
(2R)-4-[(8R)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000131
(2R)-4-[(8S)-8-(2-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000116
(2R)-4-[(8S)-8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00032
(2R)-4-[(8S)-8-(4-methoxybenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00014
(2R)-4-[(8S)-8-benzyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000113
(2R)-4-[(8S)-8-ethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000274
(2R)-4-[(8S)-8-methyl-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.000088
(2R)-4-[(8S)-8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000587
(2R)-4-[(8S)-8-[3,5-bis(trifluoromethyl)benzyl]-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000045
(2R)-4-[1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.0005
(2R)-4-[2-[(4-methylphenyl)sulfonyl]pyrazolidin-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.000029
(2R)-4-[3-(difluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00049
(2R)-4-[4-(1,3-benzodioxol-5-ylcarbonyl)-1,4-diazepan-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine hydrochloride
Homo sapiens
-
0.0000058
(2R)-4-[4-(4-fluorobenzyl)-1-methyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.0031
(2R)-4-[4-(methylsulfonyl)-1,4-diazepan-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.00035
(2R)-4-[4-[(4-methylphenyl)sulfonyl]-1,4-diazepan-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.0015
(2R)-4-[4-[(4-methylpiperazin-1-yl)carbonyl]-1,4-diazepan-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.000405
(2R)-4-[4-[(4-nitrophenyl)sulfonyl]-1,4-diazepan-1-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
0.000092
(2R)-4-[5,5-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000175
(2R)-4-[8,8-dimethyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.000002
(2R)-4-[8-(1H-imidazol-1-ylmethyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
mixture of diastereomers at position 8
0.000004
(2R)-4-[8-(4-fluorobenzyl)-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.00000018
(2R)-4-[8-(4-fluorobenzyl)-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.000025
(2R)-4-[8-methyl-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.0000043
(2R)-4-[8-methyl-3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.0044
(2R,3R)-1-(2,5-difluorophenyl)-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]butan-2-amine
Homo sapiens
-
-
0.0006
(2R,3R)-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.000046
(2R,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.00011
(2R,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.0000016
(2R,3S)-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N1,N1-dimethyl-4-oxobutane-1,3-diamine
Homo sapiens
-
0.000093
(2R,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
Rattus norvegicus
-
-
0.00938
(2R,3S,11bS)-3-(3,4-dimethylphenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.00005
(2R,3S,11bS)-3-(3-chlorophenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.00513
(2R,3S,11bS)-9,10-dimethoxy-3-(3-methoxyphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.000032
(2R,3S,11bS)-9,10-dimethoxy-3-(3-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.01059
(2R,3S,11bS)-9,10-dimethoxy-3-(4-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.00027
(2R,3S,11bS)-9,10-dimethoxy-3-phenyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.00099
(2R,3S,11bS)-9,10-dimethoxy-3-pyridin-2-yl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.00007
(2R,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.000016
(2R,4R)-2-(dihydroxyboranyl)-4-hydroxypyrrolidin-1-yl (4S)-4-hydroxy-L-prolinate
Homo sapiens
-
pH 7.8, temperature not specified in the publication
0.0003
(2R,4R)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.0003 mM
0.0003
(2R,4R)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.0003 mM
0.0003
(2R,4S)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.0003 mM
0.000246
(2R,4S)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000047
(2S)-1-(3-furyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.000017
(2S)-1-(5-morpholin-4-yl-5-oxo-L-norvalyl)pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000015
(2S)-1-(5-oxo-5-piperidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000007
(2S)-1-(5-oxo-5-pyrrolidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000027
(2S)-1-([(2S,4S)-4-[(2E)-but-2-en-1-yl]pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.00000013
(2S)-1-([(2S,4S)-4-[(3-chloro-4-cyanophenyl)amino]pyrrolidin-2-yl]carbonyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.00001
(2S)-1-([(3R,4R)-4-amino-1-[4-(1,2,3-thiadiazol-4-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
0.00001
(2S)-1-([(3R,4R)-4-amino-1-[4-(1-methyl-1H-pyrazol-4-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
0.0000032
(2S)-1-([(3R,4R)-4-amino-1-[4-(1H-1,2,4-triazol-1-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
0.0000067
(2S)-1-([(3R,4R)-4-amino-1-[4-(1H-pyrazol-5-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
0.0000054
(2S)-1-([(3R,4R)-4-amino-1-[4-(2H-1,2,3-triazol-2-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
0.0000053
(2S)-1-([(3R,4R)-4-amino-1-[4-(3-methyl-1H-1,2,4-triazol-1-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
0.0000085
(2S)-1-([(3R,4R)-4-amino-1-[4-(5-methyl-1,3,4-oxadiazol-2-yl)benzyl]pyrrolidin-3-yl]carbonyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
0.000071
(2S)-1-([[2-methyl-4-oxo-4-(pyrrolidin-1-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000028
(2S)-1-cyclopentyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.003653
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-1-oxo-3-phenylpropan-2-amine
Homo sapiens
-
-
0.003257
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-1-oxohexan-2-amine
Homo sapiens
-
-
0.000356
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-3,3-dimethyl-1-oxobutan-2-amine
Homo sapiens
-
-
0.000877
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-3-(4-chlorophenyl)-1-oxopropan-2-amine
Homo sapiens
-
-
0.001065
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-3-methyl-1-oxobutan-2-amine
Homo sapiens
-
-
0.000112
(2S)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-4-methyl-3-(1-methylethyl)-1-oxopentan-2-amine
Homo sapiens
-
-
0.00000054 - 0.0014
(2S)-1-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-1-oxopropan-2-aminium
0.000298
(2S)-1-[(2S)-2-amino-4-(1,3-dihydro-2H-isoindol-2-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.00001
(2S)-1-[(2S)-2-amino-6-(1,3-dihydro-2H-isoindol-2-yl)-6-oxohexanoyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.00002
(2S)-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
0.000031
(2S)-1-[(2S,3R)-2-amino-3-ethyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]pentanoyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.0098
(2S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
-
0.000047
(2S)-1-[(4R)-4-tricyclo[3.3.1.13,7]dec-2-yl-L-prolyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.000984
(2S)-1-[(4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-5,5-dimethyl-L-prolyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000011
(2S)-1-[(4S)-4-(azocan-1-ylcarbonyl)-L-prolyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000008
(2S)-1-[([2-[(5-nitropyridin-2-yl)amino]ethyl]amino)acetyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000018
(2S)-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0187
(2S)-1-[3-([2-[(5-nitropyridin-2-yl)amino]ethyl]amino)propanoyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000031
(2S)-1-[3-methyl-5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000012
(2S)-1-[3-methyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000013
(2S)-1-[3-methyl-5-[(2R)-2-methylpyrrolidin-1-yl]-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000012
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000002
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000016
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000005
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000025
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000006
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000007
(2S)-1-[5-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.00001
(2S)-1-[5-oxo-5-(1,3-thiazolidin-3-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000019
(2S)-1-[5-oxo-5-(4-pyridin-4-ylpiperazin-1-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000006
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000009
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000008
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000005
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000008
(2S)-1-[5-oxo-5-[4-(trifluoroacetyl)piperazin-1-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000014
(2S)-1-[5-[(2R)-2-(methoxyamino)pyrrolidin-1-yl]-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000022
(2S)-1-[5-[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000007
(2S)-1-[5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.00004
(2S)-1-[5-[2-(4-fluorophenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-6-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000035
(2S)-1-[5-[6,7-dimethoxy-1-(1-methylethyl)-3,4-dihydroisoquinolin-2(1H)-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
Rattus norvegicus
-
-
0.000015
(2S)-1-[N-[3-(1,3-dihydro-2H-isoindol-2-yl)-1,1-dimethyl-3-oxopropyl]glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000015
(2S)-1-[N-[4-(1,3-dihydro-2H-isoindol-2-yl)-2-methyl-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000003
(2S)-1-[[(1R,3S,5R,7R)-tricyclo[3.3.1.13,7]dec-2-ylamino]acetyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000013
(2S)-1-[[(1R,5R)-tricyclo[3.3.1.13,7]dec-2-ylamino]acetyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000091
(2S)-1-[[(2S,4R)-4-(2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000089
(2S)-1-[[(2S,4R)-4-(2-ethyl-4-hydroxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000038
(2S)-1-[[(2S,4R)-4-(2-hydroxyethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000091
(2S)-1-[[(2S,4R)-4-(2-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000053
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,4,6-trimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.000022
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000049 - 0.0000071
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
0.0000039
(2S)-1-[[(2S,4R)-4-(3-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.000023
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethoxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000033
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2,6-dimethylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000083
(2S)-1-[[(2S,4R)-4-(4-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.000025
(2S)-1-[[(2S,4R)-4-(4-hydroxyphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.000038
(2S)-1-[[(2S,4R)-4-cyclohexylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.00006
(2S)-1-[[(2S,4R)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000017
(2S)-1-[[(2S,4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000083
(2S)-1-[[(2S,4S)-4-(azepan-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000004
(2S)-1-[[(2S,4S)-4-(azetidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000063
(2S)-1-[[(2S,4S)-4-(hydroxymethyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000043
(2S)-1-[[(2S,4S)-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000049
(2S)-1-[[(2S,4S)-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000056
(2S)-1-[[(2S,4S)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000048
(2S)-1-[[(2S,4S)-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000035 - 0.000038
(2S)-1-[[(2S,4S)-4-allylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
0.00004
(2S)-1-[[(2S,4S)-4-isobutylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.000017
(2S)-1-[[(2S,4S)-4-phenylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000034 - 0.00005
(2S)-1-[[(2S,4S)-4-propylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
0.0000056
(2S)-1-[[(2S,4S,5S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000013
(2S)-1-[[(2S,4S,5S)-4-(azetidin-1-ylcarbonyl)-5-methylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.00002
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000013
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000065
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000062
(2S)-1-[[(2S,4S,5S)-5-methyl-4-(thiomorpholin-4-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000051
(2S)-1-[[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000051
(2S)-1-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000033 - 0.0000036
(2S)-1-[[(3R,4R)-4-amino-1-(3-cyano-4-fluorobenzyl)pyrrolidin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
0.0000013
(2S)-1-[[(3R,4R)-4-amino-1-(4-cyano-3-methylbenzyl)pyrrolidin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000024
(2S)-1-[[(3R,4R)-4-amino-1-(4-cyanobenzyl)pyrrolidin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
0.0000062
(2S)-1-[[(3R,4R)-4-amino-1-(quinolin-3-ylmethyl)pyrrolidin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
0.0000000095
(2S)-2-(4-[[(1-[(3S)-3-amino-4-[2,5-difluoro-4-(trifluoromethyl)phenyl]butanoyl]-L-prolyl)amino]methyl]phenoxy)-3-methylbutanoic acid
Homo sapiens
-
0.00000000083
(2S)-2-(4-[[(1-[(3S)-3-amino-4-[2-fluoro-4-(trifluoromethyl)phenyl]butanoyl]-L-prolyl)amino]methyl]phenoxy)-3-methylbutanoic acid
Homo sapiens
-
0.0000003
(2S)-2-(4-[[(1-[(3S)-3-amino-4-[2-fluoro-5-(trifluoromethoxy)phenyl]butanoyl]-L-prolyl)amino]methyl]phenoxy)-3-methylbutanoic acid
Homo sapiens
-
0.000000012
(2S)-2-(4-[[(1-[(3S)-3-amino-4-[2-fluoro-5-(trifluoromethyl)phenyl]butanoyl]-L-prolyl)amino]methyl]phenoxy)-3-methylbutanoic acid
Homo sapiens
-
0.0000000003
(2S)-2-(4-[[([(4R)-3-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-1,3-thiazolidin-4-yl]carbonyl)amino]methyl]phenyl)-3-methylbutanoic acid
Homo sapiens
-
0.0000072
(2S)-2-[2-[([1-[(2S)-2-amino-2-cyclohexylacetyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
Homo sapiens
-
0.00000048
(2S)-2-[4-[([1-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
Homo sapiens
-
-
0.000000013
(2S)-2-[4-[([1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
Homo sapiens
-
0.00000000048
(2S)-2-[4-[([1-[(3S)-3-amino-4-(2,5-difluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
Homo sapiens
-
0.0000000017
(2S)-2-[4-[([1-[(3S)-3-amino-4-(2-chloro-4-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
Homo sapiens
-
0.0000000018
(2S)-2-[4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
Homo sapiens
-
0.000000012 - 0.000000081
(2S)-2-[4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]propanoic acid
0.0000000016
(2S)-2-[4-[([1-[(3S)-3-amino-4-(3,4-difluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
Homo sapiens
-
0.0000000016
(2S)-2-[4-[([1-[(3S)-3-amino-4-(5-chloro-2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
Homo sapiens
-
0.000000033
(2S)-2-[4-[([1-[(3S)-3-amino-4-(5-fluoro-2-methylphenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
Homo sapiens
-
0.0000000081
(2S)-2-[4-[([1-[(3S)-3-amino-4-(pentafluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
Homo sapiens
-
0.000000018
(2S)-2-[4-[([1-[(3S)-3-amino-4-phenylbutanoyl]-L-prolyl]amino)methyl]phenoxy]-3-methylbutanoic acid
Homo sapiens
-
0.00000098
(2S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxopropan-2-amine
Homo sapiens
-
0.000021
(2S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoropropan-2-aminium
Rattus norvegicus
-
-
0.0016
(2S)-5-(1,3-dihydro-2H-isoindol-2-yl)-1,5-dioxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine
Rattus norvegicus
-
-
0.00149
(2S,3R)-1-cyclopentylidene-1-fluoro-3-(3-[4-[(trifluoromethyl)sulfonyl]phenyl]-1,2,4-oxadiazol-5-yl)butan-2-aminium
Rattus norvegicus
-
-
0.00009
(2S,3R)-1-cyclopentylidene-1-fluoro-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]butan-2-aminium
Rattus norvegicus
-
-
0.001165
(2S,3R)-1-cyclopentylidene-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.000731
(2S,3R)-1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-3-methyl-1-oxopentan-2-amine
Homo sapiens
-
-
0.000057
(2S,3R)-3-(3-[2-chloro-4-[(methylsulfonyl)amino]phenyl]-1,2,4-oxadiazol-5-yl)-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.000645
(2S,3R)-3-[3-(4-bromo-2-chlorophenyl)-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.00005
(2S,3R)-3-[3-[2-chloro-4-(ethylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.0000032
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluoro-5-hydroxypentan-2-aminium
Rattus norvegicus
-
-
0.0000075
(2S,3R)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.000525
(2S,3R)-3-[3-[2-chloro-4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-cyclopentylidene-1-fluorobutan-2-aminium
Rattus norvegicus
-
-
0.0011
(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.0018
(2S,3S)-1-oxo-1-pyrrolidin-1-yl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]butan-2-amine
Homo sapiens
-
-
0.00011
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-(4-pyridin-4-ylphenyl)butan-2-amine
Homo sapiens
-
-
0.0000014
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-phenylbutan-2-amine
Homo sapiens
-
0.00000013
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[2'-(trifluoromethyl)biphenyl-4-yl]butan-2-amine
Homo sapiens
-
0.000000098
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[3'-(1H-1,2,4-triazol-3-yl)biphenyl-4-yl]butan-2-amine
Homo sapiens
-
0.00000014
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[3'-(1H-tetrazol-1-yl)biphenyl-4-yl]butan-2-amine
Homo sapiens
-
0.000000006
