Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
((S)-1-[1-[4(R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxoazepan-1-yl]methanoyl]-3-methylbutl)carbamic acid benzyl ester
-
the faster eluting diastereomer C34H46N4O7*0.4H2O; the slower eluting diastereomer C34H46N4O7*0.3H2O
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxopiperidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-4-oxopyrrolidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylmethylamino-4-methylpentanoylamino)-4-oxopyrrolidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
(1'S)-7-(1-aminoethyl)-2-(2-methoxyphenyl)pyrazolo[1,5-a] pyrimidine hydrochloride
-
(1'S)-7-(1-aminoethyl)-2-(3-trifluoromethylphenyl)pyrazolo-[1,5-a]pyrimidine hydrochloride
-
(1'S)-7-(1-aminoethyl)-2-benzyl-3-phenylpyrazolo[1,5-a]pyrimidine hydrochloride
-
(1'S)-7-(1-aminoethyl)-2-phenylpyrazolo[1,5-a]pyrimidine hydrochloride
-
(1'S)-7-(1-aminoethyl)pyrazolo[1,5-a]pyrimidine-3-(N-methylcarboxamide) hydrochloride
-
(1'S)-7-(1-aminoethyl)pyrazolo[1,5-a]pyrimidine-3-carboxylate hydrochloride
-
(11R,12R)-14,14-difluoro-34-(methylsulfanyl)-N-(prop-2-yn-1-yl)-11,12,13,14,15,16-hexahydro[11,21:22,31-terphenyl]-12-carboxamide
-
(1R)-1-benzyl-2-methylpropyl [(1S)-1-formylpentyl]carbamate
-
-
(1R)-1-benzyl-2-methylpropyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
(1R,2R)-5,5-dichloro-2-[4-[4-(methanesulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrrol-3-yl]-N-(prop-2-yn-1-yl)cyclohexane-1-carboxamide
-
(1R,2R)-5,5-dichloro-N-(1-cyanocyclopropyl)-2-[4-[4-(methylsulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
i.e. MK-1256, a nonbasic, nitrile-containing cathepsin K inhibitor, that shows high selectivity for Cat K, 1100fold versus Cat B, L, S, C, H, Z, and V, 110fold versus Cat F
(1R,2R)-5,5-difluoro-2-[4-[4-(methanesulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrrol-3-yl]-N-(prop-2-yn-1-yl)cyclohexane-1-carboxamide
-
(1R,2R)-N-(1-cyanocyclopropyl)-2-(6-methoxy-1,3,4,5-tetrahydro-2H-pyrido[4,3-b]indole-2-carbonyl)cyclohexane-1-carboxamide
-
(1R,2R)-N-(1-cyanocyclopropyl)-5,5-difluoro-2-[4-[4-(methylsulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfonyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4-[4-(methylsulfonyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
(1R,2S)-N-(cyanomethyl)-2-[2-[4-(methylsulfanyl)phenyl]ethyl]cyclohexanecarboxamide
-
-
(1S)-1-methyl-2-phenylethyl [(1S)-1-formylpentyl]carbamate
-
-
(1S)-1-methyl-2-phenylethyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
(1S)-1-[(5,6-dichloro-1H-benzimidazol-1-yl)methyl]-2,2-dimethylpropyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-1-[(5,6-dichloro-1H-benzimidazol-1-yl)methyl]-2,2-dimethylpropyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-([[(6-fluoropyridin-2-yl)carbonyl]amino]acetyl)pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(morpholin-4-ylcarbonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[(3-pyridin-3-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[(3-pyridin-4-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[[3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]propyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
-
-
(1S)-2,2-dimethyl-1-[[3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
-
-
(2E,4E)-5-(1-hydroxy-2,6,6-trimethyl-4-oxocyclohex-2-en-1-yl)-3-methylpenta-2,4-dienoic acid
-
(2R)-2-[3'-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
-
(2R)-3,3-dimethyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)butan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[2-oxo-3-[4-(trifluoromethyl)phenyl]imidazolidin-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1,3-thiazol-2-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-3,3-dimethyl-1-[4-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]butan-2-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(2R)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((R)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2R)-N-(cyanomethyl)-2-[3'-(2-[[3-(dimethylamino)pyrrolidin-1-yl]methyl]-1,3-thiazol-4-yl)biphenyl-3-yl]-4-methylpentanamide
-
-
(2R)-N-(cyanomethyl)-4-methyl-2-[3'-[2-(piperazin-1-ylmethyl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
-
-
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)biphenyl-3-yl]pentanamide
-
-
(2R)-N-cyano-4-methyl-2-[4'-(piperazin-1-yl)[1,1'-biphenyl]-3-yl]pentanamide
-
(2S)-1-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-3,3-dimethylbutan-2-yl [(3S)-1,2-dioxo-1-[(pyridin-3-ylmethyl)amino]heptan-3-yl]carbamate
-
-
(2S)-1-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-3,3-dimethylbutan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2S)-2-(biphenyl-2-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
-
(2S)-2-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
-
(2S)-2-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
-
-
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
-
-
(2S)-3,3-dimethyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)butan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2S)-3,3-dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]butan-2-yl [(3S)-1,2-dioxo-1-[(2-oxo-1,3-oxazolidin-3-yl)amino]heptan-3-yl]carbamate
-
-
(2S)-3-methyl-1-(5-phenyl-1,3,4-oxadiazol-2-yl)butan-2-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(2S)-4,4-dichloro-N-(1-cyanocyclopropyl)-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
-
-
(2S)-4-fluoro-4-methyl-N-(1-(2-(methylsulfonyl)phenyl)-3-oxopiperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(1-(methylsulfonyl)-3-oxoazepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(1-(methylsulfonyl)-4-oxopyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
racemate
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)piperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-phenylpiperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(3-oxoazepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(4-oxo-1-(pyridin-2-ylsulfonyl)pyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-4-fluoro-4-methyl-N-(4-oxopyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-(benzylsulfonyl)-3-oxoazepan-4-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-acetyl-4-oxopyrrolidin-3-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-benzoyl-4-oxopyrrolidin-3-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(2S)-N-(1-cyanocyclopropyl)-4,4,4-trifluoro-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
-
-
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(3-phenoxyphenoxy)pentanamide
-
-
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(4-phenoxyphenoxy)pentanamide
-
-
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-phenoxypentanamide
-
-
(2S,3S)-3-([(1S)-3-methyl-1-[(2-methylpropoxy)methyl]butyl]carbamoyl)oxirane-2-carboxylate
-
through screening, a potent orally active cathepsin K inhibitor named NC-2300 is obtained, which suppresses autoimmune inflammation of the joints as well as osteoclastic bone resorption in an adjuvant-induced arthritis animal model in rats. Computer-assisted simulation of the cathepsin K/NC-2300 complex indicates that NC-2300 blocks the active-site cleft where Cys25 and His162 of cathepsin K form the catalytic site. Pharmacological inhibition of cathepsin K results in defective Toll-like receptor 9 signaling in dendritic cells in response to unmethylated CpG DNA, which in turn leads to an attenuated induction of T helper 17 cells, without affecting the antigen-presenting ability of dendritic cells
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
(3S)-1-(1H-indol-6-ylcarbonyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(2,2-dimethylpropoxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(benzylcarbamoyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(benzylsulfonyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(biphenyl-4-ylcarbonyl)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(dicyclopentylmethoxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-(heptan-4-yloxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-([(2R)-1-[5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl]-3,3-dimethylbutan-2-yl]oxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(3S)-2-oxopiperidin-3-yl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-([(3S)-1-[(3,5-dimethyl-1,2-oxazol-4-yl)carbonyl]-4,4-dimethylpyrrolidin-3-yl]oxy)-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-benzyl-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-tert-butoxy-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[(thiophen-2-ylmethyl)amino]heptan-3-yl]carbamate
-
-
(3S)-1-tert-butoxy-4,4-dimethylpyrrolidin-3-yl [(3S)-1-(ethylamino)-1,2-dioxoheptan-3-yl]carbamate
-
-
(3S)-1-[(1-benzylcyclobutyl)methoxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[(2,4-dimethylpentan-3-yl)oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[(3,3-dimethylbutan-2-yl)oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(2R)-3,3-dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]butan-2-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(3S)-1-[[(2R)-3,3-dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]butan-2-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3R)-2,2-dimethyl-6-phenylhexan-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3R)-4,4-dimethyl-1-phenylpentan-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3S)-1-(1-benzothiophen-2-ylcarbonyl)-4,4-dimethylpyrrolidin-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3S)-1-benzoyl-4,4-dimethylpyrrolidin-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[(3S)-4,4-dimethyl-1-phenylpentan-3-yl]oxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-1-[[1-(4-fluorobenzyl)cyclobutyl]methoxy]-4,4-dimethylpyrrolidin-3-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-5-ylamino)heptan-3-yl]carbamate
-
-
(3S)-2-oxo-N-[(1R)-1-phenylethyl]-3-[([[1-(2-phenylethyl)cyclobutyl]oxy]acetyl)amino]heptanamide
-
-
(3S)-2-oxo-N-[(1R)-1-phenylethyl]-3-[([[1-(3-phenylpropyl)cyclobutyl]oxy]acetyl)amino]heptanamide
-
-
(3S)-3-([[(2-methyl-1-phenylpropan-2-yl)oxy]acetyl]amino)-2-oxo-N-[(1R)-1-phenylethyl]heptanamide
-
-
(3S)-4,4-dimethyl-1-(1,2-oxazol-5-ylcarbonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(4-phenylbutanoyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(naphthalen-2-ylcarbonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(pentan-3-yloxy)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(phenylacetyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(phenylcarbamoyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(phenylsulfonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-(pyridin-3-ylcarbonyl)pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-[(2,2,4,4-tetramethylpentan-3-yl)oxy]pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-[(2-phenylethyl)carbamoyl]pyrrolidin-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
(3S)-4,4-dimethyl-1-[4-(trifluoromethyl)benzoyl]pyrrolidin-3-yl [(3S)-1,2-dioxo-1-(1H-pyrazol-3-ylamino)heptan-3-yl]carbamate
-
-
(4-[[(2S)-2-([1-[([1,1'-biphenyl]-3-yl)amino]cyclohexane-1-carbonyl]amino)butyl]amino]phenoxy)acetic acid
-
(4R)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
(4S)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
(S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
-
-
(S,S)-piperidine-4-carboxylic acid [1-[1-(benzoxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
1,3-bis(CBZ-Leu-NH)-2-propanone
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[(1-[4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamido]cyclohexane-1-carbonyl)amino]-L-erythro-hex-2-ulose
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,5-(N-benzyloxycarbonylleucyl)carbohydrazide
-
1,6-dimethyl-1,2-dihydrophenanthro[1,2-b]furan-10,11-dione
-
1-(3-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-cyanophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
-
-
1-(4-cyclohexylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(4-ethylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-2-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1R)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]butyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]pentyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-4-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
-
-