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[3'-(1H-tetrazol-5-yl)biphenyl-4-yl]butan-2-amine
Homo sapiens
-
0.00000051
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4'-(trifluoromethyl)biphenyl-4-yl]butan-2-amine
Homo sapiens
-
0.0000006
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4-(trifluoromethyl)phenyl]butan-2-amine
Homo sapiens
-
0.00044 - 0.00347
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
0.00000011
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(2'-methoxybiphenyl-4-yl)-1-oxobutan-2-amine
Homo sapiens
-
0.00000015
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(2'-methylbiphenyl-4-yl)-1-oxobutan-2-amine
Homo sapiens
-
0.00000013
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4'-methoxybiphenyl-4-yl)-1-oxobutan-2-amine
Homo sapiens
-
0.00000039
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4'-methylbiphenyl-4-yl)-1-oxobutan-2-amine
Homo sapiens
-
0.00000078
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-methoxyphenyl)-1-oxobutan-2-amine
Homo sapiens
-
0.000027 - 0.000097
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl](methyl)amino]cyclohexyl)-1-oxobutan-2-aminium
0.000074 - 0.00021
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl]amino]cyclohexyl)-1-oxobutan-2-aminium
0.000000069
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[3'-(1,3,4-oxadiazol-2-yl)biphenyl-4-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.00000011
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[3'-(methylsulfonyl)biphenyl-4-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.00000042
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4'-(methylsulfonyl)biphenyl-4-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.00000036
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4-(methylthio)phenyl]-1-oxobutan-2-amine
Homo sapiens
-
0.000054
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-[4-fluoro-2-(trifluoromethyl)phenyl]-1-oxobutan-2-amine
Homo sapiens
-
0.00053
(2S,3S)-2-amino-1-((1S,5S)-2-azabicyclo[3.1.0]hexan-2-yl)-3-methylpentan-1-one
Homo sapiens
-
-
0.000000037
(2S,3S)-3-(2',4'-difluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.00000015
(2S,3S)-3-(2',5'-difluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.000000085
(2S,3S)-3-(2'-chlorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.0000001
(2S,3S)-3-(2'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.0000042
(2S,3S)-3-(2,4-difluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.000002
(2S,3S)-3-(2-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.0000011
(2S,3S)-3-(2-fluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.00000006
(2S,3S)-3-(3',4'-difluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.00000024
(2S,3S)-3-(3',5'-difluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.0000011
(2S,3S)-3-(3,4-difluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.0000037
(2S,3S)-3-(3,5-difluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.0000028
(2S,3S)-3-(3-chloro-4-fluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.0000011
(2S,3S)-3-(3-chlorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.0000037
(2S,3S)-3-(3-fluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.0000000091
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-4-pyrrolidin-1-ylbutan-2-amine
Homo sapiens
-
0.0000035
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-5-pyrrolidin-1-ylpentan-2-amine
Homo sapiens
-
0.000000065 - 0.000064
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
0.000064
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Homo sapiens
-
0.00000025 - 0.000245
(2S,3S)-3-(4-bromophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
0.00000048
(2S,3S)-3-(4-chloro-2-fluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.00000028
(2S,3S)-3-(4-fluorophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.00046 - 0.00149
(2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.00033 - 0.00051
(2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.00016 - 0.0003
(2S,3S)-3-(4-[[(4-fluorophenyl)carbonyl](methyl)amino]phenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.000000013
(2S,3S)-3-amino-2-(2',4'-difluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
Homo sapiens
-
0.000000056
(2S,3S)-3-amino-2-(2',5'-difluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
Homo sapiens
-
0.000000021
(2S,3S)-3-amino-2-(3',4'-difluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
Homo sapiens
-
0.000000043
(2S,3S)-3-amino-2-(3'-ethynylbiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
Homo sapiens
-
0.00000003
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3R)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
Homo sapiens
-
0.00000039
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutan-1-ol
Homo sapiens
-
0.00000011
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanamide
Homo sapiens
-
0.0000000066
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanoic acid
Homo sapiens
-
0.000000068
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N',N'-dimethyl-4-oxobutanehydrazide
Homo sapiens
-
0.000000012
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxobutanamide
Homo sapiens
-
0.0000001
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N-(1-methylethyl)-4-oxobutanamide
Homo sapiens
-
0.000000093
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N-(2-hydroxyethyl)-4-oxobutanamide
Homo sapiens
-
0.000000045
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N-methoxy-N-methyl-4-oxobutanamide
Homo sapiens
-
0.000000037
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N-methyl-4-oxobutanamide
Homo sapiens
-
0.00000052
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-morpholin-4-yl-4-oxobutanamide
Homo sapiens
-
0.0000000091
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxo-4-(1,3-thiazolidin-3-yl)butanamide
Homo sapiens
-
0.00000055
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxo-4-piperidin-1-ylbutanamide
Homo sapiens
-
0.0000000074
(2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxo-4-pyrrolidin-1-ylbutanamide
Homo sapiens
-
0.00000023
(2S,3S)-3-amino-4-(1,1-dioxido-1,3-thiazolidin-3-yl)-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxobutanamide
Homo sapiens
-
0.000000029
(2S,3S)-3-amino-4-(3,3-difluoroazetidin-1-yl)-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxobutanamide
Homo sapiens
-
0.000000027
(2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxobutanamide
Homo sapiens
-
0.0000088
(2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]pyridin-6-ylphenyl)butanamide
Homo sapiens
-
-
0.0000048
(2S,3S)-3-amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(trans-4-[1,2,4]triazolo[1,5-a]pyridin-6-ylcyclohexyl)butanamide
Homo sapiens
-
-
0.000000017
(2S,3S)-3-amino-4-(3-fluoroazetidin-1-yl)-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxobutanamide
Homo sapiens
-
0.0000001
(2S,3S)-3-amino-4-aziridin-1-yl-2-(4'-fluorobiphenyl-4-yl)-N,N-dimethyl-4-oxobutanamide
Homo sapiens
-
0.000000021
(2S,3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-2-[3'-(methylsulfonyl)biphenyl-4-yl]-4-oxobutanamide
Homo sapiens
-
0.000000019
(2S,3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-(4-pyridin-3-ylphenyl)butanamide
Homo sapiens
-
0.00000002
(2S,3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-(4-pyridin-4-ylphenyl)butanamide
Homo sapiens
-
0.0000000022
(2S,3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-N,N-dimethyl-4-oxo-2-[3'-(2H-tetrazol-2-yl)biphenyl-4-yl]butanamide
Homo sapiens
-
0.000000059
(2S,3S)-3-amino-N,N-diethyl-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanamide
Homo sapiens
-
0.000000011
(2S,3S)-3-amino-N-(3,4-dihydro-2H-tetrazol-2-yl)-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanamide
Homo sapiens
-
0.000000071
(2S,3S)-3-amino-N-cyclopropyl-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanamide
Homo sapiens
-
0.00000011
(2S,3S)-3-amino-N-ethyl-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanamide
Homo sapiens
-
0.00000002
(2S,3S)-3-amino-N-ethyl-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-N-methyl-4-oxobutanamide
Homo sapiens
-
0.00000012
(2S,3S)-3-biphenyl-4-yl-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.00000014
(2S,3S)-3-[3'-(5-cyclopropyl-2,3-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.000203
(2S,3S)-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
Rattus norvegicus
-
-
0.000615
(2S,3S)-3-[3-(2,4-dichlorophenyl)-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
-
0.000017
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
Rattus norvegicus
-
-
0.00004
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
-
0.00004
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Rattus norvegicus
-
-
0.00007
(2S,3S)-3-[3-[2-chloro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-5-hydroxy-1-oxopentan-2-aminium
Rattus norvegicus
-
-
0.000122
(2S,3S)-3-[3-[4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-oxo-1-pyrrolidin-1-ylbutan-2-aminium
Rattus norvegicus
-
-
0.000071
(2S,3S)-3-[4-(3-chloropyridin-4-yl)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
-
0.0006
(2S,3S)-3-[4-(acetylamino)phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Homo sapiens
-
0.000022 - 0.000047
(2S,3S)-3-[4-[(cyclopropylcarbonyl)(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.000016 - 0.00004
(2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
0.000029 - 0.00019
(2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.00021
(2S,3S)-3-[4-[acetyl(methyl)amino]phenyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Homo sapiens
-
0.00015
(2S,3S)-3-[4-[acetyl(methyl)amino]phenyl]-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
Homo sapiens
-
0.00036 - 0.00128
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
0.00087
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-3-[4-[(phenylsulfonyl)amino]phenyl]butan-2-aminium
Homo sapiens
-
0.000025
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[methyl[(4-methylphenyl)carbonyl]amino]phenyl)-1,4-dioxobutan-2-aminium
Homo sapiens
-
0.00043
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[methyl[(4-methylphenyl)sulfonyl]amino]phenyl)-1,4-dioxobutan-2-aminium
Homo sapiens
-
0.000012
(2S,3S)-4-(dimethylamino)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
Homo sapiens
-
0.000022 - 0.0002
(2S,3S)-4-(dimethylamino)-3-(4-[[(3-fluorophenyl)carbonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
0.000028
(2S,3S)-4-(dimethylamino)-3-(4-[[(4-fluorophenyl)carbonyl](methyl)amino]phenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
Homo sapiens
-
0.000000044
(2S,3S)-4-azetidin-1-yl-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-amine
Homo sapiens
-
0.000019
(2S,3S)-4-cyclopropyl-3-[3-[2-fluoro-4-(methylsulfonyl)phenyl]-1,2,4-oxadiazol-5-yl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Rattus norvegicus
-
-
0.0000046
(2S,3S)-9,10-dimethoxy-3-(3-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.000142
(2S,3S,11bS)-3-(1,1-dioxido-1,2-thiazinan-2-yl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Rattus norvegicus
-
-
0.0000017
(2S,3S,11bS)-3-(2,5-dimethylphenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.00373
(2S,3S,11bS)-3-(3,4-dimethylphenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.000004 - 0.0000042
(2S,3S,11bS)-3-(3-chlorophenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
0.000038
(2S,3S,11bS)-3-(3-cyclopropylphenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.000061
(2S,3S,11bS)-3-(3-ethylphenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.00052
(2S,3S,11bS)-3-butyl-9,10-dimethoxy-1,2,3,4,6,7-hexahydro-11bH-pyrido[2,1-a]isoquinoline-2,11b-diamine
Homo sapiens
-
pH 8.0, 37°C
0.0000005
(2S,3S,11bS)-3-[3-(fluoromethyl)phenyl]-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.0000012
(2S,3S,11bS)-3-[4-(fluoromethyl)pyridin-2-yl]-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.00065
(2S,3S,11bS)-9,10-dimethoxy-3-(3-methoxyphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.000004 - 0.0000046
(2S,3S,11bS)-9,10-dimethoxy-3-(3-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
0.00037
(2S,3S,11bS)-9,10-dimethoxy-3-(4-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.000019
(2S,3S,11bS)-9,10-dimethoxy-3-(4-methylpyridin-2-yl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.0002
(2S,3S,11bS)-9,10-dimethoxy-3-phenyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.00152
(2S,3S,11bS)-9,10-dimethoxy-3-pyridin-2-yl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.0055
(2S,3S,11bS)-9,10-dimethoxy-3-[3-(propan-2-yl)phenyl]-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.000016
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-ethyl-N,N-dimethylpyrrolidine-3-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.00001
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
0.000015
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N,2-dimethylpyrrolidine-3-carboxamide
Homo sapiens
-
-
0.000042
(2S,4R)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000006
(2S,4R)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000006
(2S,4S)-1-((2S)-2-amino-3-methylpentanoyl)-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000041
(2S,4S)-1-(N-1-adamantylglycyl)-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000031
(2S,4S)-1-(N-2-adamantylglycyl)-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000031
(2S,4S)-1-(N-cyclobutylglycyl)-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000033
(2S,4S)-1-(N-cyclooctylglycyl)-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000026
(2S,4S)-1-(N-cyclopentylglycyl)-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000033
(2S,4S)-1-(N-cyclopropylglycyl)-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000027
(2S,4S)-1-(N-[2-[(5-chloropyridin-2-yl)amino]ethyl]-glycyl)-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000021
(2S,4S)-1-(O-benzyl-L-threonyl)-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000012
(2S,4S)-1-L-alloisoleucyl-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000011
(2S,4S)-1-[(2S)-2-amino-2-cyclohexylacetyl]-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000015
(2S,4S)-1-[2-(1,1-dimethyl-3-oxo-3-pyrrolidin-1-yl-propylamino)acetyl]-4-fluoro-pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000029
(2S,4S)-1-[N-(tert-butyl)glycyl]-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000016
(2S,4S)-1-[N-[(2E)-1,1-dimethyl-3-phenylprop-2-en-1-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000088
(2S,4S)-1-[N-[1-(1-benzofuran-2-yl)-1-methylethyl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000027
(2S,4S)-1-[N-[2-(3,4-dimethoxyphenyl)ethyl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000252
(2S,4S)-1-[N-[2-(diethylamino)-1,1-dimethylethyl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000018
(2S,4S)-1-[N-[4-(3,6-dihydropyridin-1(2H)-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000066
(2S,4S)-1-[N-[4-(7-azabicyclo[2.2.1]hept-7-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.00016
(2S,4S)-1-[N-[4-(azepan-1-yl)-2-methyl-4-oxobutan-2-yl]glycyl]-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000049
(2S,4S)-1-[O-(tert-butyl)-L-threonyl]-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000025
(2S,4S)-1-[[(3S)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]-4-fluoropyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0003
(2S,4S)-4-fluoro-1-(3-methyl-D-valyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.0003 mM
0.0000006
(2S,4S)-4-fluoro-1-(3-methyl-L-valyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000078
(2S,4S)-4-fluoro-1-(N-isopropylglycyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0001
(2S,4S)-4-fluoro-1-(N-methyl-L-isoleucyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.0001 mM
0.000032
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[(2R)-2-methylpyrrolidin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000024
(2S,4S)-4-fluoro-1-(N-[2-methyl-4-[4-(methylsulfonyl)piperazin-1-yl]-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000039
(2S,4S)-4-fluoro-1-(N-[2-[(4-cyanobenzyl)amino]-1,1-dimethylethyl]glycyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000011
(2S,4S)-4-fluoro-1-(N-[2-[(5-cyanopyridin-2-yl)-amino]ethyl]glycyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000024
(2S,4S)-4-fluoro-1-(N-[4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]glycyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000047
(2S,4S)-4-fluoro-1-(O-methyl-L-threonyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000027
(2S,4S)-4-fluoro-1-([[2-methyl-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-yl]amino]acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000007
(2S,4S)-4-fluoro-1-L-valyl-pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000008
(2S,4S)-4-fluoro-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000022
(2S,4S)-4-fluoro-1-[(3S)-1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000039
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-fluoropyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.00003
(2S,4S)-4-fluoro-1-[([4-[(3R)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.00005
(2S,4S)-4-fluoro-1-[([4-[(3S)-3-hydroxypyrrolidin-1-yl]-2-methyl-4-oxobutan-2-yl]amino)acetyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000022
(2S,4S)-4-fluoro-1-[N-(1-methyl-1-pyridin-2-ylethyl)glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000046
(2S,4S)-4-fluoro-1-[N-(2-hydroxy-1,1-dimethylethyl)glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
potent and long-acting DPP-IV inhibitor and effective with single daily dosing
0.000013
(2S,4S)-4-fluoro-1-[N-(2-methoxy-1,1-dimethylethyl)glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000031