1-(N-benzyloxycarbonyl-leucyl)-5-(N-Boc-phenylalanylleucyl)carbohydrazide
-
cathepsin K inhibitor
1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
-
1-(phenoxymethyl)cyclobutyl (3aR,6aS)-6-oxohexahydro-1H-furo[3,2-c]pyrazole-1-carboxylate
-
1-(phenoxymethyl)cyclobutyl (3aS,6aR)-3-oxohexahydro-4H-furo[3,2-b]pyrrole-4-carboxylate
-
1-benzylcyclopentyl [(1S)-1-formylpentyl]carbamate
-
-
1-benzylcyclopentyl [(1S)-1-[(E)-[(2,3-dihydro-1H-indol-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
1-benzylcyclopentyl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
1-cyano-3-azetidinyl cyclohexylmethyl ether
-
IC 50: 20 nM
1-ethyl-2-[(4-methylpiperazin-1-yl)methyl]-6-[3-(trifluoromethyl)phenyl]-2,3-dihydro-1H-indole-4-carbonitrile
-
1-Isopropyl-2-methylpropyl (1S)-1-cyclohexylmethyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 14 nM
1-Isopropyl-2-methylpropyl (1S)-1-isoprpyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 47 nM
1-Isopropyl-2-methylpropyl (1S)-1-methyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 360 nM
1-Isopropyl-2-methylpropyl (1S)-1-[(isoxazol-3-ylamino)(oxo)acetyl]pentylcarbamate
-
IC50: 5.1 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1,3,4-thiadiazol-2-ylamino)acetyl]pentylcarbamate
-
IC50: 83 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1,3-thiazol-2-ylamino)acetyl]pentylcarbamate
-
IC50: 40 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(isoquinolin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 4.8 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyrazin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 52 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyridin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 32 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyridin-3-ylamino)acetyl]pentylcarbamate
-
IC50: 95 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(quinolin-2-ylamino)acetyl]pentylcarbamate
-
IC50: 250 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]pentylcarbamate
-
IC50: 9.2 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[(3-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.71 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-bromo-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.24 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-cyano-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.91 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-fluoro-1H-indazol-3-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.26 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
1-Isopropyl-2-methylpropyl (1S)-2,3-dioxo--1-phenyl-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 27 nM
1-Isopropyl-2-methylpropyl (1S)-3-methyl-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]butylcarbamate
-
IC50: 24 nM
1-Isopropyl-2-methylpropyl (1S,2S)-2-methyl-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]butylcarbamate
-
IC50: 87 nM
1-Isopropyl-2-methylpropyl 2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
-
IC50: 0.012 mM
1-methylethyl (2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazinecarboxylate
-
-
1-[(1H-imidazol-4-yl)methyl]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole
-
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-(3-methylphenyl)urea
-
-
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-phenylurea
-
-
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-[3-(trifluoromethyl)phenyl]urea
-
-
13-methyl-2H,10H-[1,3]benzodioxolo[5,6-c][1,3]dioxolo[4,5-i]phenanthridin-13-ium
-
2,2'-N,N'-bis(benzyloxycarbonyl)-L-leucinylcarbohydrazide
-
-
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-6-[5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl]-2,3-dihydro-4H-1-benzopyran-4-one
-
2-(3-methoxyphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(3-methylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(3-tert-butylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxoazepan-1-ylsulfonyl)pyridine 1-oxide
-
-
2-(biphenyl-3-yl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-(cyclohexylamino)pyrimidine-4-carbonitrile
-
-
2-(cyclohexylmethyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-amino-4-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
2-cyano-4-(cyclohexylamino)-N-(4-methoxyphenethyl)-pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-(3-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-(4-pyrrolidin-1-ylphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[3-[2-(1H-imidazol-1-yl)ethoxy]-4-methoxyphenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[3-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[(1-methylpiperidin-4-yl)oxy]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(3-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-pyrrolidin-1-ylphenyl)ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[3-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
-
-
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(4-methoxyphenethyl)-4-(neopentylamino)pyrimidine-5-carboxamide
-
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cycloheptyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cycloheptyl-3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cycloheptyl-4-[2-(dimethylamino)ethyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cycloheptyl-4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cyclohexyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-cyclopentyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-methyl-1-phenylpropan-2-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
2-methylpropyl [(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
2-phenylethyl (4S)-4-[[(4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidin-1-yl]oxy]-3,3-dimethylpyrrolidine-1-carboxylate
-
-
2-phenylpropan-2-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
2-[3-(hydroxymethyl)phenyl]-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
2-[[2-cyano-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methyl]-N-cyclohexyl-1,3-dioxo-2,8-diazaspiro[4.5]decane-8-carboxamide
-
-
2-[[2-cyano-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methyl]-N-methyl-1,3-dioxo-2,8-diazaspiro[4.5]decane-8-carboxamide
-
-
3,3'-[(3-carboxy-4-oxocyclohexa-2,5-dien-1-ylidene)methylene]bis(6-hydroxybenzoic acid)
-
3,5-dioxo-2-phenyl-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-2-[3-(propan-2-yl)phenyl]-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-(2-phenylethyl)-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-phenyl-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-propyl-2-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-[2-(piperidin-1-yl)ethyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(propan-2-yl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-2-oxopropylcarbamate
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxo-N-(phenylsulfonyl)pyrrolidine-1-carboxamide
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxo-N-phenylpyrrolidine-1-carboxamide
-
-
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxamide
-
-
3-(4-([4'-((1-[(cyanomethyl)carbamoyl]cyclohexyl)carbamoyl)biphenyl-4-yl]oxy)piperidin-1-yl)propanoic acid
-
-
3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoic acid
-
-
3-(benzyloxy)-1-cyanoazetidine
-
IC 50: 40 nM
3-(cyclohexylamino)benzonitrile
-
-
3-amino-4-[(tetrahydro-2-furanylmethyl)amino] benzoic acid
-
-
3-benzylpentan-3-yl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
3-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
3-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
3-[(6-deoxy-L-mannopyranosyl)oxy]-5-hydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-en-1-yl)-4-oxo-4H-1-benzopyran-7-yl D-glucopyranoside
-
3-[(benzyloxy)methyl]-1-cyanopyrrolidine
-
IC 50: 100 nM
3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoic acid
-
-
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4'-(4-tert-butylpiperazin-1-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
-
4'-(4-tert-butylpiperazin-1-yl)-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide
-
strong inhibition
4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl][1,1'-biphenyl]-4-sulfonic acid
-
4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl][1,1'-biphenyl]-4-sulfonic acid
-
4'-[4-(tert-butylamino)piperidin-1-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
-
4'-[4-(tert-butylamino)piperidin-1-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide
-
strong inhibition
4-(2-[(3R)-3-aminopyrrolidin-1-yl]-1,3-thiazol-4-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-(3,4-dimethylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyanophenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile
-
-
4-(4-acetylpiperazin-1-yl)-5-amino-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
4-(cyclohexylamino)-6-(piperazin-1-yl)-1,3,5-triazine-2-carbonitrile
-
4-(cyclohexylamino)pyrimidine-2-carbonitrile
-
-
4-(dimethylamino)-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
-
-
4-(trifluoromethoxy)-N-(1-[[(1S)-1-([5-[3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamoyl]cyclohexyl)benzamide
-
-
4-(trifluoromethoxy)-N-(1-[[(1S)-1-([5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamoyl]cyclohexyl)benzamide
-
-
4-amino-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-amino-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
4-benzyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
4-butyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-cyano-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
moderate inhibition
4-cycloheptyl-6-propylpyrimidine-2-carbonitrile
-
-
4-cycloheptyl-6-[3-(piperidin-1-yl)propyl]pyrimidine-2-carbonitrile
4-cyclohexyl-6-propylpyrimidine-2-carbonitrile
-
-
4-cyclooctyl-6-propylpyrimidine-2-carbonitrile
-
-
4-cyclopentyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-dihydrotanshinone
potent exosite inhibitor of cathepsin K
4-ethyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-fluoro-N-(3-oxoazepan-4-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-(4-oxopyrrolidin-3-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-(5-oxo-2-phenylpiperidin-4-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-prop-2-yn-1-yl-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
4-fluoro-N-[1-(methylsulfonyl)-3-oxoazepan-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[1-(methylsulfonyl)-4-oxopyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
-
-
4-fluoro-N-[2-[2-(methylsulfonyl)phenyl]-5-oxopiperidin-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[3-oxo-1-(pyridin-2-ylsulfonyl)piperidin-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-(phenylcarbamoyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-(phenylcarbonyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-(pyridin-2-ylsulfonyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-fluoro-N-[4-oxo-1-[(phenylsulfonyl)carbamoyl]pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
4-methyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-Morpholinecarbonyl-Ala-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-aminohexanoic acid-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Gly-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Ile-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Leu-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Met-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-methionine dioxide-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Phe-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-Morpholinecarbonyl-Val-homophenylalanine-PSI(CH=CH-SO2-Ph)
-
-
4-phenyl-6-propylpyrimidine-2-carbonitrile
-
-
4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
moderate cathepsin K potency
4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)(4-iodobenzyl)amino]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)amino]-5-(3-[4-[(4-methoxyphenyl)sulfonyl]piperazin-1-yl]prop-1-yn-1-yl)pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)amino]-5-[3-(pyridin-3-yloxy)prop-1-yn-1-yl]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)amino]-5-[3-[4-(4-methylpiperazin-1-yl)phenyl]prop-1-yn-1-yl]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-(1H-1,2,4-triazol-1-ylmethyl)benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-(3-piperidin-1-ylprop-1-yn-1-yl)benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-[3-(1H-1,2,4-triazol-1-yl)prop-1-yn-1-yl]benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[(2,2-dimethylpropyl)[4-[3-(4-methylpiperazin-1-yl)prop-1-yn-1-yl]benzyl]amino]pyrimidine-2-carbonitrile