(2S,4S)-4-fluoro-1-[N-(3-hydroxy-1-adamantyl)-glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000087
(2S,4S)-4-fluoro-1-[N-(3-isopropoxypropyl)glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000083
(2S,4S)-4-fluoro-1-[N-(3-methoxy-1-adamantyl)-glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000053
(2S,4S)-4-fluoro-1-[N-(5-hydroxy-2-adamantyl)-glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000086
(2S,4S)-4-fluoro-1-[N-[1-(2-furyl)-1-methylethyl]-glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000033
(2S,4S)-4-fluoro-1-[N-[1-(hydroxymethyl)cyclopentyl]glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000012
(2S,4S)-4-fluoro-1-[N-[1-methyl-1-(2-thienyl)-ethyl]glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000028
(2S,4S)-4-fluoro-1-[N-[2-(pyridin-2-ylamino)ethyl]-glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000093
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(4-methylpiperazin-1-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.00002
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-(morpholin-4-yl)-4-oxobutan-2-yl]glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000026
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(4-oxopiperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000027
(2S,4S)-4-fluoro-1-[N-[2-methyl-4-oxo-4-(piperidin-1-yl)butan-2-yl]glycyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000012
(2S,4S)-4-fluoro-1-[[(3S)-7-hydroxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.0000017
(2S,4S)-4-fluoro-1-[[(3S)-7-methoxy-1,2,3,4-tetrahydroisoquinolin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000011
(2S,4S,5S)-N-(cyanomethyl)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-N-ethyl-5-methylpyrrolidine-2-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.00006
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-prop-2-yn-1-ylpyrrolidine-2-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.0006
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methyl-N-propylpyrrolidine-2-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.013
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.000025
(2S,4S,5S)-N-(cyanomethyl)-4-isobutyryl-N,5-dimethylpyrrolidine-2-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.000056
(2S,4S,5S)-N-(cyanomethyl)-N-cyclopropyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.000024
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.000024
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(morpholin-4-ylcarbonyl)pyrrolidine-2-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.000017
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(piperidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.000016
(2S,4S,5S)-N-(cyanomethyl)-N-ethyl-5-methyl-4-(pyrrolidin-1-ylcarbonyl)pyrrolidine-2-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.000041
(2S,4S,5S)-N-allyl-N-(cyanomethyl)-4-isobutyryl-5-methylpyrrolidine-2-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.000051
(2S,4S,5S)-N4-benzyl-N2-(cyanomethyl)-N2-ethyl-5-methylpyrrolidine-2,4-dicarboxamide
Homo sapiens
-
37°C, pH 7.4
0.000121 - 0.000127
(3'S,5'S)-5'-(1,3-thiazolidin-3-ylcarbonyl)-1,3'-bipyrrolidine
0.000338
(3,3-difluoro-pyrrolidin-1-yl)-[(2S,4R)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin)-2-yl]-methanone
Homo sapiens
-
0.0000129
(3,3-difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl)-piperazin-1-yl)-pyrrolidin-2-yl]-methanone
Homo sapiens
-
0.000032
(3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]phenyl)methanol
Homo sapiens
-
-
0.0000042 - 0.0000053
(3R)-1-[(1R)-1-(dihydroxyboranyl)ethyl]-2-oxopyrrolidin-3-aminium
0.000046
(3R)-3-amino-1-diaminophosphinyl-2-piperidinone
Rattus norvegicus
-
IC50: 46 nM
0.0000061
(3R)-3-amino-1-[(2S)-2-([[2-(trifluoromethyl)pyrimidin-4-yl]oxy]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
Homo sapiens
-
-
0.0000039
(3R)-3-amino-1-[(2S)-2-([[4-(trifluoromethyl)pyrimidin-2-yl]amino]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
Homo sapiens
-
-
0.000015
(3R)-3-amino-1-[(2S)-2-([[6-(trifluoromethyl)pyridin-3-yl]amino]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
Homo sapiens
-
-
0.00001
(3R)-3-amino-1-[(2S)-2-[(cyclopropylmethoxy)methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
Homo sapiens
-
-
0.0000054
(3R)-3-amino-1-[(2S)-2-[(pyrimidin-2-ylamino)methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
Homo sapiens
-
-
0.0000063
(3R)-3-amino-1-[(2S)-2-[[(5-fluoropyridin-2-yl)amino]methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
Homo sapiens
-
-
0.0000071
(3R)-3-amino-1-[(2S)-2-[[(5-fluoropyrimidin-2-yl)amino]methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
Homo sapiens
-
-
0.00003
(3R)-3-amino-1-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
Homo sapiens
-
-
0.000055
(3R)-3-amino-4-(2,5-difluorophenyl)-1-(3-methyl-1,2,4-oxadiazol-5-yl)butan-1-one
Homo sapiens
-
-
0.0000066
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,3-dimethyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000151
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-(2-hydroxyethyl)-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.000008
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-cyclopropyl-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000096
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-tert-butyl-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000105
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1-[2-(benzyloxy)ethyl]-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000026
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000066
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000192
(3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
Homo sapiens
-
-
0.000009
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-1-cyclopropyl-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000207
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-1-ethyl-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000115
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000116
(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-1-(2-oxopropyl)-1,4-diazepan-2-one
Homo sapiens
-
-
0.000085
(3R)-4-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
Homo sapiens
-
-
0.00004
(3R)-4-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.00012
(3R)-4-[(3S)-3-amino-4-(2-oxopiperidin-1-yl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
Homo sapiens
-
-
0.00002
(3R)-4-[(3S)-3-amino-4-(2-oxopiperidin-1-yl)butanoyl]-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.000062
(3R,4R)-1-(1,3-benzothiazol-2-ylcarbonyl)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.000042
(3R,4R)-1-(1,3-benzothiazol-6-ylcarbonyl)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.000005
(3R,4R)-1-(2-methyl-3-oxo-2,3-dihydro[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000007
(3R,4R)-1-(2-methyl-4-oxo-3,4-dihydropyrido[3,2-d]pyrimidin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000008
(3R,4R)-1-(2-methyl-4-oxo-4H-pyrimido[1,2-b]pyridazin-7-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
pharmacokinetic properties
0.000079
(3R,4R)-1-(2-naphthoyl)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.0000012 - 0.000002
(3R,4R)-1-(2-oxo-2H-pyrimido[1,2-b]pyridazin-7-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
0.00008
(3R,4R)-1-(3,4-difluorobenzyl)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.000006
(3R,4R)-1-(3-ethyl[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000006
(3R,4R)-1-(3-methyl[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-amine
Homo sapiens
-
-
0.000006
(3R,4R)-1-(3-methyl[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
pharmacokinetic properties
0.000014
(3R,4R)-1-(4-cyanopyridin-2-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000008
(3R,4R)-1-(4-cyclopropylpyrido[3,2-d]pyrimidin-6-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000047
(3R,4R)-1-(isoquinolin-3-ylcarbonyl)-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.0037
(3R,4R)-1-isoquinolin-1-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.00021
(3R,4R)-1-phenyl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000043
(3R,4R)-1-pteridin-7-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000013
(3R,4R)-1-pyrazino[2,3-b]pyrazin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000058
(3R,4R)-1-pyridin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000144
(3R,4R)-1-pyridin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000125
(3R,4R)-1-pyridin-4-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.00013
(3R,4R)-1-pyrido[2,3-b]pyrazin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000007
(3R,4R)-1-pyrido[2,3-b]pyrazin-6-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000054
(3R,4R)-1-quinolin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000012
(3R,4R)-1-quinoxalin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000086
(3R,4R)-1-[(5-chloro-1-benzofuran-2-yl)carbonyl]-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.000026
(3R,4R)-1-[1,2,4]triazolo[4,3-a]pyrimidin-7-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
pharmacokinetic properties
0.000031
(3R,4R)-1-[1,2,4]triazolo[4,3-b]pyridazin-6-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000083
(3R,4R)-1-[1-methyl-1-(4-nitrophenyl)ethyl]-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.000022
(3R,4R)-1-[2-(trifluoromethyl)imidazo[1,2-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000005
(3R,4R)-1-[2-(trifluoromethyl)[1,2,4]triazolo[1,5-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000016
(3R,4R)-1-[3-(4-fluorophenyl)[1,2,4]triazolo[4,3-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000111
(3R,4R)-1-[3-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000009
(3R,4R)-1-[3-(trifluoromethyl)[1,2,4]triazolo[4,3-b]pyridazin-6-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000067
(3R,4R)-1-[4-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000463
(3R,4R)-1-[5-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.00065
(3R,4R)-1-[6-(trifluoromethyl)pyridin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.0184
(3R,4R)-3-butyl-1-(3,4,5-trimethoxyphenyl)piperidin-4-amine
Homo sapiens
-
-
0.026
(3R,4R)-3-butyl-1-(3,4-dimethoxyphenyl)piperidin-4-amine
Homo sapiens
-
-
0.0134
(3R,4R)-3-butyl-1-(4-methylphenyl)piperidin-4-amine
Homo sapiens
-
-
0.0052
(3R,4R)-3-butyl-1-(4-phenoxyphenyl)piperidin-4-amine
Homo sapiens
-
-
0.142
(3R,4R)-3-butyl-1-(6-methoxybiphenyl-3-yl)piperidin-4-amine
Homo sapiens
-
-
0.0094
(3R,4R)-3-butyl-1-naphthalen-2-ylpiperidin-4-amine
Homo sapiens
-
-
0.0063
(3R,4R)-3-butyl-1-phenylpiperidin-4-amine
Homo sapiens
-
-
0.00049
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-(quinolin-3-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.000027
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-(quinolin-3-ylmethyl)pyrrolidin-3-amine
Homo sapiens
-
0.000038
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-(quinolin-6-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.000091
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-[4-(1,2,3-thiadiazol-4-yl)benzyl]pyrrolidin-3-amine
Homo sapiens
-
0.00004
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-[4-(1H-1,2,4-triazol-1-yl)benzoyl]pyrrolidin-3-amine
Homo sapiens
-
0.000069
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-[4-(1H-1,2,4-triazol-1-yl)benzyl]pyrrolidin-3-amine
Homo sapiens
-
0.00003
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-[4-(1H-tetrazol-1-yl)benzoyl]pyrrolidin-3-amine
Homo sapiens
-
0.00005
(3R,4R)-4-(pyrrolidin-1-ylcarbonyl)-1-[4-(1H-tetrazol-1-yl)benzyl]pyrrolidin-3-amine
Homo sapiens
-
0.00002 - 0.000021
(3R,4S)-1-(6-phenylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
0.000031
(3R,4S)-1-(6-pyridin-3-ylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.0027
(3R,4S)-1-acetyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine
Homo sapiens
-
0.0034
(3R,4S)-1-benzyl-4-(2,4-dichlorophenyl)pyrrolidin-3-amine
Homo sapiens
-
0.0000021
(3R,4S)-1-[4-[3-(methylsulfonyl)phenyl]-1,3,5-triazin-2-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
0.000261
(3R,4S)-1-[6-(2-chlorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.000057
(3R,4S)-1-[6-(2-fluorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.00018
(3R,4S)-1-[6-(2-methoxyphenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.00019
(3R,4S)-1-[6-(3-chlorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.0029
(3R,4S)-1-[6-(3-chlorophenyl)pyrimidin-4-yl]-4-phenylpyrrolidin-3-amine
Homo sapiens
-
-
0.000051
(3R,4S)-1-[6-(3-fluorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.000047
(3R,4S)-1-[6-(3-methoxyphenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.000014 - 0.00012
(3R,4S)-1-[6-(3-nitrophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
0.000006 - 0.000017
(3R,4S)-1-[6-(3-thienyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
0.00047
(3R,4S)-1-[6-(4-chlorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.000051
(3R,4S)-1-[6-(4-fluorophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.00012
(3R,4S)-1-[6-(4-methoxyphenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.0023
(3R,4S)-1-[6-(4-methoxyphenyl)pyrimidin-4-yl]-4-phenylpyrrolidin-3-amine
Homo sapiens
-
-
0.000037
(3R,4S)-1-[6-(6-methoxypyridin-3-yl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.0000035
(3R,4S)-1-[6-[3-(methylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
0.0000017
(3R,4S)-1-[6-[3-(morpholin-4-ylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
0.0013
(3R,4S)-1-[6-[3-(trifluoromethoxy)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.000071
(3R,4S)-1-[6-[3-(trifluoromethyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.000009
(3R,4S)-1-[6-[3-fluoro-5-(methylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
0.00019
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-(3-fluorobenzyl)pyrrolidine-1-carboxamide
Homo sapiens
-
0.00022
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-(3-methoxybenzyl)-N-methylpyrrolidine-1-carboxamide
Homo sapiens
-
0.00061
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-ethyl-N-methylpyrrolidine-1-carboxamide
Homo sapiens
-
0.00028
(3R,4S)-3-amino-4-(2,4-dichlorophenyl)-N-ethylpyrrolidine-1-carboxamide
Homo sapiens
-
0.00014
(3R,4S)-4-(2,4-dichlorophenyl)-1-(6-phenylpyridin-2-yl)pyrrolidin-3-amine
Homo sapiens
-
0.0028
(3R,4S)-4-(2,4-dichlorophenyl)-1-phenylpyrrolidin-3-amine
Homo sapiens
-
0.00079
(3R,4S)-4-(2,4-dichlorophenyl)-1-pyridin-2-ylpyrrolidin-3-amine
Homo sapiens
-
0.00021
(3R,4S)-4-(2,4-dichlorophenyl)-1-pyrimidin-2-ylpyrrolidin-3-amine
Homo sapiens
-
0.013
(3R,4S)-4-(2,4-dichlorophenyl)-1-[(4-methylphenyl)sulfonyl]pyrrolidin-3-amine
Homo sapiens
-
0.002
(3R,4S)-4-(2,4-dichlorophenyl)-1-[2-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
Homo sapiens
-
0.000076
(3R,4S)-4-(2,4-dichlorophenyl)-1-[4-(3-thienyl)pyrimidin-2-yl]pyrrolidin-3-amine
Homo sapiens
-
0.00043
(3R,4S)-4-(2,4-dichlorophenyl)-1-[5-(4-methoxyphenyl)pyrimidin-2-yl]pyrrolidin-3-amine
Homo sapiens
-
0.000015
(3R,4S)-4-(2,4-dichlorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
Homo sapiens
-
0.000035
(3R,4S)-4-(2-chloro-4,5-difluorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
Homo sapiens
-
0.000034
(3R,4S)-4-(2-chloro-4-fluorophenyl)-1-[6-(3-thienyl)pyrimidin-4-yl]pyrrolidin-3-amine
Homo sapiens
-
0.00079
(3R,4S)-4-phenyl-1-(6-phenylpyrimidin-4-yl)pyrrolidin-3-amine
Homo sapiens
-
-
0.0000097
(3R,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6-dimethyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.000139
(3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-7-(trifluoromethyl)-1,4-diazepan-2-one
Homo sapiens
-
-
0.000126
(3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-(2-fluorobenzyl)-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.000296
(3R,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-ethyl-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.000765 - 0.00105
(3R,S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-methyl-1,4-diazepan-2-one
Homo sapiens
-
absolute configuration of 3-methyl group not determined
0.000017
(3S)-1-oxo-5-phenyl-1-(1,3-thiazolidin-3-yl)pentan-3-amine
Homo sapiens
-
0.00046 - 0.00048
(3S)-1-[(1R)-1-(dihydroxyboranyl)ethyl]-2-oxopyrrolidin-3-aminium
0.00013
(3S)-3-amino-1-diaminophosphinyl-2-perhydroazepinone
Rattus norvegicus
-
IC50: 130 nM
0.000094
(3S)-3-amino-1-diaminophosphinyl-2-piperidinone
Rattus norvegicus
-
IC50: 94 nM
0.000011
(3S)-3-amino-1-diaminophosphinyl-2-pyrrolidinone
Rattus norvegicus
-
IC50: 11 nM
0.0088
(3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-1-(3-methyl-1,2,4-oxadiazol-5-yl)-4-oxobutan-1-one
Homo sapiens
-
-
0.000142
(3S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6,6-trimethyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000036
(3S)-N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-fluoro-3-methylbutanamide
Rattus norvegicus
-
-
0.0023
(3S,4R)-3-butyl-1-(3,4,5-trimethoxyphenyl)piperidin-4-amine
Homo sapiens
-
-
0.0033
(3S,4R)-3-butyl-1-(3,4-dichlorophenyl)piperidin-4-amine
Homo sapiens
-
-
0.0049
(3S,4R)-3-butyl-1-(3,4-dimethoxyphenyl)piperidin-4-amine
Homo sapiens
-
-
0.0947
(3S,4R)-3-butyl-1-(4-methylphenyl)piperidin-4-amine
Homo sapiens
-
-
0.015
(3S,4R)-3-butyl-1-(4-phenoxyphenyl)piperidin-4-amine
Homo sapiens
-
-
0.0058
(3S,4R)-3-butyl-1-(6-methoxybiphenyl-3-yl)piperidin-4-amine
Homo sapiens
-
-
0.0357
(3S,4R)-3-butyl-1-(diphenylmethyl)piperidin-4-amine
Homo sapiens
-
-
0.0186 - 0.0452
(3S,4R)-3-butyl-1-cyclohexylpiperidin-4-amine
0.0015
(3S,4R)-3-butyl-1-naphthalen-2-ylpiperidin-4-amine
Homo sapiens
-
-
0.0021
(3S,4R)-3-butyl-1-[3-methoxy-5-(trifluoromethyl)phenyl]piperidin-4-amine
Homo sapiens
-
-
0.0028
(3S,4R)-3-butyl-1-[4-chloro-3-(trifluoromethyl)phenyl]piperidin-4-amine
Homo sapiens
-
-
0.000082
(3S,4S)-1-pyrazin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000063
(3S,4S)-1-pyridazin-3-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.00009
(3S,4S)-1-pyrimidin-2-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000037
(3S,4S)-1-pyrimidin-4-yl-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.000004
(3S,4S)-5-(dimethylamino)-2-[(3S)-3-fluoropyrrolidin-1-yl]-5-oxo-4-(4-[1,2,4]triazolo[1,5-a]pyridin-6-ylphenyl)pent-1-en-3-aminium
Homo sapiens
-
0.000006
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-diethylpyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000018
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N-dimethylpyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000049
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethyl-N-methylpyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000044
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-ethylpyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000035
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-methylpyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000057
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N-propylpyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000077
(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.002587
(3S,5S)-N-(2-phenylethyl)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.0000551
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.0000549
(3S,5S)-N-(4-methoxyphenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.000021
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.000171
(3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.001957
(3S,5S)-N-benzyl-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.00019
(3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.00413
(3S,5S)-N-phenyl-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide
Homo sapiens
-
-
0.000033
(3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6-dimethyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000603
(3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-ethyl-6-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.000143
(3S,6R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-6-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000097
(3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,6-dimethyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000373
(3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-ethyl-6-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000246
(3S,6S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-6-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000151
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,7-dimethyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000277
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2-fluorobenzyl)-7-methyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000343
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one
Homo sapiens
-
-
0.00000149
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(2-methylbenzyl)-1,4-diazepan-2-one
Homo sapiens
-
-
0.000011
(3S,7R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-7-methyl-3-(pyridin-2-ylmethyl)-1,4-diazepan-2-one
Homo sapiens
-
-
0.000397
(3S,7S)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3,7-dimethyl-1,4-diazepan-2-one
Homo sapiens
-
-
0.0000016 - 0.0000022
(4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]phenyl)ethynamine
0.000000037
(4-[[([(4R)-3-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-1,3-thiazolidin-4-yl]carbonyl)amino]methyl]phenyl)acetic acid
Homo sapiens
-
0.00000016
(4-[[([(4R)-3-[(3R)-3-amino-4-phenylbutanoyl]-1,3-thiazolidin-4-yl]carbonyl)amino]methyl]phenyl)acetic acid
Homo sapiens
-
0.000638
(4R)-3-([1-[1-(2-phenoxyethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.00071
(4R)-3-([1-[1-(4-cyanobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.002228
(4R)-3-([1-[1-(4-fluorobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.000698
(4R)-3-([1-[1-(4-nitrobenzyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001459
(4R)-3-([1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.004767
(4R)-3-([1-[1-(pyridin-3-ylmethyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.003755
(4R)-3-([2-ethyl-1-[1-(methylsulfonyl)piperidin-4-yl]hydrazinyl]acetyl)-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001022
(4R)-3-[(1-[1-[(2'-cyanobiphenyl-4-yl)methyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001449
(4R)-3-[(1-[1-[(4-chlorophenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.006677
(4R)-3-[(1-[1-[(4-methoxyphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.002701
(4R)-3-[(1-[1-[(4-methylphenyl)sulfonyl]piperidin-4-yl]hydrazinyl)acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.001631
(4R)-3-[[1-(1-benzylpiperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.00176
(4R)-3-[[1-(1-[3-[2-(aminooxy)cyclopropyl]propyl]piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.012
(4R)-3-[[1-(piperidin-4-yl)hydrazinyl]acetyl]-1,3-thiazolidine-4-carbonitrile
Rattus norvegicus
-
-
0.000037
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxo-N-phenylpentanamide
Rattus norvegicus
-
-
0.000011
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-N-cyclopentyl-5-oxopentanamide
Rattus norvegicus
-
-
0.00024
(6-methylpyridin-2-yl)methyl (3R,4S)-3-amino-4-(2,4-dichlorophenyl)pyrrolidine-1-carboxylate
Homo sapiens
-
0.0014
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid
Homo sapiens
-
0.0037
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid (1H-benzoimidazol-2-ylmethyl)amide
Homo sapiens
-
0.0016
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid (4-morpholin-4-ylphenyl)amide
Homo sapiens
-
0.0091
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid (4-sulfamoyl phenyl)amide
Homo sapiens
-
0.0013
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid 4-amino benzyl amide
Homo sapiens
-
0.0016
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid 4-ethoxycarbonyl phenyl ester
Homo sapiens
-
0.0027
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid 4-methoxycarbonyl benzyl ester
Homo sapiens
-
0.0019
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid 4-methoxycarbonyl methyl phenyl ester
Homo sapiens
-
0.0056
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid amide
Homo sapiens
-
0.0016
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid benzyl amide
Homo sapiens
-
0.00071
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid benzyl ester
Homo sapiens
-
0.0016
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid phenyl amide
Homo sapiens
-
0.0022
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid phenyl ester
Homo sapiens
-
0.0074
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carboxylic acid(pyridin-2-ylmethyl)amide
Homo sapiens
-
0.0031
(R)-2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-4-sulfamoyl benzyl amide
Homo sapiens
-
0.00000032
(R)-3-amino-1-((R)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.00043
(R)-3-amino-1-((S)-8-((S)-(4-fluorophenyl)(hydroxy)methyl)-3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)butan-1-one
Rattus norvegicus
-
-
0.000027
(R)-3-amino-4-(2,5-difluorophenyl)-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)butan-1-one
Mus musculus
-
-
0.00077
(R)-4-([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino) benzoic acid ethyl ester
Homo sapiens
-
0.0089
(R)-4-([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)benzenesulfonic acid
Homo sapiens
-
0.0059
(R)-4-([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)benzoic acid
Homo sapiens
-
0.0014
(R)-4-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]benzoic acid
Homo sapiens
-
0.003
(R)-4-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]benzoic acid methyl ester
Homo sapiens
-
0.0085
(R)-[2-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid
Homo sapiens
-
0.0048
(R)-[2-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid ethyl ester
Homo sapiens
-
0.0028
(R)-[3-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]phenoxy]acetic acid
Homo sapiens
-
0.002
(R)-[3-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]phenoxy]acetic acid ethyl ester
Homo sapiens
-
0.0043
(R)-[3-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid
Homo sapiens
-
0.0019
(R)-[3-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid ethyl ester
Homo sapiens
-
0.0025
(R)-[4-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]phenoxy]acetic acid
Homo sapiens
-
0.0021
(R)-[4-[([2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino)methyl]phenoxy]acetic acid ethyl ester
Homo sapiens
-
0.0022
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]-(R)-isopropyl acetic acid
Homo sapiens
-
0.0036
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]-(R)-isopropyl acetic acid ethyl ester
Homo sapiens
-
0.0027
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]-(S )-isopropyl acetic acid
Homo sapiens
-
0.0026
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]-(S )-isopropyl acetic acid ethyl ester
Homo sapiens
-
0.00051
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid
Homo sapiens
-
0.00069
(R)-[4-[[2-[3-amino-4-(2,4,5-trifluorophenyl)butyryl]-3,4-dihydro-2H-pyrazole-3-carbonyl]amino]phenoxy]acetic acid ethyl ester
Homo sapiens
-
0.0001656
(S)-1-(2-(2-(2-oxo-3-(3,4,5-trimethoxyphenyl)imidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000293
(S)-1-(2-(2-(2-oxo-3-p-tolylimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000348
(S)-1-(2-(2-(2-oxo-3-phenylimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0001336
(S)-1-(2-(2-(3-(2-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.000002
(S)-1-(2-(2-(3-(3,4-dimethoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000204
(S)-1-(2-(2-(3-(3,5-dimethoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000601
(S)-1-(2-(2-(3-(3-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000651
(S)-1-(2-(2-(3-(3-methoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000258
(S)-1-(2-(2-(3-(4-chlorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000445
(S)-1-(2-(2-(3-(4-fluorophenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000824
(S)-1-(2-(2-(3-(4-methoxyphenyl)-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000535
(S)-1-(2-(2-(3-butyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000686
(S)-1-(2-(2-(3-cyclohexyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000478
(S)-1-(2-(2-(3-isopropyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000681
(S)-1-(2-(2-(3-tert-butyl-2-oxoimidazolidin-1-yl)ethylamino)acetyl)pyrrolidine-2-carbonitrile
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.001
1-(1-methyl-6-phenyl-1H-benzimidazol-7-yl)methanamine
Homo sapiens
-
0.0000041 - 0.0000072
1-(2-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.00023
1-(2-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]phenyl)ethanone
Homo sapiens
-
-
0.0000042 - 0.0000072
1-(3,4-dichlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.0313
1-(3,4-dimethoxyphenyl)-3-(3,4-dimethylphenyl)piperidin-4-amine
Homo sapiens
-
-
0.0256
1-(3,4-dimethoxyphenyl)-3-(3-methoxyphenyl)piperidin-4-amine
Homo sapiens
-
-
0.0006
1-(3,4-dimethoxyphenyl)-3-(3-methylphenyl)piperidin-4-amine
Homo sapiens
-
-
0.0148
1-(3,4-dimethoxyphenyl)-3-(4-methylphenyl)piperidin-4-amine
Homo sapiens
-
-
0.0089
1-(3,4-dimethoxyphenyl)-3-pyridin-2-ylpiperidin-4-amine
Homo sapiens
-
-
0.0003
1-(3-benzyl-4-oxido-3H-imidazo[4,5-b]pyridin-2-yl)piperidin-3-aminium
Homo sapiens
-
-
0.0000087 - 0.0000103
1-(3-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.000014
1-(3-methyl-1,2,4-thiadiazol-5-yl)-4-[[(2S,3S,5S)-2-methyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]carbonyl]piperazine
Homo sapiens
-
-
0.000019
1-(3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]phenyl)ethanone
Homo sapiens
-
-
0.0000108 - 0.0000109
1-(4-bromophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.0000122 - 0.0000175
1-(4-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.0000762
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
0.000001 - 0.0000014
1-(4-ethynylpyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.0000135 - 0.0000169
1-(4-fluorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.0000109 - 0.0000176
1-(4-methoxyphenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.0000029
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,4-diazepane
0.0000082 - 0.000009
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.000016
1-(4-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]phenyl)ethanone
Homo sapiens
-
-
0.0000025 - 0.0000031
1-(5-chloropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.00000092 - 0.0000011
1-(5-nitropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.00071
1-(6-chloro-2-isobutyl-4-phenyl-3,4-dihydroquinolin-3-yl)methanamine
Homo sapiens
-
pH 8.0, 37°C
0.000021 - 0.0000314
1-(diphenylmethyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.0000305 - 0.0000383
1-benzyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.00046
1-cyclohexyl-2-oxo-2-(1,3-thiazolidin-3-yl)ethanaminium 2,2,2-trifluoro-1-oxoethanide
Homo sapiens
-
0.0000575 - 0.0000811
1-methyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.000151
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
0.0000109 - 0.0000176
1-phenyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.0000027 - 0.0000035
1-pyridin-2-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.0000031 - 0.0000039
1-pyridin-4-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
0.00101
1-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-4,4-dimethyl-1-oxopentan-2-amine
Homo sapiens
-
-
0.00012
1-[(2S)-2-amino-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butyl]piperidin-2-one
Homo sapiens
-
-
0.000019
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-4-methylpiperidin-2-one
Rattus norvegicus
-
-
0.0000037
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-5-methylpiperidin-2-one
Rattus norvegicus
-
-
0.00043
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]azepan-2-one
Rattus norvegicus
-
-
0.000022 - 0.0078
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
0.0019
1-[(3R)-3-amino-4-phenylbutanoyl]-N-[5-chloro-2-[2-(cyclopropylamino)-2-oxoethoxy]benzyl]-L-prolinamide
Homo sapiens
-
-
0.0000034
1-[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]indane-5-carbonitrile
Homo sapiens
-
0.0000052
1-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
0.00000054
1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-N-benzyl-L-prolinamide
Homo sapiens
-
0.0000016
1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-N-[4-(1H-1,2,3-triazol-4-yl)butyl]-L-prolinamide
Homo sapiens
-
0.000000039
1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-N-[4-(2,3-dihydro-1H-tetrazol-5-yl)butyl]-L-prolinamide
Homo sapiens
-
0.00000072
1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-N-[4-(trifluoromethyl)benzyl]-L-prolinamide
Homo sapiens
-
0.000024
1-[(3S,4S)-4-amino-1-[4-(3,3-difluoropyrrolidin-1-yl)-1,3,5-triazin-2-yl]pyrrolidin-3-yl]-4,4-difluoropiperidin-2-one
Homo sapiens
-
-
0.0000998
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
0.0000047 - 0.0000072
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)phenyl]piperazine
0.0000015
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
-
0.0000015 - 0.0000018
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
0.0000476 - 0.0000744
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
0.000009
1-[1-(2-chlorobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.000011 - 0.00045
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
0.000002 - 0.0006
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
0.00026
1-[1-(2-cyanobenzyl)-5-methyl-4-oxo-4,5-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.000005
1-[1-(2-cyanobenzyl)-6-methyl-7-oxo-3a,6,7,7a-tetrahydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.0012
1-[1-(3-cyanobenzyl)-6-methyl-7-oxo-6,7-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.000102
1-[1-benzyl-6-(2-chlorophenyl)-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.000098
1-[1-methyl-6-(2-methylphenyl)-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.000011
1-[1-[3-(cyanomethyl)benzyl]-6-methyl-7-oxo-6,7-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.000527
1-[3-[2-[2-cyano-(S)-pyrrolidin-1-yl]-2-oxoethylamino]-1-oxopropyl]-4-[benzothiazol-2-yl]piperazine
Homo sapiens
-
-
0.000025
1-[4,9-dioxo-1-[2-(trifluoromethyl)benzyl]-4,9-dihydro-1H-naphtho[2,3-d]imidazol-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.000029
1-[5-benzyl-1-(3-cyanobenzyl)-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.00005
1-[5-bromo-6-(2-chlorophenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.000022
1-[5-methyl-4,6-dioxo-1-[2-(trifluoromethoxy)benzyl]-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.00001
1-[5-methyl-4,6-dioxo-1-[2-(trifluoromethyl)benzyl]-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.000066
1-[6-(2,4-dichlorophenyl)-1-ethyl-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.000062
1-[6-(2,4-dichlorophenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.00063
1-[6-(2,4-dichlorophenyl)-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.00079
1-[6-(2,4-difluorophenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.00032
1-[6-(2-chloro-5-fluorophenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.00016
1-[6-(2-chlorophenyl)-1,2-dimethyl-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.000061
1-[6-(2-chlorophenyl)-1-methyl-1H-1,2,3-benzotriazol-7-yl]methanamine