-
-
4-[2-(1,4'-bipiperidin-1'-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-[2-(1,4'-bipiperidin-1'-yl)-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
strong inhibition
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
4-[2-(4-methylpiperazin-1-yl)-4,5-dihydro-1,3-thiazol-4-yl]-N-(1-[[(3S,4R)-2-oxo-4-phenoxyazetidin-3-yl]carbamoyl]cyclohexyl)benzamide
-
4-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
4-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
strong inhibition
4-[2-(dimethylamino)ethyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-[2-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[2-[(3R)-3-aminopyrrolidin-1-yl]-1,3-thiazol-4-yl]-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
-
strong inhibition
4-[3-(dimethylamino)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-[3-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
-
-
4-[3-(pentan-3-ylamino)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[3-(piperidin-1-yl)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[3-(tert-butylamino)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
-
-
4-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
-
-
4-[benzyl(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzoic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-[[4-[3-(1,4'-bipiperidin-1'-yl)prop-1-yn-1-yl]benzyl](2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
4-[[4-[3-(4-acetylpiperazin-1-yl)prop-1-yn-1-yl]benzyl](2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-(3-[4-[(3-chloropropyl)sulfonyl]piperazin-1-yl]prop-1-yn-1-yl)-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-(3-hydroxyazetidin-1-yl)-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-(bicyclo[2.2.1]hept-2-ylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-(cyclohexylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-(cyclopentylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-(phenylamino)pyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-(tetrahydrofuran-3-ylamino)pyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-piperidin-1-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-morpholin-4-yl-6-pyrrolidin-1-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(1,1-dioxidotetrahydrothiophen-3-yl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-[(1-methylethyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(1-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(2,2-dimethylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(2-methoxyethyl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-amino-4-[(2-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(2-methylpropyl)amino]-6-piperazin-1-ylpyrimidine-2-carbonitrile
-
-
5-amino-4-[(2-methylpropyl)amino]-6-[(tetrazolidin-5-ylmethyl)amino]pyrimidine-2-carbonitrile
-
-
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
5-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)thiophene-2-carboxamide
-
-
5-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]thiophene-2-carboxamide
-
moderate inhibition
5-[3-(1,3-dihydro-2H-isoindol-2-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-[3-(3,4-dihydroisoquinolin-2(1H)-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
5-[3-(4,5-dichloro-1H-imidazol-1-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
-
-
6,8-dihydroxy-3-(3,4,5-trihydroxyphenyl)-2,3-dihydro-1,4-benzodioxin-2-yl 3,4,5-trihydroxybenzoate
-
6-(4-chlorobenzyl)-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(2-piperidin-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3,3,3-trifluoropropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-(4,4,4-trifluorobutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-(4-chlorobenzyl)-7-[2-(piperidin-1-yl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(bromomethyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(cyclohexylamino)-9-[(2S,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-9H-purine-2-carbonitrile
-
-
6-(cyclohexylamino)-9-[2-(4-methylpiperazin-1-yl)ethyl]-9H-purine-2-carbonitrile
-
-
6-(cyclohexylamino)pyrazine-2-carbonitrile
-
-
6-(cyclohexylamino)pyridine-2-carbonitrile
-
-
6-benzyl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-benzyl-7-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-cyano-2-(3-trifluoromethyl-phenyl)-3,5-dioxo-1,2,4-triazine
-
poor catK potency
6-[(1'-acetyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(4,5-dichloro-1H-imidazol-1-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(5,5-dimethyl-2,4-dioxo-1,3-oxazolidin-3-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(8-acetyl-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[(8-benzyl-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[4-[(diethylamino)methyl]benzyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[4-[3-(diethylamino)propoxy]-3-(trifluoromethyl)phenyl]-1-ethyl-2,3-dihydro-1H-indole-4-carbonitrile
-
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(4-acetyl-1,4-diazepan-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)-3-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[8-(2,4-dimethoxyphenyl)-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl]methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-(1H-1,2,3-triazol-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-(1H-imidazol-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(1,3-dioxo-2,8-diazaspiro[4.5]decan-2-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(5-fluoro-1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(5-methoxy-1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
7-(2,2-dimethylpropyl)-6-[(pyridin-4-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[4-(4-methylpiperazin-1-yl)benzyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[4-(morpholin-4-yl)benzyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[[2-oxo-1'-(propan-2-yl)spiro[indole-3,4'-piperidin]-1(2H)-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[[4-(4-fluorophenyl)piperazin-1-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[[8-(morpholin-4-ylacetyl)-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridin-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridin-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
antipain
98.91% inhibition at 0.1 mM
Aprotinin
25.08% inhibition at 0.1 mM
benzofuran-2-carboxylic acid [(S)-3-methyl-1-[2-oxo-3-(pyridin-2-ylsulfonylamino)propylcarbamoyl]butyl]amide
-
-
benzyl (1-[(cyanomethyl)carbamoyl]-2-hydroxypropyl)carbamate
-
-
benzyl (2S)-2-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)-4-methylpentanoate
-
-
benzyl (2S,3R)-1-(cyanomethylamino)-3-hydroxy-1-oxobutan-2-ylcarbamate
-
weak inhibition
benzyl (2S,3S)-1-(cyanomethylamino)-3-methyl-1-oxopentan-2-ylcarbamate
-
weak inhibition
benzyl 1-cyano-3-pyrrolidinylcarbamate
-
IC 50: 40 nM
benzyl [(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
benzyl [(1S)-1-[(cyanomethyl)carbamoyl]-2,2-dimethylpropyl]carbamate
-
weak inhibition
benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]carbamate
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
benzyl [(5S,13S)-11,15-dimethyl-5-(2-methylpropyl)-3,6,9,12-tetraoxo-1-phenyl-2-oxa-4,7,11-triazahexadecan-13-yl]carbamate
-
benzyl [1-[(cyanomethyl)carbamoyl]cyclohexyl]carbamate
benzyl [1-[(cyanomethyl)carbamoyl]cyclopentyl]carbamate
-
weak inhibition
Benzyloxycarbonyl-Phe-Ala-CHN2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
biphenyl-4-yl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
biphenyl-4-ylmethyl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
Boc-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
-
Boc-I
-
lysosomotropic, water-soluble polymer selective catK inhibitor. Inhibition of catK greatly reduces melanoma cell invasion through Matrigel basement membrane matrix and increases detection of internalized collagen
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
carbobenzyloxy-Phe-Phe-CH2F
-
-
carboxybenzoyl-Phe-Phe-CHN2
-
-
cathepsin K inhibitor II
-
-
cathepsin K propeptide
-
-
-
CatK-II
-
specific inhibitor
-
CatK-selective inhibitor II
Co2+
5.09% residual activity at 5 mM
Cu2+
24.86% residual activity at 5 mM
cystatin
-
different types, expression analysis in various cell types isolated from normal and neoplastic breast tissue, overview
-
dibenzyl [(2-oxopropane-1,3-diyl)bis[azanediyl[(2S)-4-methyl-1-oxopentane-1,2-diyl]]]biscarbamate
-
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
EDTA
3.72% inhibition at 0.1 mM
ethyl (4S)-4-[(4-fluoro-N-[2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucyl)amino]-3-oxopiperidine-1-carboxylate
-
ethyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
-
-
ethyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
-
ethyl 4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxoazepane-1-carboxylate
-
-
ethyl 4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxopiperidine-1-carboxylate
-
-
ethyl 4-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-3-oxoazepane-1-carboxylate
-
-
ethyl 4-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-5-oxopiperidine-2-carboxylate
-
-
Ethyl 5-[((3S)-3[[(isopropyl-2-methylpropoxy)carbonyl]amide]-2-oxoheptanoyl)amino]-1H-pyrazole-4-carboxylate
-
IC50: 1.7 nM
ethyl N-[[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]-b-alaninate
-
-
ethyl N-[[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]glycinate
-
-
H-kininogen
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
Hg2+
25.27% residual activity at 5 mM
Human squamous cell carcinoma antigen 1
-
i.e. SCCA1
-
kushennol F
shows inhibitory effects on the bone resorption process related to cathepsin K
L-13006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-kininogen
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
leupeptazin
-
isolated from a liquid culture of soil Streptomyces sp. IS2-4
methyl (3S)-3-[(4-fluoro-N-[2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
methyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
-
-
methyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
-
methyl 4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
-
-
methyl 5-acetoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
-
methyl 5-hydroxy-7,12-dioxo-7,12-dihydrodinaphtho[1,2-b:2',3'-d]furan-6-carboxylate
-
methyl 5-hydroxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
furanquinone from Paulownia tomentosa stem
methyl 5-methoxy dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
-
methyl 5-propoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
-
methyl methanethiolsulfonate
-
methyl N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninate
-
-
methyl [[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]carbamate
-
-
mPEG-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
Mu-Leu-Hph-fluoromethylketone
MV061194
-
selective, potent reversible cathepsin K inhibitor
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-3-yl)pentanehydrazide
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)pentanehydrazide
N'-cyano-N,N',4-trimethyl-2-([11,21:24,31-terphenyl]-14-yl)pentanehydrazide
-
N-((S)-4-methyl-1-oxo-1-((S)-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-ylamino)pentan-2-yl)benzofuran-2-carboxamide
-
-
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
N-(1-acetyl-4-oxopyrrolidin-3-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-carbamoyl-4-oxopyrrolidin-3-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyano-1-methylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyano-3-pyrrolidinyl)benzamide
-
IC 50: 370 nM
N-(1-cyano-3-pyrrolidinyl)[1,1'-biphenyl]-4-carboxamide
-
IC 50: 290 nM
N-(1-cyano-3pyrrolidinyl)benzenesulfonamide
-
IC 50: 50 nM