Homo sapiens
-
0.000063
1-[6-(2-chlorophenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.000011
1-[6-(2-chlorophenyl)-1-methyl-2-pyridin-3-yl-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.000097
1-[6-(2-chlorophenyl)-2-ethyl-1-methyl-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.000066
1-[6-(2-chlorophenyl)-2-methoxy-1-methyl-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.002
1-[6-(2-methoxyphenyl)-1-methyl-1H-benzimidazol-7-yl]methanamine
Homo sapiens
-
0.000002 - 0.000007
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
0.000057
1-[7-fluoro-6-methoxy-1-[2-(trifluoromethyl)benzyl]-1H-benzimidazol-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.000012
1-[amino(cyclohexyl)acetyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
pH 8.0, 37°C
0.000012 - 0.000014
1-[[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-2-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[1,5-a]pyrazin-8-yl]methyl]cyclopropanol
0.000109
2,2-bis(4-chlorophenyl)-N-[2-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-2-methylpropyl]acetamide
Homo sapiens
-
-
0.00032
2-(2-[4-(4-chloro-phenyl)-piperazin-1-yl]-2-oxoethylsulfanyl)-4-hydroxy-6-phenyl-pyrimidine-5-carbonitrile
Homo sapiens
-
pH not specified in the publication, 37°C
0.000582
2-(3-aminopiperidin-1-yl)-1-but-2-yn-1-yl-4-cyano-N-(naphthalen-1-ylmethyl)-1H-imidazole-5-carboxamide
Homo sapiens
-
-
0.000107
2-(3-aminopiperidin-1-yl)-1-but-2-yn-1-yl-N-(naphthalen-1-ylmethyl)-1H-imidazole-5-carboxamide
Homo sapiens
-
-
0.003059
2-(3-aminopiperidin-1-yl)-1-but-2-yn-1-yl-N-methyl-N-(naphthalen-1-ylmethyl)-1H-imidazole-5-carboxamide
Homo sapiens
-
-
0.000099
2-(3-aminopiperidin-1-yl)-1-but-2-yn-1-yl-N-[(3-methylisoquinolin-1-yl)methyl]-1H-imidazole-5-carboxamide
Homo sapiens
-
-
0.000014
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-(10,11-dihydrodibenzo[b,f][1,4]oxazepin-11-ylmethyl)-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000026
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-(2-oxo-2-phenylethyl)-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000089
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-(naphthalen-1-ylmethyl)-3,5-dihydro-4H-imidazo[4,5-c]pyridin-4-one
Homo sapiens
-
-
0.000013
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-(naphthalen-1-ylmethyl)-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000025
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(11R)-10,11-dihydrodibenzo[b,f][1,4]oxazepin-11-ylmethyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000003
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(11S)-10,11-dihydrodibenzo[b,f][1,4]oxazepin-11-ylmethyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000021
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(3-methylisoquinolin-1-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-c]pyridin-4-one
Homo sapiens
-
-
0.000005
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(3-methylisoquinolin-1-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000001
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000004
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-5-[(6-methyl-1,3-benzoxazol-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000052
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-7-methoxy-5-(naphthalen-1-ylmethyl)-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000019
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-7-methoxy-5-[(3-methylisoquinolin-1-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000007
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-7-methyl-5-[(3-methylisoquinolin-1-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000001
2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-7-methyl-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000559
2-(3-aminopiperidin-1-yl)-4-bromo-1-but-2-yn-1-yl-N-(naphthalen-1-ylmethyl)-1H-imidazole-5-carboxamide
Homo sapiens
-
-
0.0000073
2-(3-but-2-yn-1-yl-4-oxo-2-piperazin-1-yl-3,4-dihydro-5H-imidazo[4,5-d]pyridazin-5-yl)benzonitrile
Homo sapiens
-
-
0.000025
2-(4-[(3R,5S)-5-[(3,3,4,4-tetrafluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
Homo sapiens
-
0.000134
2-(4-[(3R,5S)-5-[(3,3-difluoroazetidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
Homo sapiens
-
0.0000058 - 0.0000082
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)-1,3-benzoxazole
0.0000056
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrazine
Homo sapiens
-
0.0000048
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyridine-3-carbonitrile
Homo sapiens
-
0.0000087
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
Homo sapiens
-
0.0000052
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)[1,3]oxazolo[5,4-b]pyridine
Homo sapiens
-
0.000041
2-(4-[(3R,5S)-5-[(3-fluoroazetidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)pyrimidine
Homo sapiens
-
0.0000023
2-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methoxy)pyridine-4-carbonitrile
Homo sapiens
-
-
0.000129
2-([(3S,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]carbonyl)isoindoline
Homo sapiens
-
-
0.00025
2-([2-(4-aminopiperidin-1-yl)-2-oxoethyl]sulfanyl)-4-hydroxy-6-phenylpyrimidine-5-carbonitrile
Homo sapiens
-
pH not specified in the publication, 37°C
0.000013
2-([2-[(3R)-3-aminopiperidin-1-yl]-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-5-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000019
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,7-dimethoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000013
2-([2-[(3R)-3-aminopiperidin-1-yl]-6,8-dichloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-bromo-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000004 - 0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
0.000008
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000015
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000004
2-([2-[(3R)-3-aminopiperidin-1-yl]-7-fluoro-6-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000029
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-chloro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.00003
2-([2-[(3R)-3-aminopiperidin-1-yl]-8-methoxy-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000018
2-([2-[(3S)-3-aminopiperidin-1-yl]-6-fluoro-7-morpholin-4-yl-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000007
2-([6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl]methyl)benzonitrile
Homo sapiens
-
-
0.0000362
2-([8-[(3R)-3-aminopiperidin-1-yl]-3-methyl-7-(3-methylbut-2-en-1-yl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-1-yl]methyl)benzonitrile
Homo sapiens
pH not specified in the publication, 37°C
0.0065
2-ethoxy-4-[2-(methylsulfanyl)ethyl]-1,3,2-oxazaphospholidine 2-sulfide
Homo sapiens
-
0.000001
2-[(2-aminoethyl)(methyl)amino]-3-but-2-yn-1-yl-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.0000025
2-[(2R)-2-amino-4-oxo-4-(1,3-thiazolidin-3-yl)butyl]benzonitrile
Homo sapiens
-
0.0000056
2-[(2S,3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-2-methylpyrrolidin-3-yl]-N,N-dimethylacetamide
Homo sapiens
-
37°C, pH 7.4
0.00099
2-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-phenylpyrazolidine-1-carboxamide
Homo sapiens
-
-
0.000005
2-[(3R)-3-aminopiperidin-1-yl]-3-but-2-yn-1-yl-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.000014
2-[(3R)-4-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-3-benzylpiperazin-1-yl]-N-[3-[(methylsulfonyl)amino]phenyl]acetamide
Homo sapiens
-
-
0.0000045
2-[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylacetamide
Homo sapiens
-
-
0.0000195 - 0.000039
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000165
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
0.0000022
2-[(7-but-2-yn-1-yl-2-methoxy-6-oxo-8-piperazin-1-yl-6,7-dihydro-1H-purin-1-yl)methyl]benzonitrile
Homo sapiens
-
-
0.0000028
2-[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000377
2-[(8S)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-8-yl]-N,N-dimethylacetamide
Rattus norvegicus
-
-
0.0000032
2-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)amino]pyridine-3-carbonitrile
Homo sapiens
-
-
0.00051
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-fluorobenzyl)acetamide
Rattus norvegicus
-
-
0.001027
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(2-methoxyethyl)acetamide
Rattus norvegicus
-
-
0.000185
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4,5-dimethyl-1,3-thiazol-2-yl)acetamide
Rattus norvegicus
-
-
0.00009 - 0.000098
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
0.000143
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(pyrimidin-2-yl)acetamide
Rattus norvegicus
-
-
0.000523
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(tricyclo[3.3.1.13,7]dec-1-yl)acetamide
Rattus norvegicus
-
-
0.000506
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclohexylacetamide
Rattus norvegicus
-
-
0.000217 - 0.000236
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
0.000415
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[2-(thiophen-2-yl)ethyl]acetamide
Rattus norvegicus
-
-
0.000468
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[3-(propan-2-yloxy)propyl]acetamide
Rattus norvegicus
-
-
0.000308
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-[4-(trifluoromethyl)phenyl]acetamide
Rattus norvegicus
-
-
0.000817
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.011
2-[4-[(2S)-2-amino-3-phenylpropyl]-3-benzylpiperazin-1-yl]-N-[3-[(methylsulfonyl)amino]phenyl]acetamide
Homo sapiens
-
-
0.000309
2-[4-[(3R,5S)-5-(azetidin-1-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
Homo sapiens
-
0.000031
2-[4-[(3R,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
Homo sapiens
-
0.000051
2-[4-[(3R,5S)-5-[[(3R)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
Homo sapiens
-
0.000309
2-[4-[(3R,5S)-5-[[(3R,4R)-3,4-difluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
Homo sapiens
-
0.000013
2-[4-[(3R,5S)-5-[[(3R,4S)-3,4-difluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
Homo sapiens
-
0.000031
2-[4-[(3R,5S)-5-[[(3S)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]piperazin-1-yl]pyrimidine
Homo sapiens
-
0.0000012
2-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
0.000093
2-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzonitrile
Homo sapiens
-
-
0.004
2-[7-(aminomethyl)-1-methyl-1H-benzimidazol-6-yl]benzamide
Homo sapiens
-
0.0016
2-[7-(aminomethyl)-1-methyl-1H-benzimidazol-6-yl]phenol
Homo sapiens
-
0.000096
2-[7-(aminomethyl)-6-(2-chlorophenyl)-1H-benzimidazol-1-yl]ethanol
Homo sapiens
-
0.000002
2-[[(2S)-2-aminopropyl](methyl)amino]-3-but-2-yn-1-yl-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.0000033
2-[[(3S)-3-[[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]carbonyl]-1,2,3,4-tetrahydroisoquinolin-7-yl]oxy]acetamide
Homo sapiens
-
-
0.000084
2-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
Homo sapiens
-
-
0.000073
2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]-5-(trifluoromethyl)isoindoline
Homo sapiens
-
-
0.000109
2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
Homo sapiens
-
-
0.000228
2-[[(3S,5S)-5-[[(3R)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]carbonyl]isoindoline
Homo sapiens
-
-
0.000245
2-[[(3S,5S)-5-[[(3S)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]carbonyl]isoindoline
Homo sapiens
-
-
0.000049
3-(1-amino-2-oxo-2-pyrrolidin-1-ylethyl)tricyclo[3.3.1.13,7]decan-1-ol
Homo sapiens
-
-
0.000000003
3-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-yl)-1,2,4-oxadiazolidin-5-one
Homo sapiens
-
0.00025
3-(aminomethyl)-2-isobutyl-4-phenylisoquinolin-1(2H)-one
Homo sapiens
-
pH 8.0, 37°C
0.000007
3-(aminomethyl)-4-(2,4-dichlorophenyl)-7,8-dimethoxy-5H-indeno[1,2-b]pyridin-2-amine
Homo sapiens
-
-
0.00037
3-(aminomethyl)-4-(2,4-dichlorophenyl)quinolin-2-amine
Homo sapiens
-
pH 8.0, 37°C
0.000026
3-([2-[(2S)-2-cyano-4,4-difluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000056
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000047
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.00006
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[3-(trifluoromethyl)phenyl]cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000085
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[2-[4-(trifluoromethyl)phenyl]cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000084
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(2,4-di-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000068
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000063
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000101
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,4-di-methoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000075
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3,5-di-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000042
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000064
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000073
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000086
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000054
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(4-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000085
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-phenylcyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000116
3-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
Homo sapiens
-
-
0.000016
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]-amino)-3-methyl-N-[trans-2-(4-methyl-1,3-thiazol-5-yl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000019
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-(pyridin-2-yl)butanamide
Homo sapiens
-
-
0.000027
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1R,2S)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000015
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000017
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-ethoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000021
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-fluorophenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000026
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-methoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.00002
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(3-trifluoromethoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000022
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-(4-methoxyphenyl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000019
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[(1S,2R)-2-phenylcyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000024
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methyl-N-[trans-2-(pyridin-3-yl)cyclopropyl]butanamide
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000019 - 0.000027
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
0.000029
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-cyclopentyl-3-methylbutanamide
Homo sapiens
-
-
0.00005
3-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)benzoic acid
Homo sapiens
-
0.000003
3-but-2-yn-1-yl-2-(1,4-diazepan-1-yl)-5-[(4-methylquinazolin-2-yl)methyl]-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.0001
3-but-2-yn-1-yl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one
Homo sapiens
-
-
0.0001 - 0.00036
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
0.0136
3-butyl-1-(5,6,7,8-tetrahydronaphthalen-1-yl)piperidin-4-amine
Homo sapiens
-
-
0.0035
3-butyl-1-(diphenylmethyl)piperidin-4-amine
Homo sapiens
-
-
0.0053
3-butyl-1-naphthalen-1-ylpiperidin-4-amine
Homo sapiens
-
-
0.0084
3-butyl-1-[3-methoxy-5-(trifluoromethyl)phenyl]piperidin-4-amine
Homo sapiens
-
-
0.0026
3-butyl-1-[4-chloro-3-(trifluoromethyl)phenyl]piperidin-4-amine
Homo sapiens
-
-
0.00064
3-butyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.0000089
3-[(2R)-2-amino-4-oxo-4-(1,3-thiazolidin-3-yl)butyl]benzonitrile
Homo sapiens
-
0.000538 - 0.000607
3-[(2S)-pyrrolidin-2-ylcarbonyl]-1,3-thiazolidine
0.000142
3-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-1,3-oxazinan-2-one
Rattus norvegicus
-
-
0.0000024
3-[(3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]-N,N-dimethylpropanamide
Homo sapiens
-
-
0.00142
3-[1-amino-2-(2H-isoindol-2-yl)-2-oxoethyl]tricyclo[3.3.1.13,7]decan-1-ol
Homo sapiens
-
-
0.003311
3-[1-amino-2-(4,5-dihydro-1H-pyrazol-1-yl)-2-oxoethyl]tricyclo[3.3.1.13,7]decan-1-ol
Homo sapiens
-
-
0.000028
3-[1-amino-2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]tricyclo[3.3.1.13,7]decan-1-ol
Homo sapiens
-
-
0.001944
3-[1-amino-2-[(1R,5S)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]tricyclo[3.3.1.13,7]decan-1-ol
Homo sapiens
-
-
0.0000029 - 0.000607
3-[1-amino-2-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]-5,7-dimethyltricyclo[3.3.1.13,7]decan-1-ol
0.00001
3-[1-amino-2-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]tricyclo[3.3.1.13,7]decan-1-ol
Homo sapiens
-
-
0.000007
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]-N,N-dimethylbenzamide
Homo sapiens
-
0.0000018 - 0.000005
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
0.000037
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzonitrile
Homo sapiens
-
-
0.00007
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]phenol
Homo sapiens
-
-
0.0014
3-[6-[(3R,4S)-3-amino-4-phenylpyrrolidin-1-yl]pyrimidin-4-yl]benzonitrile
Homo sapiens
-
-
0.000032
4'-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]biphenyl-3-carboxamide
Homo sapiens
-
-
0.0000001 - 0.0001
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-carboxamide
0.000000056
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-carboxylic acid
Homo sapiens
-
0.00000014
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-sulfonamide
Homo sapiens
-
0.00000037
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-4-carboxylic acid
Homo sapiens
-
0.0000093
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
0.00000011
4-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-yl)-1,3-dihydro-2H-imidazol-2-one
Homo sapiens
-
0.0000033
4-(4-nitrophenyl)-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
0.0000125
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.000005
4-([1-[(2-oxo-2-thiophen-3-ylethyl)amino]cyclopentyl]methoxy)benzamide
Homo sapiens
-
-
0.000067
4-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)benzamide
Homo sapiens
-
0.00026
4-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)benzenesulfonamide
Homo sapiens
-
0.000223
4-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)benzoic acid
Homo sapiens
-
0.00015
4-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]sulfonyl)benzoic acid
Homo sapiens
-
0.000005
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.0000136
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.0000343
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.000168
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
0.0000341
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
0.00021 - 0.214
4-nitrobenzyl[(5S)-5-amino-6-oxo-6-(1-pyrrolidinyl)hexyl]carbamate
0.0000096
4-phenyl-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
0.000005
4-[(1-[[2-oxo-2-(3-thienyl)ethyl]amino]cyclopentyl)methoxy]benzamide
Homo sapiens
-
0.0000147
4-[(2R)-2-amino-4-oxo-4-(1,3-thiazolidin-3-yl)butyl]benzonitrile
Homo sapiens
-
0.003007
4-[(2S)-2-amino-3-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-3-oxopropyl]phenol
Homo sapiens
-
-
0.00005
4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-(4-methylphenyl)-1,4-diazepane-1-carboxamide
Homo sapiens
-
0.001392
4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-phenyl-1,4-diazepane-1-carboxamide
Homo sapiens
-
0.00028
4-[(3R)-3-[(2-oxo-2-phenylethyl)amino]butyl]benzamide
Homo sapiens
-
0.0038
4-[(3R)-3-[[2-(2-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide
Homo sapiens
-
0.000039
4-[(3R)-3-[[2-(3,4-difluorophenyl)-2-oxoethyl]amino]butyl]benzamide
Homo sapiens
-
0.00082
4-[(3R)-3-[[2-(4-chlorophenyl)-2-oxoethyl]amino]butyl]benzamide
Homo sapiens
-
0.000084
4-[(3R)-3-[[2-(4-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide
0.00011
4-[(3R)-3-[[2-oxo-2-(3-thienyl)ethyl]amino]butyl]benzamide
Homo sapiens
-
0.0000139 - 0.0000189
4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]morpholine
0.0000042
4-[([1-[(2S)-2-amino-2-cyclohexylacetyl]-L-prolyl]amino)methyl]benzoic acid
Homo sapiens
-
0.0435
4-[2-(methylsulfanyl)ethyl]-2-phenoxy-1,3,2-oxazaphospholidine 2-sulfide
Homo sapiens
-
0.0000018
4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]benzene-1,2-dicarbonitrile
0.000085
4-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
Homo sapiens
-
0.00013
4-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzonitrile
Homo sapiens
-
-
0.00034
4-[[(2R)-2-[[2-oxo-2-(3-thienyl)ethyl]amino]propyl]oxy]benzamide
Homo sapiens
-
0.000081
4-[[(3R,4R)-3-amino-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]methyl]benzonitrile
Homo sapiens
-
0.0000047
4-[[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]methyl]-2,6-diethylbenzonitrile
Homo sapiens
-
0.0000011
4-[[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]methyl]-2,6-dimethylbenzonitrile
Homo sapiens
-
0.0000013
4-[[(3R,4R)-3-amino-4-[[(2R)-2-cyanocyclopentyl]carbonyl]pyrrolidin-1-yl]methyl]-2-methylbenzonitrile
Homo sapiens
-
0.0000336
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
0.000004
4-[[2-(3-aminopiperidin-1-yl)-3-but-2-yn-1-yl-4-oxo-3,4-dihydro-5H-imidazo[4,5-d]pyridazin-5-yl]methyl]naphthalene-1-carbonitrile
Homo sapiens
-
-
0.000144
5,6-dichloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
Homo sapiens
-
-
0.000024
5-(3-aminopiperidin-1-yl)-4-but-2-yn-1-yl-N-[(3-methylisoquinolin-1-yl)methyl]-4H-1,2,4-triazole-3-carboxamide
Homo sapiens
-
-
0.000000095
5-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-4-yl)-1,2,4-triazolidin-3-one
Homo sapiens
-
0.01
5-(aminomethyl)-6-(1,3-benzodioxol-5-yl)-2-phenylpyrimidin-4-amine
Homo sapiens
-
-
0.0000001
5-(aminomethyl)-6-(2,4-dichlorophenyl)-2-(3,5-dimethoxyphenyl)pyrimidin-4-amine
Homo sapiens
-
-
0.000003
5-(aminomethyl)-6-(2,4-dichlorophenyl)-2-phenylpyrimidin-4-amine
Homo sapiens
-
-
0.000009
5-(aminomethyl)-6-(2,4-dichlorophenyl)-N2-(2-methoxyethyl)-N2-methylpyrimidine-2,4-diamine
0.003081
5-([2-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]amino)tricyclo[3.3.1.13,7]decane-1,3-diol
Homo sapiens
-
-
0.00015
5-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)pyridine-2-carboxylic acid
Homo sapiens
-
0.000067
5-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)pyridine-3-carboxylic acid
Homo sapiens
-
0.00026
5-([4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepan-1-yl]carbonyl)tetrahydrofuran-2-carboxylic acid
Homo sapiens
-
0.0000107
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000134
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.00005
5-chloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
Homo sapiens
-
-
0.0000101
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.000073
5-fluoro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
Homo sapiens
-
-
0.0000061
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.000072
5-methyl-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
Homo sapiens
-
-
0.0000103
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.00027
5-[1-amino-2-(3-azabicyclo[3.1.0]hex-3-yl)-2-oxoethyl]tricyclo[3.3.1.13,7]decane-1,3-diol
Homo sapiens
-
-
0.000014
5-[1-amino-2-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]tricyclo[3.3.1.13,7]decane-1,3-diol
Homo sapiens
-
-
0.000078
5-[[(3R,4R)-3-amino-4-(pyrrolidin-1-ylcarbonyl)pyrrolidin-1-yl]methyl]-2-fluorobenzonitrile
Homo sapiens
-
0.0000099
6-(aminomethyl)-1,3-dimethyl-7-(1-methylpiperazinium)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0000046
6-(aminomethyl)-1,3-dimethyl-7-(morpholin-4-yl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000002
6-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methoxy)pyridine-3-carbonitrile
Homo sapiens
-
-
0.000004
6-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)(methyl)amino]pyridine-3-carbonitrile
Homo sapiens
-
-
0.0000035
6-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)amino]pyridine-3-carbonitrile
Homo sapiens
-
-
0.0000016 - 0.0000019
6-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
0.000022
6-[[2-([2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl]amino)ethyl]amino]nicotinonitrile
Homo sapiens
-
pH 8.0, 37°C
0.0000024
6-[[2-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)ethyl]amino]nicotinamide
Homo sapiens
-
-
0.00014 - 0.00078
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
0.000007 - 0.000022
6-{[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)ethyl]amino}pyridine-3-carbonitrile
0.000052
7-(aminomethyl)-6-(2-chlorophenyl)-1-methyl-1,3-dihydro-2H-benzimidazol-2-one
Homo sapiens
-
0.000008
7-(aminomethyl)-6-(2-chlorophenyl)-1-methyl-1H-benzimidazole-5-carbonitrile
Homo sapiens
-
0.000032
7-(aminomethyl)-6-(2-chlorophenyl)-1-methyl-1H-benzimidazole-5-carboxamide
Homo sapiens
-
0.0000048
7-amino-6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.00002
7-amino-6-(aminomethyl)-5-(2-fluoro-6-methoxyphenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.0039
7-benzyl-3-methyl-8-piperazin-1-yl-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
-
0.000089
7-but-2-ynyl-9-(6-methoxy-pyridin-3-yl)-6-piperazin-1-yl-7,9-dihydro-purin-8-one trifluoroacetate
Homo sapiens
-
-
0.0145
7-[(2-butyl-1,3-dioxo-2,3-dihydro-1H-benzo[de]isoquinolin-6-yl)amino]-N-[(3R)-1-[3-[(2-cyanophenyl)methyl]-1-methyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl]piperidin-3-yl]heptanamide
Homo sapiens
pH not specified in the publication, temperature not specified in the publication
0.000001
7-[(2E)-but-2-en-1-yl]-8-(3,3-dimethylpiperazin-1-yl)-3-methyl-1-(2-oxo-2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
-
0.000234
7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-N-tert-butyl-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxamide
Rattus norvegicus
-
-
0.0000012
7-[(3R,4R)-3-amino-4-(2,4,5-trifluorophenyl)piperidin-1-yl]-2H-pyrimido[1,2-b]pyridazin-2-one
Homo sapiens
-
-
0.002
7-[(3R,4R)-3-amino-4-(2-methoxyphenyl)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
Homo sapiens
-
-
0.0002
7-[(3R,4S)-3-amino-4-(2-methoxyphenyl)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
Homo sapiens
-
-
0.001
7-[(3R,4S)-3-amino-4-(3,4-dichlorophenyl)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
Homo sapiens
-
-
0.00014
7-[(3R,4S)-3-amino-4-(4-fluorophenyl)pyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
Homo sapiens
-
-
0.00015
7-[(3R,4S)-3-amino-4-phenylpyrrolidin-1-yl]-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
Homo sapiens
-
-
0.000015
8-(3-aminopiperidin-1-yl)-7-but-2-yn-1-yl-3-methyl-1-(naphthalen-1-ylmethyl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
-
0.000002
8-(3-aminopiperidin-1-yl)-7-but-2-yn-1-yl-3-methyl-1-[(3-methylisoquinolin-1-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
-
0.0000235
8-[(3R)-3-aminopiperidin-1-yl]-1-[(1,3-benzothiazol-2-yl)methyl]-3-methyl-7-(3-methylbut-2-en-1-yl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
pH not specified in the publication, 37°C
0.000006
8-[(3R)-3-aminopiperidin-1-yl]-3-methyl-7-(3-methylbut-2-en-1-yl)-1-(2-oxo-2-phenylethyl)-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
-
0.000001
8-[(3R)-3-aminopiperidin-1-yl]-7-but-2-yn-1-yl-3-methyl-1-[(4-methylquinazolin-2-yl)methyl]-3,7-dihydro-1H-purine-2,6-dione
Homo sapiens
-
-
0.000001
ABT-279
Homo sapiens
-
-
0.647
Ala-Ala-Leu-Glu-Gln-Thr-Glu-Arg
Homo sapiens
-
pH 8.0, 37°C
0.0000069 - 0.000024
alogliptin
0.00000236 - 0.00000553
ASP-8497
0.0000026 - 0.0000073
ASP8497
0.175
atorvastatin
Sus scrofa
-
37°C, pH 8.0
0.00049
benzyl 4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-1,4-diazepane-1-carboxylate
Homo sapiens
-
0.0000007
benzyl 6-([5-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-(4S)-4-amino-5-oxopentanoyl]amino)hexanoate
Homo sapiens
-
-
0.0000014
benzyl [(5S)-5-amino-6-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-6-oxohexyl]carbamate
Homo sapiens
-
-
0.0133
Berberine
Homo sapiens
in Tris buffer (pH 7.5, 50 mM), at 37°C
0.000001
Bl-1356
Homo sapiens
-
-
0.0000037
BMS-477118
Homo sapiens
-
-
0.0000068
carmegliptin
Rattus norvegicus
-
-
0.0023
D-Val-L-boroPro
Homo sapiens
-
pH 2
0.000022
denagliptin
Homo sapiens
-
-
0.000089
ER-319711-15
Homo sapiens
-
-
0.00049
ethyl (3R,4S)-3-amino-4-(2,4-dichlorophenyl)pyrrolidine-1-carboxylate
Homo sapiens
-
0.000000076
ethyl 4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-carboxylate
Homo sapiens
-
0.00000044
ethyl 4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-4-carboxylate
Homo sapiens
-
0.000031
ethyl 4-[(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxopentanoyl]piperazine-1-carboxylate
Rattus norvegicus
-
-
0.000063
ethyl 4-[3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanoyl]piperazine-1-carboxylate
Homo sapiens
-
-
0.000219
ethyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
Rattus norvegicus
-
-
0.00019
ethyl 7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazine-3-carboxylate
Rattus norvegicus
-
-
0.0000153
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
0.00115
ethyl [(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]carbamate
Rattus norvegicus
-
-
0.00456
ethyl-2-(4-(((S)-1-((S)-2-amino-(4-fluorophenyl)propanoyl)pyrrolidine-2-carboxamido)-methyl)phenoxy)acetate
Homo sapiens
pH 7.5, temperature not specified in the publication
0.0084
ethyl-2-(4-(((S)-1-((S)-2-amino-3-(2-fluorophenyl)propanoyl)pyrrolidine-2-carboxamido)-methyl)phenoxy)acetate
Homo sapiens
pH 7.5, temperature not specified in the publication
0.00000161
GRC 8200
Homo sapiens
-
-
0.022
L-isoleucinepyrrolidine
Homo sapiens
-
IC50: 0.022 mM
0.0000016 - 0.0012
L-Val-L-boroPro
0.0000035
LAF-237
Homo sapiens
-
-
0.000034
LY-2463665
Homo sapiens
-
-
0.329
Lys-Ala-Val-Gly-Glu-Pro-Pro-Leu-Phe
Homo sapiens
-
pH 8.0, 37°C
0.0013
Lys[Z(NO2)]-pyrrolidide
Mus musculus
-
-
0.00041
Lys[Z(NO2)]-thiazolidide
Mus musculus
-
-
0.0003
MCB3937
Homo sapiens
-
-
0.00000022
methyl (2S,3S)-3-amino-2-(4'-fluorobiphenyl-4-yl)-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanoate
Homo sapiens
-
0.000000087
methyl (4-[[([(4R)-3-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]-1,3-thiazolidin-4-yl]carbonyl)amino]methyl]phenyl)acetate
Homo sapiens
-
0.0000036
methyl 4-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]benzenesulfinate
Homo sapiens
-
0.00000017
methyl 4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]benzoate
Homo sapiens
-
0.000018
MK-0431
Homo sapiens
-
-
0.00000135
MP-513
Homo sapiens
-
-
0.000021
N,N-diallyl-3-(bicyclo[3.2.0]hept-6-ylsulfonyl)-1H-1,2,4-triazole-1-carboxamide
Homo sapiens
-
pH 8.0, 37°C
0.000134
N-(1,3-benzothiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000119 - 0.000124
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
0.000359
N-(3-chloro-4-fluorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000000027
N-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-yl)-1,1,1-trifluoromethanesulfonamide
Homo sapiens
-
0.00000015
N-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-yl)methanesulfonamide
Homo sapiens
-
0.00000071
N-(4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-4-yl)methanesulfonamide
Homo sapiens
-
0.000258
N-(4-chlorophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000023
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
0.0002
N-(4-cyanophenyl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000226
N-(5-bromo-1,3-thiazol-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00049
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-ethylhydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.03845
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-hydroperoxyhydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000088 - 0.00012
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
0.00011 - 0.00013
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
0.0000015
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1,1,1-trifluoro-N-methylmethanesulfonamide
Homo sapiens
-
-
0.000012
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1,1,1-trifluoromethanesulfonamide
Homo sapiens
-
-
0.0000027
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1-(trifluoromethyl)cyclopropanecarboxamide
Homo sapiens
-
-
0.0000056
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2,2-trifluoroethanesulfonamide
Homo sapiens
-
-
0.0000078
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluoro-N-methylpropanamide
Homo sapiens
-
-
0.0000013
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluorocyclopropanecarboxamide
Homo sapiens
-
-
0.0000059
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluoropropanamide
Homo sapiens
-
-
0.0000037
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-dimethylpropanamide
Homo sapiens
-
-
0.0000063
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluoro-2-methylpropanamide
Homo sapiens
-
-
0.0000035
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3,3,3-trifluoropropanamide
Homo sapiens
-
-
0.0000068
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N,2,2-trimethylpropanamide
Homo sapiens
-
-
0.0000027
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N-cyclopropyl-1,1,1-trifluoromethanesulfonamide
Homo sapiens
-
-
0.0000011
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N-methylcyclopropanecarboxamide
Homo sapiens
-
-
0.0000022
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclobutanecarboxamide
Homo sapiens
-
-
0.000009
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
Homo sapiens
-
-
0.000008
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
0.0000048
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclopentanecarboxamide
Homo sapiens
-
-
0.000027
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)methanesulfonamide
Homo sapiens
-
-
0.000027
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.000049
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzamide
Rattus norvegicus
-
-
0.000092
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzamide
Rattus norvegicus
-
-
0.000077
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.000092
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzamide
Rattus norvegicus
-
-
0.00009
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
Rattus norvegicus
-
-
0.000047
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-2-carboxamide
Rattus norvegicus
-
-
0.000087
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-3-carboxamide
Rattus norvegicus
-
-
0.000066
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-4-carboxamide
Rattus norvegicus
-
-
0.000009
N-([(2S)-1-[(3R)-3-amino-4-(3,4,6-trifluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
Rattus norvegicus
-
-
0.000014
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.00000038
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-(methylsulfonyl)benzamide
Rattus norvegicus
-
-
0.000027
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
Rattus norvegicus
-
-
0.000012
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
Rattus norvegicus
-
-
0.00003
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
Rattus norvegicus
-
-
0.000008
N-([(2S)-1-[(3R)-3-amino-4-(5-chlorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
Rattus norvegicus
-
-
0.000024
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2,5-dichlorobenzenesulfonamide
Rattus norvegicus