N-(1-cyanocyclopropyl)-4,4-difluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-norvalinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(1-hydroxycyclopropyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(1-hydroxycyclopropyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2-hydroxypropan-2-yl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2-hydroxypropan-2-yl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-(4-methyl-4,5-dihydro-1,3-thiazol-2-yl)phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-(quinolin-6-yl)phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-[5-(1-hydroxycyclopropyl)pyridin-2-yl]phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-[6-(methylsulfonyl)pyridin-3-yl]phenyl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl][1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1S)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1S)-2,2-difluoro-1-hydroxyethyl][1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2-difluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(1-ethynylcyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-2-pyridin-4-yl-1,3-thiazole-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(4-fluoropiperidin-4-yl)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(dimethylamino)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(piperazin-1-ylsulfonyl)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([(2S)-1-methylpyrrolidin-2-yl]methoxy)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([1-(2-hydroxyethyl)piperidin-4-yl]oxy)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([4-(2,2,2-trifluoroethyl)piperazin-1-yl]sulfonyl)biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-isoxazol-5-ylbiphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-piperazin-1-ylbiphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-3-yl)oxy]biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-4-yl)oxy]biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[methyl(1-methylpyrrolidin-3-yl)amino]biphenyl-4-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[methyl(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-morpholin-4-yl-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)amino]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[3-(dimethylamino)pyrrolidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-methylpiperazin-1-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(dimethylamino)benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-ethynylbenzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-morpholin-4-ylbenzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)carbonyl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)sulfonyl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1,4-dimethylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(4-morpholin-4-ylpiperidin-1-yl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(morpholin-4-ylmethyl)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(piperidin-4-yloxy)-1,3-thiazol-4-yl]benzamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-3-carboxamide
-
-
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
-
N-(1-[[(1S)-1-[[5-(1-methylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
N-(1-[[(1S)-1-[[5-(3-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
N-(1-[[(1S)-1-[[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
N-(2,3-dichlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: 9 nM
N-(2-chlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: 6 nM
N-(3-bromoprop-2-yn-1-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(3-[[(3R)-3-([1,1'-biphenyl]-3-yl)-5-methylhex-1-en-2-yl]amino]-2-oxopropyl)-4-phenoxybenzene-1-sulfonamide
-
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-(4-chlorophenyl)-2-methylalanyl-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-L-leucinamide
-
IC50 is below 1 nM
N-(4-methyl-1-oxo-1-[[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]pentan-2-yl)-1-benzofuran-2-carboxamide
-
-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)propanamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(5-isopropyl)pyridine-2-carboxyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: less than 3 nM
N-(cyanomethyl)-1-[(3-phenylpropanoyl)amino]cyclohexanecarboxamide
-
-
N-(cyanomethyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-(cyanomethyl)-4-methyl-2-[3'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
-
-
N-(cyanomethyl)-4-methyl-2-[3'-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
-
-
N-(cyanomethyl)-4-methyl-2-[4'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
-
-
N-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(piperazin-1-yl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-4-benzyloxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: 6 nM
N-4-isopropylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: less than 3 nM
N-4-methoxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
-
N-4-propylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
IC50: less than 3 nM
N-Acetyl-Leu-Leu-methional
-
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxamide
-
-
N-but-3-yn-2-yl-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-cyano-N2-[4-[4-(piperazin-1-yl)phenyl]thiophen-3-yl]-L-leucinamide
-
N-cyano-tetrahydro-pyridazine compounds
-
-
-
N-[(1-cyano-2-pyrrolidinyl)methyl]benzamide
-
IC 50: 0.013 mM
N-[(1-cyano-2-pyrrolidinyl)methyl]benzenesulfonamide
-
IC 50: 0.012 mM
N-[(1-cyano-3-azetidinyl)methyl]benzamide
-
IC 50: 70 nM
N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide
-
IC 50: 20 nM
N-[(1-cyano-3-azetidinyl)methyl]cyclohexanecarboxamide
-
IC 50: 5 nM
N-[(1-cyano-3pyrrolidinyl)methyl]benzenesulfonamide
-
IC 50: 200 nM
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-N2-(piperazin-1-ylcarbonyl)-D-leucinamide
-
i.e. APC3328
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(2-methyl-1H-imidazol-1-yl)acetyl]-L-leucinamide
-
IC50: 190 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(4-phenylpiperidin-1-yl)acetyl]-L-leucinamide
-
IC50: 84 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(4-pyridin-4-ylpiperazin-1-yl)acetyl]-L-leucinamide
-
IC50: 9 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(5-methyl-1H-imidazol-4-yl)acetyl]-L-leucinamide
-
IC50: 24 nM
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[2-(4-chlorophenoxy)-2-methylpropanoyl]-L-leucinamide
-
IC50 is below 1 nM
N-[(1S)-1-((3-hydroxy-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)-3-methylbutyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-([(1R)-2-(benzyloxy)-1-cyanoethyl]carbamoyl)-3-methylbutyl]-1-methyl-1H-indole-2-carboxamide
-
IC50 is below 1 nM
N-[(1S)-1-([(1R)-2-(benzyloxy)-1-cyanoethyl]carbamoyl)-3-methylbutyl]-1H-indole-2-carboxamide
-
IC50: 430 nM
N-[(1S)-1-([1-(2-hydroxy-2,3-dihydro-1,4-benzodioxin-2-yl)ethenyl]carbamoyl)-3-methylbutyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-([3-(2-hydroxyphenoxy)-1-methylidene-2-oxopropyl]carbamoyl)-3-methylbutyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1S)-1-carbamoyl-3-(methylsulfonyl)propyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-carbamoyl-3-phenylpropyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-cyano-2-phenylethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-cyano-3-(methylsulfanyl)propyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
N-[(1S)-1-cyclohexyl-3-[(2Z)-2-[(4R)-3,4-dimethyl-1,3-thiazolidin-2-ylidene]hydrazinyl]-2,3-dioxopropyl]cycloheptanecarboxamide
-
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-2-phenylacetamide
-
-
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-3-phenylpropanamide
-
-
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-N2-(2,2,2-trifluoroethyl)-L-leucinamide
-
-
N-[(1S)-1-[2-(methylsulfanyl)ethyl]-2-oxopropyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-3-(methylsulfonyl)-L-alaninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-alaninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninamide
-
excellent selectivity against the cathepsins B, L and S
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methionine
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-phenylalaninamide
-
excellent selectivity against the cathepsins B, L and S
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N,N-dimethyl-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-(2,2,2-trifluoroethyl)-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-(methylsulfonyl)-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-benzyl-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-methyl-L-methioninamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-S-methyl-L-cysteinamide
-
-
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucylglycinamide
-
-
N-[(1S)-3-methyl-1-(((4R)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[(1S)-3-methyl-1-([(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamoyl)butyl]-1-benzofuran-2-carboxamide
-
-
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
N-[(1S)-3-methyl-1-[[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]carbamoyl]butyl]-1-benzofuran-2-carboxamide
-
-
N-[(2S)-1-[4-(benzyloxy)anilino]butan-2-yl]-N2-(morpholine-4-carbonyl)-L-leucinamide
-
N-[(2S)-1-[4-(morpholin-4-yl)anilino]butan-2-yl]-N2-[(1S)-2,2,2-trifluoro-1-(4-hydroxyphenyl)ethyl]-L-leucinamide
-
N-[(2S)-1-[[(2R,4S)-2,4-dimethyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzofuran-2-carboxamide
-
-
N-[(2S)-1-[[(4S,5S)-4,5-dimethyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzofuran-2-carboxamide
-
-
N-[(2S)-4-methyl-1-([2-[4-(2-methylpropoxy)anilino]ethyl]amino)-1-oxopentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
-
N-[(2S)-4-methyl-1-oxo-1-[(3aS,6aR)-3-oxohexahydro-4H-furo[3,2-b]pyrrol-4-yl]pentan-2-yl]-4-(4-methylpiperazin-1-yl)benzamide
-
N-[(2S)-4-methyl-1-oxo-1-[(3aS,7aR)-3-oxohexahydrofuro[3,2-b]pyridin-4(2H)-yl]pentan-2-yl]-4-(4-methylpiperazin-1-yl)benzamide
-
N-[(2S)-4-methyl-1-oxo-1-[[(4R)-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]amino]pentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
-
N-[(2S)-4-methyl-1-[(3aS,6S,6aR)-6-methyl-3-oxohexahydro-4H-furo[3,2-b]pyrrol-4-yl]-1-oxopentan-2-yl]-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
N-[(2S)-4-methyl-1-[[(4S,7R)-7-methyl-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]amino]-1-oxopentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
-
N-[(4S)-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]-N2-[2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
-
N-[1-(benzylcarbamoyl)-4-oxopyrrolidin-3-yl]-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[1-(benzylsulfonyl)-3-oxoazepan-4-yl]-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[1-([(1S)-1-[(5-ethyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-methoxy-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-phenyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-tert-butyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-([(1S)-1-[(5-thiophen-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-2-pyridin-4-yl-1,3-thiazole-4-carboxamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(4-fluoropiperidin-4-yl)biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(dimethylamino)biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-(piperazin-1-ylsulfonyl)biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-isoxazol-5-ylbiphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-piperazin-1-ylbiphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[(1-methylpiperidin-3-yl)oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[(1-methylpiperidin-4-yl)oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[methyl(1-methylpyrrolidin-3-yl)amino]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[1-(2-hydroxyethyl)piperidin-4-yl]oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[1-(2-methoxyethyl)piperidin-4-yl]oxy]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4'-[[4-(2,2,2-trifluoroethyl)piperazin-1-yl]sulfonyl]biphenyl-4-carboxamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-morpholin-4-yl-1,3-thiazol-4-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-[4-[(1-methylethyl)amino]piperidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(2-[4-[methyl(1-methylethyl)amino]piperidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-methylpiperazin-1-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-morpholin-4-ylbenzamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[(4-methylpiperazin-1-yl)carbonyl]benzamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[(4-methylpiperazin-1-yl)sulfonyl]benzamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-morpholin-4-ylpiperidin-1-yl)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(morpholin-4-ylmethyl)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(piperidin-4-yloxy)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[3-(dimethylamino)pyrrolidin-1-yl]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-[methyl(4-methylpiperazin-1-yl)amino]-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-3-carboxamide