-
-
0.000053
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzenesulfonamide
Rattus norvegicus
-
-
0.000094
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzenesulfonamide
Rattus norvegicus
-
-
0.00002
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-chlorobenzenesulfonamide
Rattus norvegicus
-
-
0.000027
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzenesulfonamide
Rattus norvegicus
-
-
0.000034
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
Rattus norvegicus
-
-
0.000015
N-[(1S,2R)-2-(3-chlorophenyl)cyclopropyl]-3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-3-methylbutanamide
Homo sapiens
-
-
0.01
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-2-methylbutanamide
Rattus norvegicus
-
-
0.0000026 - 0.000013
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
0.000013
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylpentanamide
Rattus norvegicus
-
-
0.00051
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]butanamide
Rattus norvegicus
-
-
0.0022
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]pentanamide
Rattus norvegicus
-
-
0.00133
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]propane-1-sulfonamide
Rattus norvegicus
-
-
0.000031
N-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butyl]-6-(trifluoromethyl)-3,4-dihydropyrrolo[1,2-a]pyrazine-2(1H)-carboxamide
Homo sapiens
-
pH 7.5, temperature not specified in the publication
0.000236
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
0.000013
N-[2-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-2-methylpropyl]-1-methylcyclohexanecarboxamide
Homo sapiens
-
-
0.0000058
N-[2-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-2-methylpropyl]-2,2-dimethylpropanamide
Homo sapiens
-
-
0.0113
N-[2-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-2-oxoethyl]-N-methyl-5-oxoprolinamide
Homo sapiens
-
23°C, pH 7.4
0.0000015
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-1H-1,2,3-benzotriazole-5-carboxamide
Homo sapiens
-
-
0.0000057
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-1H-benzimidazole-5-carboxamide
Homo sapiens
-
-
0.0000029
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-2,3-dihydro-1-benzofuran-5-carboxamide
Homo sapiens
-
-
0.0000062
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-N-(4-cyanobenzyl)benzamide
Homo sapiens
-
-
0.0000073
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-N-isobutylbenzamide
Homo sapiens
-
-
0.000031
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]-N-methylbenzenesulfonamide
Homo sapiens
-
-
0.0000045
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]benzamide
Homo sapiens
-
-
0.000075
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]benzenesulfonamide
Homo sapiens
-
-
0.0000082
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]pyridine-2-carboxamide
Homo sapiens
-
-
0.0000054
N-[2-[[2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino]-2-methylpropyl]thiophene-2-carboxamide
Homo sapiens
-
-
0.011
N-[3-[(2-[4-[(2S)-2-amino-3-phenylpropyl]-3-benzylpiperazin-1-yl]ethyl)amino]phenyl]methanesulfonamide
Homo sapiens
-
-
0.000022
NVP DPP728
Homo sapiens
-
-
0.000011
P-[(3S)-3-amino-2-oxopyrrolidin-1-yl]phosphonic diamide
Homo sapiens
-
pH 8.0, 37°C
0.00042
P32/98
Homo sapiens
-
-
0.00042
P32/P98
Homo sapiens
-
-
0.0000006 - 0.00005
saxagliptin
0.00000996 - 0.000087
sitagliptin
0.000018
SSR-162369
Homo sapiens
-
-
0.000021
sulphostin
Rattus norvegicus
-
IC50: 21 nM
0.000007
SYR-322
Homo sapiens
-
-
0.001534
tert-butyl 2-(1-acetylpiperidin-4-yl)-2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.004149
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,2-dimethylpropanoyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.001793
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(2,3-dichlorobenzoyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.001228
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(dimethylcarbamoyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.00083
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.00079
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(morpholin-4-ylcarbonyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.000667
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-(pyridin-3-ylacetyl)piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
0.000866
tert-butyl 2-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]-2-[1-[(4-methylcyclohexyl)carbonyl]piperidin-4-yl]hydrazinecarboxylate
Rattus norvegicus
-
-
1.2
TLCK
Rattus norvegicus
-
pH 8.0, 37°C
0.44
Val-pyrrolidide
Homo sapiens
-
recombinant enzyme
0.00000167 - 0.000062
vildagliptin
0.451
[(2R)-1-(4-oxo-4-phenylbutanoyl)pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.006871
[(2R)-1-(N-acetyl-N-methylglycyl)pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.000377
[(2R)-1-(N-acetylglycyl)pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.0227
[(2R)-1-[(1-oxo-1,3-dihydro-2H-isoindol-2-yl)acetyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.182
[(2R)-1-[(2-oxopyridin-1(2H)-yl)acetyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.608
[(2R)-1-[N-(2,2-dimethylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.0043
[(2R)-1-[N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.007391
[(2R)-1-[N-(cyclohexylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.00908
[(2R)-1-[N-(cyclopentylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.000068 - 0.00143
[(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]boronic acid
0.0384
[(2R)-1-[N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.0046
[(2R)-1-[N-methyl-N-(2-methylpropanoyl)glycyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.0195
[(2R)-1-[N-methyl-N-(phenylcarbonyl)glycyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.0095
[(2R)-1-[N-[(2,5-dichlorophenyl)carbonyl]glycyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.0000003
[(2R,4R)-1-(L-arginyl)-4-hydroxypyrrolidin-2-yl]boronic acid
Homo sapiens
-
pH 7.8, temperature not specified in the publication
0.0002
[(2S)-1-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]pyrrolidin-2-yl]methanol
Homo sapiens
-
-
0.0092
[(2S)-1-[(3S)-3-amino-4-[(3S)-3-fluoropyrrolidin-1-yl]-4-oxobutanoyl]pyrrolidin-2-yl]methanol
Homo sapiens
-
-
0.0000699
[(3R)-4-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-3-methyl-2-oxo-1,4-diazepan-1-yl]acetic acid
Homo sapiens
-
-
0.000016
[(3R,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]acetic acid
Homo sapiens
-
-
0.0000163
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
0.000025
[(R)-amino[(3S)-3-amino-2-oxoazepan-1-yl]phosphoryl]sulfamic acid
Homo sapiens
-
pH 8.0, 37°C
0.000021
[(R)-amino[(3S)-3-amino-2-oxopiperidin-1-yl]phosphoryl]sulfamic acid
Homo sapiens
-
pH 8.0, 37°C
0.0000036
[2-[([1-[(2S)-2-amino-2-cyclohexylacetyl]-L-prolyl]amino)methyl]phenyl]acetic acid
Homo sapiens
-
0.0000012
[2-[([1-[(3S)-3-amino-4-phenylbutanoyl]-L-prolyl]amino)methyl]phenyl]acetic acid
Homo sapiens
-
0.0004
[2-[7-(aminomethyl)-1-methyl-1H-benzimidazol-6-yl]phenyl]methanol
Homo sapiens
-
0.0000033
[3-[([1-[(2S)-2-amino-2-cyclohexylacetyl]-L-prolyl]amino)methyl]phenyl]acetic acid
Homo sapiens
-
0.0000012
[3-[([1-[(3S)-3-amino-4-phenylbutanoyl]-L-prolyl]amino)methyl]phenyl]acetic acid
Homo sapiens
-
0.00000012
[4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]acetic acid
Homo sapiens
-
0.000000054
[4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenyl]acetic acid
Homo sapiens
-
0.000000074
[4-[([1-[(3S)-3-amino-4-(3,4-difluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenyl]acetic acid
Homo sapiens
-
0.00000051
[4-[([1-[(3S)-3-amino-4-phenylbutanoyl]-L-prolyl]amino)methyl]phenyl]acetic acid
Homo sapiens
-
0.000069
[7-[(3R)-3-amino-4-(2,5-difluorophenyl)butanoyl]-5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyrazin-3-yl]methanol
Rattus norvegicus
-
-
additional information
alogliptin
Homo sapiens
-
50% inhibition of DPP-4 activity is observed at an alogliptin plasma concentration of 3.7 ng/ml
0.000039
(1S)-1-cyclohexyl-2-(3,3-difluoropyrrolidin-1-yl)-2-oxoethanamine
Homo sapiens
-
pH 8.0, 37°C
0.000073
(1S)-1-cyclohexyl-2-(3,3-difluoropyrrolidin-1-yl)-2-oxoethanamine
Homo sapiens
-
pH 8.0, 37°C
0.00000027
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
0.00027
(2R)-1-(2,5-difluorophenyl)-4-oxo-4-(1,3-thiazolidin-3-yl)butan-2-amine
Homo sapiens
-
-
0.000098
(2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Homo sapiens
-
-
0.000098
(2R)-1-(2-fluorophenyl)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]butan-2-amine
Rattus norvegicus
-
-
0.000018
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.000018
(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
determination of the pharmacokinetic profile
0.000011
(2R)-4-[(8R)-8-[(1-fluorocyclopropyl)methyl]-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
single diastereoisomer, configuration at F unknown
0.000018
(2R)-4-[(8R)-8-[(1-fluorocyclopropyl)methyl]-2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
single diastereoisomer, configuration at F unknown
0.000045
(2R)-4-[1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Homo sapiens
-
-
0.000045
(2R)-4-[1,4-dimethyl-2-(trifluoromethyl)-1,4,6,7-tetrahydro-5H-imidazo[4,5-c]pyridin-5-yl]-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
Rattus norvegicus
-
-
0.00000054
(2S)-1-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-1-oxopropan-2-aminium
Homo sapiens
-
pH 2
0.0014
(2S)-1-[(2R)-2-(dihydroxyboranyl)pyrrolidin-1-yl]-1-oxopropan-2-aminium
Homo sapiens
-
pH 8
0.00002
(2S)-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.00002
(2S)-1-[(2S)-pyrrolidin-2-ylcarbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000049
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000071
(2S)-1-[[(2S,4R)-4-(3-hydroxy-2-methoxy-6-methylphenyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000035
(2S)-1-[[(2S,4S)-4-allylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.000038
(2S)-1-[[(2S,4S)-4-allylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000034
(2S)-1-[[(2S,4S)-4-propylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
-
0.00005
(2S)-1-[[(2S,4S)-4-propylpyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
37°C, pH 7.4
0.0000033
(2S)-1-[[(3R,4R)-4-amino-1-(3-cyano-4-fluorobenzyl)pyrrolidin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
0.0000036
(2S)-1-[[(3R,4R)-4-amino-1-(3-cyano-4-fluorobenzyl)pyrrolidin-3-yl]carbonyl]pyrrolidine-2-carbonitrile
Homo sapiens
-
0.000000012
(2S)-2-[4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]propanoic acid
Homo sapiens
-
0.000000081
(2S)-2-[4-[([1-[(3S)-3-amino-4-(2-fluorophenyl)butanoyl]-L-prolyl]amino)methyl]phenoxy]propanoic acid
Homo sapiens
-
0.00044
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
Homo sapiens
0% human serum
0.00347
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
Homo sapiens
50% human serum
0.000027
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl](methyl)amino]cyclohexyl)-1-oxobutan-2-aminium
Homo sapiens
0% human serum
0.000097
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl](methyl)amino]cyclohexyl)-1-oxobutan-2-aminium
Homo sapiens
50% human serum
0.000074
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl]amino]cyclohexyl)-1-oxobutan-2-aminium
Homo sapiens
0% human serum
0.00021
(2S,3S)-1-[(3S)-3-fluoropyrrolidin-1-yl]-3-(4-[[(4-methoxyphenyl)carbonyl]amino]cyclohexyl)-1-oxobutan-2-aminium
Homo sapiens
50% human serum
0.000000065
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.000064
(2S,3S)-3-(4'-fluorobiphenyl-4-yl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
-
0.00000025
(2S,3S)-3-(4-bromophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
0.000245
(2S,3S)-3-(4-bromophenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-amine
Homo sapiens
-
-
0.00046
(2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Homo sapiens
0% human serum
0.00149
(2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Homo sapiens
50% human serum
0.00033
(2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
Homo sapiens
0% human serum
0.00051
(2S,3S)-3-(4-[[(2,4-difluorophenyl)sulfonyl]amino]cyclohexyl)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
Homo sapiens
50% human serum
0.00016
(2S,3S)-3-(4-[[(4-fluorophenyl)carbonyl](methyl)amino]phenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Homo sapiens
-
0.0003
(2S,3S)-3-(4-[[(4-fluorophenyl)carbonyl](methyl)amino]phenyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Homo sapiens
-
0.000022
(2S,3S)-3-[4-[(cyclopropylcarbonyl)(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Homo sapiens
0% human serum
0.000047
(2S,3S)-3-[4-[(cyclopropylcarbonyl)(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Homo sapiens
50% human serum
0.000016
(2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Homo sapiens
0% human serum
0.00004
(2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-1-[(3S)-3-fluoropyrrolidin-1-yl]-1-oxobutan-2-aminium
Homo sapiens
50% human serum
0.000029
(2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
Homo sapiens
0% human serum
0.00019
(2S,3S)-3-[4-[acetyl(methyl)amino]cyclohexyl]-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
Homo sapiens
50% human serum
0.00036
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
Homo sapiens
0% human serum
0.00128
(2S,3S)-4-(dimethylamino)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxo-3-[4-([[4-(trifluoromethoxy)phenyl]sulfonyl]amino)cyclohexyl]butan-2-aminium
Homo sapiens
50% human serum
0.000022
(2S,3S)-4-(dimethylamino)-3-(4-[[(3-fluorophenyl)carbonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
Homo sapiens
0% human serum
0.000024
(2S,3S)-4-(dimethylamino)-3-(4-[[(3-fluorophenyl)carbonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
Homo sapiens
0% human serum
0.000092
(2S,3S)-4-(dimethylamino)-3-(4-[[(3-fluorophenyl)carbonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
Homo sapiens
50% human serum
0.0002
(2S,3S)-4-(dimethylamino)-3-(4-[[(3-fluorophenyl)carbonyl]amino]cyclohexyl)-1-[(3S)-3-fluoropyrrolidin-1-yl]-1,4-dioxobutan-2-aminium
Homo sapiens
50% human serum
0.000004
(2S,3S,11bS)-3-(3-chlorophenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.0000042
(2S,3S,11bS)-3-(3-chlorophenyl)-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.000004
(2S,3S,11bS)-9,10-dimethoxy-3-(3-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.0000046
(2S,3S,11bS)-9,10-dimethoxy-3-(3-methylphenyl)-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-amine
Homo sapiens
-
-
0.00001
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
Homo sapiens
-
-
0.00001
(2S,3S,5S)-5-[[(2S)-2-cyanopyrrolidin-1-yl]carbonyl]-N,N,2-trimethylpyrrolidine-3-carboxamide
Homo sapiens
-
37°C, pH 7.4
0.000121
(3'S,5'S)-5'-(1,3-thiazolidin-3-ylcarbonyl)-1,3'-bipyrrolidine
Rattus norvegicus
-
-
0.000127
(3'S,5'S)-5'-(1,3-thiazolidin-3-ylcarbonyl)-1,3'-bipyrrolidine
Homo sapiens
-
-
0.0000042
(3R)-1-[(1R)-1-(dihydroxyboranyl)ethyl]-2-oxopyrrolidin-3-aminium
Homo sapiens
-
pH 8
0.0000053
(3R)-1-[(1R)-1-(dihydroxyboranyl)ethyl]-2-oxopyrrolidin-3-aminium
Homo sapiens
-
pH 2
0.0000012
(3R,4R)-1-(2-oxo-2H-pyrimido[1,2-b]pyridazin-7-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
pharmacokinetic properties
0.000002
(3R,4R)-1-(2-oxo-2H-pyrimido[1,2-b]pyridazin-7-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-aminium
Homo sapiens
-
-
0.00002
(3R,4S)-1-(6-phenylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
0.000021
(3R,4S)-1-(6-phenylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.000014
(3R,4S)-1-[6-(3-nitrophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.00012
(3R,4S)-1-[6-(3-nitrophenyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
-
0.000006
(3R,4S)-1-[6-(3-thienyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
0.000017
(3R,4S)-1-[6-(3-thienyl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)pyrrolidin-3-amine
Homo sapiens
-
0.00046
(3S)-1-[(1R)-1-(dihydroxyboranyl)ethyl]-2-oxopyrrolidin-3-aminium
Homo sapiens
-
pH 8
0.00048
(3S)-1-[(1R)-1-(dihydroxyboranyl)ethyl]-2-oxopyrrolidin-3-aminium
Homo sapiens
-
pH 2
0.0186
(3S,4R)-3-butyl-1-cyclohexylpiperidin-4-amine
Homo sapiens
-
-
0.0452
(3S,4R)-3-butyl-1-cyclohexylpiperidin-4-amine
Homo sapiens
-
-
0.0000551
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.0000551
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.000021
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.000021
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.000171
(3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.000171
(3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.00019
(3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Rattus norvegicus
-
-
0.00019
(3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
Homo sapiens
-
0.0000016
(4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]phenyl)ethynamine
Homo sapiens
-
-
0.0000022
(4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]phenyl)ethynamine
Rattus norvegicus
-
-
0.0000041
1-(2-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000072
1-(2-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000042
1-(3,4-dichlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000072
1-(3,4-dichlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000087
1-(3-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000103
1-(3-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000108
1-(4-bromophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000109
1-(4-bromophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000122
1-(4-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000175
1-(4-chlorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000762
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
Rattus norvegicus
-
-
0.0000762
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
Homo sapiens
-
0.000001
1-(4-ethynylpyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000014
1-(4-ethynylpyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000135
1-(4-fluorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000169
1-(4-fluorophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000109
1-(4-methoxyphenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000176
1-(4-methoxyphenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000029
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,4-diazepane
Homo sapiens
-
-
0.0000029
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,4-diazepane
Rattus norvegicus
-
-
0.0000082
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.000009
1-(4-nitrophenyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000025
1-(5-chloropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000031
1-(5-chloropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.00000092
1-(5-nitropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000011
1-(5-nitropyridin-2-yl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.000021
1-(diphenylmethyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000314
1-(diphenylmethyl)-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000305
1-benzyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000383
1-benzyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000575
1-methyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000811
1-methyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.000151
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
Rattus norvegicus
-
-
0.000151
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
Homo sapiens
-
0.0000109
1-phenyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000176
1-phenyl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000027
1-pyridin-2-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000035
1-pyridin-2-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.0000031
1-pyridin-4-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Homo sapiens
-
-
0.0000039
1-pyridin-4-yl-4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazine
Rattus norvegicus
-
-
0.000022
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
Rattus norvegicus
-
-
0.0078
1-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]piperidin-2-one
Rattus norvegicus
-
-
0.0000998
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
Rattus norvegicus
-
-
0.0000998
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
Homo sapiens
-
0.0000047
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)phenyl]piperazine
Rattus norvegicus
-
-
0.0000072
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[4-(trifluoromethyl)phenyl]piperazine
Homo sapiens
-
-
0.0000015
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
Homo sapiens
-
-
0.0000018
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-4-[5-(trifluoromethyl)pyridin-2-yl]piperazine
Rattus norvegicus
-
-
0.0000476
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Homo sapiens
-
-
0.0000744
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Rattus norvegicus
-
-
0.000011
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.000017
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in absence of plasma
0.000024
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in presence of 18% plasma
0.00045
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
Homo sapiens
-
-
0.000002
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in absence of plasma
0.000002
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
Homo sapiens
-
potent and selective DPPIV inhibitor, but it showed a significant loss of activity in the presence of plasma
0.0006
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
Rattus norvegicus
in presence of 18% plasma
0.000002
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
Homo sapiens
-
-
0.000003
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
Rattus norvegicus
in absence of plasma
0.000007
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
Rattus norvegicus
in presence of 18% plasma
0.000012
1-[[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-2-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[1,5-a]pyrazin-8-yl]methyl]cyclopropanol
Homo sapiens
-
single diastereoisomer, configuration at OH unknown
0.000014
1-[[(8R)-7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-2-(trifluoromethyl)-5,6,7,8-tetrahydro[1,2,4]triazolo[1,5-a]pyrazin-8-yl]methyl]cyclopropanol
Homo sapiens
-
single diastereoisomer, configuration at OH unknown
0.0000058
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)-1,3-benzoxazole
Homo sapiens
-
0.0000074
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)-1,3-benzoxazole
Homo sapiens
-
0.0000082
2-(4-[(3R,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]piperazin-1-yl)-1,3-benzoxazole
Homo sapiens
-
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-bromo-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Homo sapiens
-
-
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-bromo-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000004
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Homo sapiens
-
-
0.000004
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
2-([2-[(3R)-3-aminopiperidin-1-yl]-6-fluoro-4-oxoquinazolin-3(4H)-yl]methyl)benzonitrile
Homo sapiens
-
-
0.0000195
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000195
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Homo sapiens
-
0.000039
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.000039
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Homo sapiens
-
0.0000165
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
Rattus norvegicus
-
-
0.0000165
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
Homo sapiens
-
0.00009
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
Rattus norvegicus
-
-
0.000098
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-(4-sulfamoylphenyl)acetamide
Rattus norvegicus
-
-
0.000217
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
Rattus norvegicus
-
-
0.000236
2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]-N-cyclopropylacetamide
Rattus norvegicus
-
-
0.0000012
2-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
Homo sapiens
-
-
0.0000012
2-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
Rattus norvegicus
-
-
0.000019
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
Homo sapiens
-
-
0.000027
3-([2-[(2S,4S)-2-cyano-4-fluoropyrrolidin-1-yl]-2-oxoethyl]amino)-N-(3,4-dimethoxyphenyl)-3-methylbutanamide
Homo sapiens
-
-
0.0001
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
Mus musculus
-
recombinant enzyme
0.0001
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
Homo sapiens
-
plasma enzyme
0.00013
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
Homo sapiens
-
recombinant enzyme
0.00028
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
Mus musculus
-
plasma enzyme
0.00036
3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate
Canis lupus familiaris
-
plasma enzyme
0.000538
3-[(2S)-pyrrolidin-2-ylcarbonyl]-1,3-thiazolidine
Homo sapiens
-
-
0.000607
3-[(2S)-pyrrolidin-2-ylcarbonyl]-1,3-thiazolidine
Rattus norvegicus
-
-
0.0000029
3-[1-amino-2-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]-5,7-dimethyltricyclo[3.3.1.13,7]decan-1-ol
Homo sapiens
-
-
0.000607
3-[1-amino-2-[(1S,5R)-2-azabicyclo[3.1.0]hex-2-yl]-2-oxoethyl]-5,7-dimethyltricyclo[3.3.1.13,7]decan-1-ol
Homo sapiens
-
-
0.0000018
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
Homo sapiens
-
0.000005
3-[6-[(3R,4S)-3-amino-4-(2,4,5-trifluorophenyl)pyrrolidin-1-yl]pyrimidin-4-yl]benzoic acid
Homo sapiens
-
-
0.0000001
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-carboxamide
Homo sapiens
-
0.0001
4'-[(1S,2S)-2-amino-3-[(3S)-3-fluoropyrrolidin-1-yl]-1-methyl-3-oxopropyl]biphenyl-3-carboxamide
Homo sapiens
-
-
0.0000093
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
Rattus norvegicus
-
-
0.0000093
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
Homo sapiens
-
0.0000033
4-(4-nitrophenyl)-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Homo sapiens
-
-
0.0000033
4-(4-nitrophenyl)-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Rattus norvegicus
-
-
0.0000125
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.0000125
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Homo sapiens
-
0.000005
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.000005
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Homo sapiens
-
0.0000136
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.0000136
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Homo sapiens
-
0.0000343
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Rattus norvegicus
-
-
0.0000343
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
Homo sapiens
-
0.000168
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Rattus norvegicus
-
-
0.000168
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Homo sapiens
-
0.0000341
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Rattus norvegicus
-
-
0.0000341
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Homo sapiens
-
0.00021
4-nitrobenzyl[(5S)-5-amino-6-oxo-6-(1-pyrrolidinyl)hexyl]carbamate
Homo sapiens
-
-
0.214
4-nitrobenzyl[(5S)-5-amino-6-oxo-6-(1-pyrrolidinyl)hexyl]carbamate
Homo sapiens
-
recombinant enzyme
0.0000096
4-phenyl-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Homo sapiens
-
-
0.0000096
4-phenyl-1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperidine
Rattus norvegicus
-
-
0.000084
4-[(3R)-3-[[2-(4-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide
Homo sapiens
-
-
0.000084
4-[(3R)-3-[[2-(4-fluorophenyl)-2-oxoethyl]amino]butyl]benzamide
Homo sapiens
-
0.0000139
4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]morpholine
Homo sapiens
-
-
0.0000189
4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]morpholine
Rattus norvegicus
-
-
0.0000018
4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]benzene-1,2-dicarbonitrile
Homo sapiens
-
-
0.0000018
4-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]benzene-1,2-dicarbonitrile
Rattus norvegicus
-
-
0.0000336
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
Rattus norvegicus
-
-
0.0000336
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
Homo sapiens
-
0.000009
5-(aminomethyl)-6-(2,4-dichlorophenyl)-N2-(2-methoxyethyl)-N2-methylpyrimidine-2,4-diamine
Homo sapiens
-
-
0.000009
5-(aminomethyl)-6-(2,4-dichlorophenyl)-N2-(2-methoxyethyl)-N2-methylpyrimidine-2,4-diamine
Homo sapiens
-
pH 8.0, 37°C
0.0000107
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000107
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Homo sapiens
-
0.0000134
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000134
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Homo sapiens
-
0.0000101
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000101
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Homo sapiens
-
0.0000061
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000061
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Homo sapiens
-
0.0000103
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Rattus norvegicus
-
-
0.0000103
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
Homo sapiens
-
0.0000016
6-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
Homo sapiens
-
-
0.0000019
6-[4-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]piperazin-1-yl]nicotinonitrile
Rattus norvegicus
-
-
0.00014
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
Homo sapiens
-
i.e. KR-62436, IC50: 0.00014 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1
0.00049
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
Sus scrofa
-
i.e. KR-62436, IC50: 0.00049 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1
0.00078
6-{2-[2-(5-cyano-4,5-dihydropyrazol-1-yl)-2-oxoethylamino]ethylamino}nicotinonitrile
Rattus norvegicus
-
i.e. KR-62436, IC50: 0.00078 mM, selective competitive inhibitor, good lead compound for further development as a new anti-diabetic agent, almost completely inhibits DPP-IV mediated degradation of glucagon-like peptide-1
0.000007
6-{[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)ethyl]amino}pyridine-3-carbonitrile
Homo sapiens
-
enzyme isolated from blood plasma
0.000022
6-{[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)ethyl]amino}pyridine-3-carbonitrile
Homo sapiens
-
enzyme isolated from Caco-2 cells
0.0000069
alogliptin
Homo sapiens
-
-
0.000007
alogliptin
Homo sapiens
-
-
0.000024
alogliptin
Homo sapiens
-
in 100 mM Tris-HCl, 100 mM NaCl, pH 7.8
0.00000236
ASP-8497
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.00000386
ASP-8497
Mus musculus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.0000053
ASP-8497
Homo sapiens
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.00000553
ASP-8497
Canis lupus familiaris
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.0000026
ASP8497
Mus musculus
-
median inhibition concentration, in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% bovine serum albumin, at pH 7.3 and 25°C
0.0000053
ASP8497
Homo sapiens
-
-
0.0000062
ASP8497
Homo sapiens
-
median inhibition concentration, in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% bovine serum albumin, at pH 7.3 and 25°C
0.0000073
ASP8497
Canis lupus familiaris
-
median inhibition concentration, in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% bovine serum albumin, at pH 7.3 and 25°C
0.000001
BI 1356
Homo sapiens
-
-
0.000001
BI 1356
Homo sapiens
-
in 100 mM Tris-HCl, 100 mM NaCl, pH 7.8
0.0000153
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
Rattus norvegicus
-
-
0.0000153
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
Homo sapiens
-
0.0000016
L-Val-L-boroPro
Homo sapiens
-
pH 2
0.0012
L-Val-L-boroPro
Homo sapiens
-
pH 8
0.029
metformin
Mus musculus
-
ob/ob diabetic mice
0.038
metformin
Mus musculus
-
normal mice
0.000119
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000124
N-(2-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000023
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
Rattus norvegicus
-
-
0.000023
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
Homo sapiens
-
0.000088
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00012
N-(5-chloropyridin-3-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00011
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.00013
N-(5-cyanopyridin-2-yl)-2-[4-(1-[2-[(4R)-4-cyano-1,3-thiazolidin-3-yl]-2-oxoethyl]hydrazinyl)piperidin-1-yl]acetamide
Rattus norvegicus
-
-
0.000008
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
Homo sapiens
-
-
0.000008
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
Rattus norvegicus
-
-
0.0000026
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
Rattus norvegicus
-
-
0.0000093
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
Rattus norvegicus
-
-
0.000013
N-[(2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-3-yl]-3-methylbutanamide
Rattus norvegicus
-
-
0.000236
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Rattus norvegicus
-
-
0.000236
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
Homo sapiens
-
0.0000006
saxagliptin
Homo sapiens
-
-
0.00000171
saxagliptin
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.00000257
saxagliptin
Mus musculus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.00000337
saxagliptin
Homo sapiens
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.00000422
saxagliptin
Canis lupus familiaris
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.00003
saxagliptin
Homo sapiens
-
-
0.00005
saxagliptin
Homo sapiens
-
in 100 mM Tris-HCl, 100 mM NaCl, pH 7.8
0.00000996
sitagliptin
Homo sapiens
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.0000108
sitagliptin
Canis lupus familiaris
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.0000115
sitagliptin
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.0000121
sitagliptin
Homo sapiens
-
-
0.000018
sitagliptin
Homo sapiens
-
-
0.000018
sitagliptin
Rattus norvegicus
-
-
0.000018
sitagliptin
Homo sapiens
-
0.000019
sitagliptin
Homo sapiens
-
in 100 mM Tris-HCl, 100 mM NaCl, pH 7.8
0.0000213
sitagliptin
Mus musculus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.00003
sitagliptin
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000087
sitagliptin
Homo sapiens
-
0.00000167
vildagliptin
Rattus norvegicus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.0000027
vildagliptin
Homo sapiens
-
enzyme isolated from blood plasma
0.00000324
vildagliptin
Mus musculus
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.00000347
vildagliptin
Canis lupus familiaris
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.0000035
vildagliptin
Homo sapiens
-
enzyme isolated from Caco-2 cells
0.00000528
vildagliptin
Homo sapiens
-
in 25 mM HEPES, 140 mM NaCl, 80 mM MgCl2, 0.5% BSA, pH 7, at 25°C
0.0000166
vildagliptin
Homo sapiens
-
in 25 mM HEPES,140 mM NaCl, 1% bovine serum albumin, 80 mM MgCl2, at 25°C
0.0000238
vildagliptin
Homo sapiens
-
-
0.000051
vildagliptin
Rattus norvegicus
-
in 25 mM tris(hydroxymethyl)-aminomethane HCl (pH 7.4), 140 mM NaCl, 10 mM KCl, and 0.1% bovine serum albumin
0.000062
vildagliptin
Homo sapiens
-
in 100 mM Tris-HCl, 100 mM NaCl, pH 7.8
0.000068
[(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.00143
[(2R)-1-[N-(methylsulfonyl)glycyl]pyrrolidin-2-yl]boronic acid
Homo sapiens
-
23°C, pH 7.4
0.0000163
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
Rattus norvegicus
-
-
0.0000163
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
Homo sapiens
-
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