-
moderate inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]biphenyl-4-carboxamide
-
moderate inhibition
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-(phenylamino)cyclohexanecarboxamide
-
-
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-phenoxycyclohexanecarboxamide
-
-
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-[4-(1-methylethyl)phenoxy]cyclohexanecarboxamide
-
-
N-[4-methyl-1-oxo-1-([2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]amino)pentan-2-yl]-1-benzofuran-2-carboxamide
-
-
N-[cyano(dicyclobutyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[cyano(dicyclopropyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[cyano(phenyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N2-(3-cyclohexylphenyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
-
-
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
-
N2-biphenyl-3-yl-N-[(1S)-1-[([4-[2-(1H-tetrazol-5-yl)ethoxy]phenyl]amino)methyl]propyl]-L-leucinamide
-
-
N2-biphenyl-3-yl-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]-L-leucinamide
-
-
N2-biphenyl-3-yl-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-leucinamide
-
-
N2-biphenyl-3-yl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2-difluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)biphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)[1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
N2-[(1S)-1-[4'-(2-amino-2-oxoethyl)[1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
N2-[(1S)-1-[4'-[(2S)-1-amino-1-oxopropan-2-yl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(1S)-1-[4-[5-(1-carbamoylcyclopropyl)pyridin-2-yl]phenyl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
-
-
N2-[(benzyloxy)carbonyl]-N-((1S)-1-cyano-2-[4-(trifluoromethyl)phenyl]ethyl)-L-leucinamide
-
IC50: 43 nM
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-2-methylleucinamide
-
weak inhibition
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-4-methyl-L-leucinamide
-
moderate inhibition
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-5,5,5-trifluoro-D-leucinamide
-
-
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-5,5,5-trifluoroleucinamide
-
moderate inhibition
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-D-leucinamide
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-isoleucinamide
-
-
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-leucinamide
-
-
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-norleucinamide
N2-[(benzyloxy)carbonyl]-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-L-leucinamide
-
IC50: 9 nM
N2-[(benzyloxy)carbonyl]-N-[(1R)-2-tert-butoxy-1-cyanoethyl]-L-leucinamide
-
IC50: 240 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(3-methylphenyl)ethyl]-L-leucinamide
-
IC50: 120 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(4-methoxyphenyl)ethyl]-L-leucinamide
-
IC50: 63 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(4-methylphenyl)ethyl]-L-leucinamide
-
IC50: 48 nM
N2-[(benzyloxy)carbonyl]-N-[(1S)-2-(4-tert-butoxyphenyl)-1-cyanoethyl]-L-leucinamide
-
IC50: 398 nM
N2-[(benzyloxy)carbonyl]-N-[2-oxo-3-[(4-phenoxybenzene-1-sulfonyl)amino]propyl]-L-leucinamide
-
N2-[(benzyloxy)carbonyl]-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
-
-
N2TY
-
slow-binding inhibitor of cathepsin K
-
Nalpha-3-chlorobenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
less efficient than Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
Nalpha-3-methoxybenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
less efficient than Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
Nalpha-3-methylbenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
-
Nalpha-4-chlorobenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
-
Nalpha-4-methoxybenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
IC50: 64 nM
Nalpha-4-methylbenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
-
Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
-
IC50: 470 nM
naphthalen-2-yl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
odanacatib 1
-
i.e. MK-0822, a reversible, non-basic, potent and selective Cat K inhibitor. The nitrile forms a hydrogen bond-stabilized thioimidate intermediate with Cys25. The leucine moiety interacts with the hydrophobic S2 subsite and the biphenyl moiety with the S3 subsite, and the hydrogen bond of the trifluroethylamine amide isostere interact with Gly66. Furthermore, odanacatib does not interact with the prime side of Cat K, binding structure, overview
pepstatin A
17.29% inhibition at 0.1 mM
Phe-Phe-fluoromethylketone
-
phenyl (4S)-4-([[(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamoyl]oxy)-3,3-dimethylpyrrolidine-1-carboxylate
-
-
phenylmethylsulfonyl fluoride
53.68% inhibition at 0.1 mM
PHPMA-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
PHPMA-GG-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
piperidin-2-yl-[2-(trifluoromethyl)-6-[4-(trifluoromethyl)phenyl]pyridin-4-yl] methanol
-
-
piperidine-4-carboxylic acid [3-methyl-1[1-(1-oxa-3-aza-cyclopenta[a]naphthalene-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
pyridoxal phosphate
-
at 1 mM 85% inhibition
quinoline-2-carboxylic acid [(S)-1-((3R,S)-4-oxotetrahydrofuran-3ylcarbamoyl)-3-methylbutyl]amide
-
-
relicatib
-
also known as SB-462795, highly potent human cathepsin K inhibitor
S-(1-methylethyl) (2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazinecarbothioate
-
-
S-[2-[2-(dihydroxymethyl)anilino]-2-oxoethyl] carbamothioate
-
SB-357114
-
specific inhibitor
SB-553484
-
inhibits bone and cartilage degradation in vivo
SDS
77.28% residual activity at 0.05% (w/v)
SM934-testosterone
inhibits proliferation and metastasis ability of breast cancer cells via inhibiting the expression of cathepsin K followed by the inhibition of Bcl-xL
sodium (2S,3S)-3-[[(2S)-4-methyl-1-(2-methylpropoxy)pentan-2-yl]amino]oxirane-2-carboxylate
-
sophoraflavanone G
shows inhibitory effects on the bone resorption process related to cathepsin K
Stefin A
-
slow-binding inhibitor of cathepsin K
-
Stefin B
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
STPHPMA-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
conjugate
Synthetic inhibitors
-
-
-
tert-butyl ([1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]carbamoyl)carbamate
-
-
tert-butyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
-
-
tert-butyl 3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoate
-
-
tert-butyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
-
-
tert-butyl 3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoate
-
-
tert-butyl [(1S)-1-([5-[4-(dimethylamino)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamate
-
-
tert-butyl [(1S)-1-formylpentyl]carbamate
-
-
tert-butyl [(1S)-1-[(5-thiophen-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-(4,5-dihydro-1,3-thiazol-2-ylhydrazono)methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-(carbamimidoylhydrazono)methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-(carbamoylhydrazono)methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(2,3-dihydro-1H-indol-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(3,4-dihydroisoquinolin-2(1H)-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(3,4-dihydroquinolin-1(2H)-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(3-methylbutanoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(benzylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(diethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(dimethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(dimethylsulfamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(ethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(methylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(phenylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(phenylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(piperidin-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(pyrrolidin-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(tert-butylcarbamoyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[(trifluoroacetyl)hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[methyl[(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[methyl[methyl(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[[(1-methylethyl)carbamothioyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[[(1-methylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[[(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[[(morpholin-4-ylcarbonyl)oxy]imino]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[(E)-[[methyl(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
-
-
tert-butyl [(1S)-1-[[5-(1-methylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamate
-
-
tert-butyl [(1S)-1-[[5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamate
-
-
tert-butyl [(3S)-1,2-dioxo-1-(phenylamino)heptan-3-yl]carbamate
-
-
tert-butyl [(3S)-1,2-dioxo-1-(propan-2-ylamino)heptan-3-yl]carbamate
-
-
tert-butyl [(3S)-1,2-dioxo-1-[[(1R)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
tert-butyl [(3S)-1,2-dioxo-1-[[(1S)-1-phenylethyl]amino]heptan-3-yl]carbamate
-
-
tert-butyl [(3S)-1-(benzylamino)-1,2-dioxoheptan-3-yl]carbamate
-
-
tert-butyl [(3S)-1-amino-1,2-dioxoheptan-3-yl]carbamate
-
-
tert-butyl [1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]carbamate
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
VEL-0230
highly selective inhibitor of CatK that significantly decreases bone resorption and increases bone formation biomarkers
Zn2+
47.5% residual activity at 5 mM
[(S)-1-((3R,S)-1-acetyl-4-oxopyrrolidin-3-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
[(S)-1-((3R,S)-4-oxotetrahydrofuran-3-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
[(S)-1-((4R,S)-3-oxotetrahydropyran-4-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
[1-(2-cyano-tetrahydro-pyridazine-1-carbonyl)-2-methyl-propyl]-carbamic acid benzyl ester
-
inhibits the bone resorptive activity of mature osteoclasts, structure and interaction pattern with cathepsin K, overview
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
-
-
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
-
-
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
-
-
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
-
-
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
-
-
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
-
IC 50: 3 nM, reversible inhibition
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
-
-
(S,S)-piperidine-4-carboxylic acid [1-[1-(benzoxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
-
(S,S)-piperidine-4-carboxylic acid [1-[1-(benzoxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-3-methyl-butyl]-amide
-
-
1,3-bis(CBZ-Leu-NH)-2-propanone
-
-
1,3-bis(CBZ-Leu-NH)-2-propanone
-
-
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
-
IC50: 0.77 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
-
IC50: 13 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 15 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 790 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 62 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 0.0012 mM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 25 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 470 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 0.65 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 12 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 0.21 nM
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
-
IC50: 1.8 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 15 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0011 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 22 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0012 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 20 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0011 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 26 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0015 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 39 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0027 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 17 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.001 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.41 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 11 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 32 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0017 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.47 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
-
IC50: 5.5 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
-
IC50: 62 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0016 mM
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
-
IC50: 27 nM
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
-
IC50: 0.0017 mM
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
-
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
4-cycloheptyl-6-[3-(piperidin-1-yl)propyl]pyrimidine-2-carbonitrile
-
-
4-cycloheptyl-6-[3-(piperidin-1-yl)propyl]pyrimidine-2-carbonitrile
-
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
balicatib
-
-
balicatib
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
balicatib
-
high degree of potency and selectivity for purified human Cat K
balicatib
-
potent human cathepsin K inhibitor with a high selectivity against human cathepsins B, L and S (> 4800fold, > 500fold and > 65000fold, respectively)
benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]carbamate
-
-
benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]carbamate
-
weak inhibition
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
-
shows any degree of Cat K selectivity (10fold vs. Cat L and F)
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
-
-
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
-
-
benzyl [1-[(cyanomethyl)carbamoyl]cyclohexyl]carbamate
-
moderate inhibition
benzyl [1-[(cyanomethyl)carbamoyl]cyclohexyl]carbamate
-
-
BML-244
-
has moderate selectivity (more than 30fold), but is a relatively weak inhibitor of human Cat K
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
-
-
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
-
-
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
-
-
CatK-selective inhibitor II
-
i.e. Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
CatK-selective inhibitor II
-
commercial preparation
chymostatin
-
-
chymostatin
44.58% inhibition at 0.1 mM
cystatin C
-
natural inhibitor of cathepsin K, reversible, tight-binding competitive inhibitor
-
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
-
-
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
-
-
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
-
-
E-64
-
a cysteine protease inhibitor
E-64
i.e. L-3-carboxy-trans-2,3-epoxypropionylleucylamido-(4-guanidino)butane
E-64
i.e. trans-epoxysuccinyl-L-leucylamido(4-guanidino)butane
E-64
irreversible inhibitor
E-64
irreversible inhibitor
E-64
-
i.e. epoxysuccinyl-L-leucylamido-{4-guanidino} butane, nonspecific inhibitor
E-64
60.15% inhibition at 0.5 mM
E64
-
i.e. L-3-carboxy-trans-2,3-epoxypropionyl-leucylamido-(4-guanidino)butane, inhibitor-enzyme complex structure 9in presence of different chondroitin 4-sulfate fractions, overview
E64
-
blocks adipocyte differentiation in early stages
E64
-
a nonselective cysteine protease inhibitor, complete inhibition
K4b
-
potent, reversible, Cat K-selective inhibitor
K4b
-
potent, reversible, Cat K-selective inhibitor
K4b
-
potent, reversible, Cat K-selective inhibitor
L-006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-006235
-
shows no selectivity in cell-based assays over cathepsins B, L, and S
L-873724
-
-
L-873724
-
a cathepsin K inhibitor
L-873724
-
highly selective for cathespin K over other cathepsins, metabolization, overview
L-873724
-
high degree of potency and selectivity (more than 100fold) for purified human Cat K
L-873724
-
has a greater than 800fold selectivity over other cysteine cathepsins
L-873724
-
the neutral Cat K inhibitor suppresses biochemical markers of bone resorption in vivo, highly selective for cathespin K over other cathepsins, metabolization, overview
L-873724
-
highly selective for cathespin K over other cathepsins, metabolization, overview
leupeptin
-
-
leupeptin
complete inhibition at 0.1 mM
LHVS
-
a cell-permeable broad spectrum cathepsin inhibitor
LHVS
-
a cell-permeable broad spectrum cathepsin inhibitor
MK-0674
-
orally bioavailable potent and selective cathepsin K inhibitor
Mu-Leu-Hph-fluoromethylketone
-
highly potent versus Cat K, but is essentially non-selective versus all human cathepsins
Mu-Leu-Hph-fluoromethylketone
-
-
Mu-Leu-Hph-fluoromethylketone
-
-
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-3-yl)pentanehydrazide
racemic
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-3-yl)pentanehydrazide
racemic
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)pentanehydrazide
racemic
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)pentanehydrazide
racemic
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
i.e. L-006235 or CRA-013788/L
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
i.e. L-006235 or CRA-013788/L
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
-
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
MIV-701
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
-
-
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide
-
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
strong inhibition
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-D-leucinamide
-
-
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-D-leucinamide
-
weak inhibition
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-norleucinamide
-
-
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-norleucinamide
-
moderate inhibition
NC-2300
-
-
NSC13345
i.e. 2-[(2-carbamoylsulfanylacetyl)-amino]benzoic acid, good selectivity for cathepsin K over related enzymes
odanacatib
-
i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib
odanacatib
-
i.e. MK-0822, a selective cathepsin K inhibitor
odanacatib
-
i.e. MK-0822, development of an enantioselective method for synthesis of the potent cathepsin K inhibitor, via triflate displacement of an alpha-trifluoromethylbenzyl triflate, overview. The key step involves the novel stereospecific SN2 triflate displacement of a chiral alpha-trifluoromethylbenzyl triflate with (S)-gamma-fluoroleucine ethyl ester to generate the required alpha-trifluoromethylbenzyl amino stereocenter
odanacatib
-
high degree of potency and selectivity for purified human Cat K
odanacatib
-
MK-0822, orally active, potent and selective cathepsin K inhibitor
odanacatib
-
formely MK-0822
odanacatib
-
MK-0822 or MK-822
odanacatib
-
i.e. MK-0822, a selective cathepsin K inhibitor
odanacatib
-
i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib
odanacatib
-
i.e. MK-0822, a selective cathepsin K inhibitor
odanacatib
-
i.e. MK-0822, a selective cathepsin K inhibitor, pharmacokinetics of odanacatib
piperidine-4-carboxylic acid [3-methyl-1[1-(1-oxa-3-aza-cyclopenta[a]naphthalene-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
-
piperidine-4-carboxylic acid [3-methyl-1[1-(1-oxa-3-aza-cyclopenta[a]naphthalene-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
-
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
-
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
-
relacatib
-
-
relacatib
-
a Cat K inhibitor in clinical development
relacatib
-
highly potent versus human Cat K, but lacks selectivity versus Cat L, S, and F
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
i.e. E-64
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
i.e. E-64
additional information
-
not inhibitory are pepstatin, phenylmethylsulfonylfluoride, EDTA, 1,10-phenanthroline
-
additional information
-
physiological inhibitors of osteoclast differentiation and activation, such as osteoprotegerin, interleukin-6, INF-gamma, can also directly suppress cathepsin K expression
-
additional information
-
structure-based design of diverse pyrimidine-based scaffolds for inhibitor design
-
additional information
-
inhibitory activities of N-cyano-tetrahydro-pyridazine derivatives, docking studies, overview
-
additional information
-
inhibitor development and structure-activity relationships, overview
-
additional information
-
construction of a three-dimensional pharmacophore model for cathepsin K inhibitor screening and development using the enzyme crystal structure complexed with a ketoamide inhibitor, docking and inhibitor binding structure, validation of pharmacophore hypothesis, overview
-
additional information
-
P2/S2 and P3/S3 interaction of cathepsin K inhibitors with pyrrolopyrimidine scaffold and structure of the common intermediate, overview
-
additional information
-
not inhibited by pyrimidine nitrile
-
additional information
-
not inhibited by N-benzoyl-4-aminosalicylic acid (NSC159686), (2-biphenylylmethyl)malonic acid (NSC94914), 1,4,7,9B-tetraazaphenalene (NSC81462), 1-[1-(2-phenylethyl)-4-piperidinyl]-methanamine, 2-[(3-nitrophenyl)carbamoyl]benzoic acid (NSC408860), and methyl N-[1-(4-methoxyphenyl)-2,5-dioxopyrrolidin-3-yl]glycinate
-
additional information
a fluorescence polarization assay is developed to screen 4761 compounds for substrate-specific ectosteric collagenase inhibitors of cathepsin K. A total of 38 compounds are identified that block the collagenase activity without interfering with the hydrolysis of active site substrates such as the synthetic peptide substrate, benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin, and gelatin. The identified inhibitors can be divided into two main classes, negatively charged and polyaromatic compounds which suggest the binding to different ectosteric sites
-
additional information
irreversible covalent inhibitors can have a beneficial pharmacokinetic/pharmacodynamics profile but are still often avoided due to the risk of indiscriminate ovalent reactivity and the resulting adverse effects. To overcome this potential liability, we introduced an alkyne moiety as a latent electrophile into small molecule inhibitors of cathepsin K (CatK). Alkyne-based inhibitors do not show indiscriminate thiol reactivity but potently inhibit CatK protease activity by formation of an irreversible covalent bond with the catalytic cysteine residue. Binding mode of alkynes is irreversible and covalent
-
additional information
-
irreversible covalent inhibitors can have a beneficial pharmacokinetic/pharmacodynamics profile but are still often avoided due to the risk of indiscriminate ovalent reactivity and the resulting adverse effects. To overcome this potential liability, we introduced an alkyne moiety as a latent electrophile into small molecule inhibitors of cathepsin K (CatK). Alkyne-based inhibitors do not show indiscriminate thiol reactivity but potently inhibit CatK protease activity by formation of an irreversible covalent bond with the catalytic cysteine residue. Binding mode of alkynes is irreversible and covalent
-
additional information
-
no inhibition of cathepsin K inhibitor III
-
additional information
-
stem bark extracts of Ulmus davidiana, a deciduous tree from Korea and an antiinflammatory in traditional Korean medicine, prevents the osteoclast-mediated intracellular processing of Cat K, suggesting that it may disrupt the intracellular transport of pro Cat K. Ulmus davidiana dose-dependently inhibits in vitro bone resorption with a potency similar to that observed for inhibition of Cat K processing
-
additional information
-
not inhibited by pyrimidine nitrile
-
additional information
-
not inhibitory are phenylmethylsulfonylfluoride, disopropyfluorophosohate, soybean inhibitor, pepstatin A
-
additional information
-
inhibitor synthesis and pharnacokinetics, overview
-
additional information
not inhibited by EGTA and 1,10-phenanthroline
-
additional information
-
not inhibited by EGTA and 1,10-phenanthroline
-
additional information
-
metabolism and pharmacokinetics, overview
-
additional information
-
P2/S2 and P3/S3 interaction of cathepsin K inhibitors with pyrrolopyrimidine scaffold and structure of the common intermediate, overview
-
additional information
-
not inhibited by pyrimidine nitrile
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.000002 - 0.000015
((S)-1-[1-[4(R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxoazepan-1-yl]methanoyl]-3-methylbutl)carbamic acid benzyl ester
0.0000023
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-4-oxopyrrolidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
0.0000006
((S)-1-[[(3R,S)-((S)-2-benzyloxycarbonylmethylamino-4-methylpentanoylamino)-4-oxopyrrolidin-1-yl]methanoyl]-3-methylbutyl)carbamic acid benzyl ester
-
-
0.288
(1'S)-7-(1-aminoethyl)-2-(2-methoxyphenyl)pyrazolo[1,5-a] pyrimidine hydrochloride
25°C, pH 5.5
0.241
(1'S)-7-(1-aminoethyl)-2-(3-trifluoromethylphenyl)pyrazolo-[1,5-a]pyrimidine hydrochloride
25°C, pH 5.5
0.077
(1'S)-7-(1-aminoethyl)-2-benzyl-3-phenylpyrazolo[1,5-a]pyrimidine hydrochloride
25°C, pH 5.5
0.236
(1'S)-7-(1-aminoethyl)-2-phenylpyrazolo[1,5-a]pyrimidine hydrochloride
25°C, pH 5.5
0.595
(1'S)-7-(1-aminoethyl)pyrazolo[1,5-a]pyrimidine-3-(N-methylcarboxamide) hydrochloride
25°C, pH 5.5
0.714
(1'S)-7-(1-aminoethyl)pyrazolo[1,5-a]pyrimidine-3-carboxylate hydrochloride
25°C, pH 5.5
0.0000003
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.0000017
(1R,2S)-N-(cyanomethyl)-2-[2-[4-(methylsulfanyl)phenyl]ethyl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
0.00000013
(2R)-2-[3'-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
-
-
0.0000003
(2R)-N-(cyanomethyl)-2-[3'-(2-[[3-(dimethylamino)pyrrolidin-1-yl]methyl]-1,3-thiazol-4-yl)biphenyl-3-yl]-4-methylpentanamide
-
-
0.00000048
(2R)-N-(cyanomethyl)-4-methyl-2-[3'-[2-(piperazin-1-ylmethyl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
-
-
0.0000008
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)biphenyl-3-yl]pentanamide
-
-
0.018
(2S)-2-amino-N-[(1S)-2-(biphenyl-4-yl)-1-cyanoethyl]butanamide
-
-
0.0019
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00024
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00073
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0015
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00029
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00043
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00045
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00057
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0011
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.001
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000098
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0012
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0022
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000025
1,4-anhydro-3,5,6-trideoxy-3-[(1-[4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamido]cyclohexane-1-carbonyl)amino]-L-erythro-hex-2-ulose
pH and temperature not specified in the publication
0.0003
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.005
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0007
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00056
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00047
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0018
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00098
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00052
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00027
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00037
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0005
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0023
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0017
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00042
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00064
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0005
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0012
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00055
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.003
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00026
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0023
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00038
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00084
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0016
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0017
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0015
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00044
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0008
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00082
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00073
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00095
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00095
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.000006
1-(N-benzyloxycarbonyl-leucyl)-5-(N-Boc-phenylalanylleucyl)carbohydrazide
-
at 37°C, pH 6.0
0.0000097
1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.0000027
2,2'-N,N'-bis(benzyloxycarbonyl)-L-leucinylcarbohydrazide
-
pH 5.5, room temperature
0.00001
2-amino-4-bromo-N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]benzamide
pH and temperature not specified in the publication
0.0005
2-methylpropyl [(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
0.0000025
3-(4-([4'-((1-[(cyanomethyl)carbamoyl]cyclohexyl)carbamoyl)biphenyl-4-yl]oxy)piperidin-1-yl)propanoic acid
-
Ki-value is below 0.0000025 mM
0.00023
3-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
0.00075
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.00095
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
100 mM sodium phosphate, 5 mM EDTA, 1 mM DTT, 0.1% PEG 4000, pH 6.5
0.0000025
4'-(4-tert-butylpiperazin-1-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000025
4'-[4-(tert-butylamino)piperidin-1-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000014
4-(2-[(3R)-3-aminopyrrolidin-1-yl]-1,3-thiazol-4-yl)-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
0.00000095
4-(dimethylamino)-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
-
-
0.000054
4-(trifluoromethoxy)-N-(1-[[(1S)-1-([5-[3-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamoyl]cyclohexyl)benzamide
-
-
0.00055
4-(trifluoromethoxy)-N-(1-[[(1S)-1-([5-[4-(trifluoromethyl)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamoyl]cyclohexyl)benzamide
-
-
0.000032
4-amino-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
0.000018
4-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
0.000019
4-fluoro-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
-
-
0.00000045
4-[2-(1,4'-bipiperidin-1'-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
0.00000029
4-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)benzamide
-
-
0.000016
5-bromo-N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)thiophene-2-carboxamide
-
-
0.0000016
benzofuran-2-carboxylic acid [(S)-3-methyl-1-[2-oxo-3-(pyridin-2-ylsulfonylamino)propylcarbamoyl]butyl]amide
-
-
0.011
benzyl (1-[(cyanomethyl)carbamoyl]-2-hydroxypropyl)carbamate
-
-
0.00000025
benzyl (2S)-2-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)-4-methylpentanoate
-
Ki: value below 0.00000025 mM
0.00014
benzyl 1-cyano-3-pyrrolidinylcarbamate
-
pH 5.5, room temperature
0.003
benzyl [(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
0.03
benzyl [(1S)-2-[(cyanomethyl)amino]-1-(naphthalen-2-ylmethyl)-2-oxoethyl]carbamate
-
-
0.000084
benzyl [1-[(cyanomethyl)carbamoyl]cyclohexyl]carbamate
-
pH and temperature not specified in the publication
0.000006
Boc-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.0000026 - 0.000147
cathepsin K propeptide
-
0.0000000041 - 0.0000000087
cystatin C
-
0.000022
dibenzyl [(2-oxopropane-1,3-diyl)bis[azanediyl[(2S)-4-methyl-1-oxopentane-1,2-diyl]]]biscarbamate
pH and temperature not specified in the publication
0.0000000054 - 0.0000000145
H-kininogen
-
0.0000000049 - 0.0000000135
L-kininogen
-
0.044
leupeptazin
-
pH and temperature not specified in the publication
0.0000066
mPEG-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.0000025
MV061194
-
pH and temperature not specified in the publication
0.00000721
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-3-yl)pentanehydrazide
racemic, pH and temperature not specified in the publication
0.00000114
N'-cyano-N,N',4-trimethyl-2-(4'-(methylsulfonyl)-[1,1'-biphenyl]-4-yl)pentanehydrazide
racemic, pH and temperature not specified in the publication
0.0000029
N'-cyano-N,N',4-trimethyl-2-([11,21:24,31-terphenyl]-14-yl)pentanehydrazide
pH and temperature not specified in the publication
0.000000073
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
-
recombinant cathepsin K
0.00009
N-(1-cyano-3pyrrolidinyl)benzenesulfonamide
-
pH 5.5, room temperature
0.0000043
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2-hydroxypropan-2-yl)biphenyl-4-yl]ethyl]-L-leucinamide
-
pH and temperature not specified in the publication
0.0000017
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
pH and temperature not specified in the publication
0.00001
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1S)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
-
pH and temperature not specified in the publication
0.00015
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-2-pyridin-4-yl-1,3-thiazole-4-carboxamide
-
-
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(4-fluoropiperidin-4-yl)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.000002
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(dimethylamino)biphenyl-4-carboxamide
-
-
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-(piperazin-1-ylsulfonyl)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([(2S)-1-methylpyrrolidin-2-yl]methoxy)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([1-(2-hydroxyethyl)piperidin-4-yl]oxy)biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000061
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-([4-(2,2,2-trifluoroethyl)piperazin-1-yl]sulfonyl)biphenyl-4-carboxamide
-
-
0.0000054
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-isoxazol-5-ylbiphenyl-4-carboxamide
-
-
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-piperazin-1-ylbiphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.00000067
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-3-yl)oxy]biphenyl-4-carboxamide
-
-
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[(1-methylpiperidin-4-yl)oxy]biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4'-[methyl(1-methylpyrrolidin-3-yl)amino]biphenyl-4-carboxamide
-
Ki-value is below 0.0000025 mM
0.00000059
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
-
0.0000016
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-(4-[methyl(1-methylethyl)amino]piperidin-1-yl)-1,3-thiazol-4-yl)benzamide
-
-
0.0000023
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-morpholin-4-yl-1,3-thiazol-4-yl)benzamide
-
-
0.00000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)amino]-1,3-thiazol-4-yl)benzamide
-
-
0.0000016
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[(4-methylpiperazin-1-yl)methyl]-1,3-thiazol-4-yl)benzamide
-
-
0.00000079
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[3-(dimethylamino)pyrrolidin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
0.00000048
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(2-methoxyethyl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
0.00000047
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(2-[4-(tetrahydro-2H-pyran-4-yl)piperazin-1-yl]-1,3-thiazol-4-yl)benzamide
-
-
0.0000015
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-methylpiperazin-1-yl)benzamide
-
-
0.0000014
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(4-propylpiperazin-1-yl)benzamide
-
-
0.0000033
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-(dimethylamino)benzamide
-
-
0.000013
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-ethynylbenzamide
-
-
0.000019
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-morpholin-4-ylbenzamide
-
-
0.000014
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)carbonyl]benzamide
-
-
0.000013
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[(4-methylpiperazin-1-yl)sulfonyl]benzamide
-
-
0.00000095
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1,4-dimethylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
-
0.00000094
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
-
-
0.0000025
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(4-morpholin-4-ylpiperidin-1-yl)-1,3-thiazol-4-yl]benzamide
-
Ki-value is below 0.0000025 mM
0.0000087
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(morpholin-4-ylmethyl)-1,3-thiazol-4-yl]benzamide
-
-
0.00000057
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)-4-[2-(piperidin-4-yloxy)-1,3-thiazol-4-yl]benzamide
-
-
0.00021
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-3-carboxamide
-
-
0.0000062
N-(1-[(cyanomethyl)carbamoyl]cyclohexyl)biphenyl-4-carboxamide
-
-
0.000035
N-(1-[[(1S)-1-[[5-(1-methylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
0.000037
N-(1-[[(1S)-1-[[5-(3-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
0.000022
N-(1-[[(1S)-1-[[5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamoyl]cyclohexyl)-4-(trifluoromethoxy)benzamide
-
-
0.000011
N-(2,3-dichlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
standard assay conditions
0.0000014
N-(3-[[(3R)-3-([1,1'-biphenyl]-3-yl)-5-methylhex-1-en-2-yl]amino]-2-oxopropyl)-4-phenoxybenzene-1-sulfonamide
pH and temperature not specified in the publication
0.00000016
N-(4-methyl-1-oxo-1-[[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]pentan-2-yl)-1-benzofuran-2-carboxamide
-
pH and temperature not specified in the publication
0.00041
N-(cyanomethyl)-1-[(3-phenylpropanoyl)amino]cyclohexanecarboxamide
-
-
0.00000008
N-(cyanomethyl)-4-methyl-2-[3'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
-
-
0.00000013
N-(cyanomethyl)-4-methyl-2-[3'-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
-
-
0.00000035
N-(cyanomethyl)-4-methyl-2-[4'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
-
-
0.000015
N-4-benzyloxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
-
standard assay conditions
0.00002
N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide
-
pH 5.5, room temperature
0.00012
N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-norvalinamide
-
-
0.000054
N-[(1S)-1-((3-hydroxy-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)-3-methylbutyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
0.0000001
N-[(1S)-1-cyclohexyl-3-[(2Z)-2-[(4R)-3,4-dimethyl-1,3-thiazolidin-2-ylidene]hydrazinyl]-2,3-dioxopropyl]cycloheptanecarboxamide
pH and temperature not specified in the publication
0.052
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-2-phenylacetamide
-
-
0.0096
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-3-phenylpropanamide
-
-
0.00012
N-[(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]-N2-(2,2,2-trifluoroethyl)-L-leucinamide
-
-
0.0000047
N-[(1S)-3-methyl-1-(((4R)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl)carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
0.0000000048 - 0.0000048
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
0.00000014
N-[(2S)-1-[[(2R,4S)-2,4-dimethyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzofuran-2-carboxamide
-
pH and temperature not specified in the publication
0.0000000099
N-[(2S)-1-[[(4S,5S)-4,5-dimethyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]-4-methyl-1-oxopentan-2-yl]-1-benzofuran-2-carboxamide
-
pH and temperature not specified in the publication
0.0000087
N-[(2S)-4-methyl-1-oxo-1-[(3aS,6aR)-3-oxohexahydro-4H-furo[3,2-b]pyrrol-4-yl]pentan-2-yl]-4-(4-methylpiperazin-1-yl)benzamide
pH and temperature not specified in the publication
0.00000016
N-[(2S)-4-methyl-1-oxo-1-[[(4R)-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]amino]pentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
pH and temperature not specified in the publication
0.0000006
N-[(2S)-4-methyl-1-[(3aS,6S,6aR)-6-methyl-3-oxohexahydro-4H-furo[3,2-b]pyrrol-4-yl]-1-oxopentan-2-yl]-4-[2-(1-methylpiperidin-4-yl)-1,3-thiazol-4-yl]benzamide
pH and temperature not specified in the publication
0.000000041
N-[(2S)-4-methyl-1-[[(4S,7R)-7-methyl-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-yl]amino]-1-oxopentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
pH and temperature not specified in the publication
0.0000079
N-[1-([(1S)-1-[(5-ethyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.00000025 - 0.0000017
N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
0.0000033
N-[1-([(1S)-1-[(5-methoxy-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.000029
N-[1-([(1S)-1-[(5-phenyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.0013
N-[1-([(1S)-1-[(5-tert-butyl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.0000052
N-[1-([(1S)-1-[(5-thiophen-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.0000016
N-[4-methyl-1-oxo-1-([2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]amino)pentan-2-yl]-1-benzofuran-2-carboxamide
-
pH and temperature not specified in the publication
0.0000012
N2-(morpholin-4-ylcarbonyl)-N-[(1E,3S)-5-phenyl-1-(phenylsulfonyl)pent-1-en-3-yl]-L-leucinamide
-
-
0.00035
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-5,5,5-trifluoro-D-leucinamide
-
-
0.013
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-D-leucinamide
-
-
0.0015
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-isoleucinamide
-
-
0.0000347
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-leucinamide
-
-
0.00049
N2-[(benzyloxy)carbonyl]-N-(cyanomethyl)-L-norleucinamide
-
-
0.028
NSC13345
at pH 5.5 and 25°C
0.00027
PHPMA-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.000392
PHPMAGG-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.000001 - 0.000002
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
0.00055
procathepsin K
-
pH 5.5, room temperatur
-
0.00027
procathepsin L
-
pH 5.5, room temperatur
-
0.0007
procathepsin S
-
pH 5.5, room temperatur
-
0.000044
quinoline-2-carboxylic acid [(S)-1-((3R,S)-4-oxotetrahydrofuran-3ylcarbamoyl)-3-methylbutyl]amide
-
-
0.00000004 - 0.000000041
relacatib
0.000000041
relicatib
-
apparent value, pH and temperature not specified in the publication
0.00000016
SB-357114
-
in 100 mM sodium acetate buffer (pH 5.5), at 37°C
0.0000000008 - 0.0000000124
Stefin B
-
0.0000113
STPHPMA-1-(N-benzyloxycarbonylleucyl)-5-(phenylalanylleucyl)carbohydrazide
37°C, pH 5.6
0.033
tert-butyl [(1S)-1-([5-[4-(dimethylamino)phenyl]-1,3,4-oxadiazol-2-yl]carbonyl)butyl]carbamate
-
-
0.00081
tert-butyl [(1S)-1-[(5-thiophen-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamate
-
-
0.0056
tert-butyl [(1S)-1-[[5-(1-methylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamate
-
-
0.017
tert-butyl [(1S)-1-[[5-(2-methoxyphenyl)-1,3,4-oxadiazol-2-yl]carbonyl]butyl]carbamate
-
-
0.000043
tert-butyl [1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]carbamate
-
-
0.00025
[(S)-1-((3R,S)-1-acetyl-4-oxopyrrolidin-3-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
0.00014
[(S)-1-((3R,S)-4-oxotetrahydrofuran-3-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
0.00015
[(S)-1-((4R,S)-3-oxotetrahydropyran-4-ylcarbamoyl)-3-methylbutyl]carbamic acid benzyl ester
-
-
0.000002
((S)-1-[1-[4(R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxoazepan-1-yl]methanoyl]-3-methylbutl)carbamic acid benzyl ester
-
the faster eluting diastereomer C34H46N4O7*0.4H2O
0.000015
((S)-1-[1-[4(R,S)-((S)-2-benzyloxycarbonylamino-4-methylpentanoylamino)-3-oxoazepan-1-yl]methanoyl]-3-methylbutl)carbamic acid benzyl ester
-
the slower eluting diastereomer C34H46N4O7*0.3H2O
0.0000026
cathepsin K propeptide
-
25°C, pH 6
-
0.000147
cathepsin K propeptide
-
25°C, pH 4
-
0.0000000041
cystatin C
-
-
-
0.0000000087
cystatin C
-
Y67L/L205A mutant cathepsin K
-
0.0000000054
H-kininogen
-
-
-
0.0000000145
H-kininogen
-
Y67L/L205A mutant cathepsin K
-
0.0000000049
L-kininogen
-
-
-
0.0000000135
L-kininogen
-
Y67L/L205A mutant cathepsin K
-
0.0000000048
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
0.0000048
N-[(1S)-3-methyl-1-([(4S)-3-oxo-1-[(3-pyridin-2-ylphenyl)acetyl]azepan-4-yl]carbamoyl)butyl]-5-(2-morpholin-4-ylethoxy)-1-benzofuran-2-carboxamide
-
-
0.00000025
N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
Ki: value below 0.00000025 mM
0.0000017
N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]-4-(trifluoromethoxy)benzamide
-
-
0.000001
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
21-24°C, pH 5.5
0.000002
piperidine-4-carboxylic acid [3-methyl-1[1-(naphtho[1,2-d]oxazole-2-carbonyl)-3-phenyl-propylcarbamoyl]-butyl]-amide trifluoroacetate
-
21-24°C, pH 5.5
0.00000004
relacatib
-
pH and temperature not specified in the publication
0.000000041
relacatib
-
pH and temperature not specified in the publication
0.0000000008
Stefin B
-
Y67L/L205A mutant cathepsin K
-
0.0000000124
Stefin B
-
wild-type cathepsin K
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
0.00000028
(11R,12R)-14,14-difluoro-34-(methylsulfanyl)-N-(prop-2-yn-1-yl)-11,12,13,14,15,16-hexahydro[11,21:22,31-terphenyl]-12-carboxamide
Homo sapiens
pH and temperature not specified in the publication
0.0000005
(1R)-1-benzyl-2-methylpropyl [(1S)-1-formylpentyl]carbamate
Homo sapiens
-
-
0.00000033
(1R)-1-benzyl-2-methylpropyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.0000005
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
0.000009
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
0.0000061
(1R,2R)-5,5-dichloro-N-(1-cyanocyclopropyl)-2-[4-[4-(methylsulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000093
(1R,2R)-N-(1-cyanocyclopropyl)-5,5-difluoro-2-[4-[4-(methylsulfonyl)phenyl]-1-(2,2,2-trifluoroethyl)-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000002
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
0.0000004 - 0.00000041
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
0.0000045
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfonyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
0.000005
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
0.000006 - 0.000008
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
0.0000003 - 0.00000032
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
0.0000186
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4-[4-(methylsulfonyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000004 - 0.000005
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
0.0000018
(1S)-1-methyl-2-phenylethyl [(1S)-1-formylpentyl]carbamate
Homo sapiens
-
-
0.00000094
(1S)-1-methyl-2-phenylethyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.0000014
(1S)-1-[(5,6-dichloro-1H-benzimidazol-1-yl)methyl]-2,2-dimethylpropyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
Homo sapiens
-
-
0.0000032
(1S)-1-[(5,6-dichloro-1H-benzimidazol-1-yl)methyl]-2,2-dimethylpropyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0000021
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-([[(6-fluoropyridin-2-yl)carbonyl]amino]acetyl)pentyl]carbamate
Homo sapiens
-
-
0.000018
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
Homo sapiens
-
-
0.000000072
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentyl]carbamate
Homo sapiens
-
-
0.00025
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(morpholin-4-ylcarbonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
value above 0.000250 mM
0.0000004
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.000065
(1S)-2,2-dimethyl-1-([3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
Homo sapiens
-
-
0.0000064
(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0000076
(1S)-2,2-dimethyl-1-([4-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-yl]methyl)propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0000055
(1S)-2,2-dimethyl-1-[(3-pyridin-3-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0000038
(1S)-2,2-dimethyl-1-[(3-pyridin-4-yl-1H-pyrazol-1-yl)methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0003
(1S)-2,2-dimethyl-1-[[3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]propyl [(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamate
Homo sapiens
-
-
0.000032
(1S)-2,2-dimethyl-1-[[3-(trifluoromethyl)-1H-pyrazol-1-yl]methyl]propyl [(1S)-1-[[(pyridin-2-ylsulfonyl)amino]acetyl]pentyl]carbamate
Homo sapiens
-
-
0.0195
(2E,4E)-5-(1-hydroxy-2,6,6-trimethyl-4-oxocyclohex-2-en-1-yl)-3-methylpenta-2,4-dienoic acid
Homo sapiens
pH 5.5, 25°C, collagenase activity, 4.9% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.000028
(2R)-2-[3'-[2-(4-tert-butylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]-N-(cyanomethyl)-4-methylpentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.00001
(2R)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((R)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000172
(2R)-N-(cyanomethyl)-2-[3'-(2-[[3-(dimethylamino)pyrrolidin-1-yl]methyl]-1,3-thiazol-4-yl)biphenyl-3-yl]-4-methylpentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.000043
(2R)-N-(cyanomethyl)-4-methyl-2-[3'-[2-(piperazin-1-ylmethyl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.000003
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(1-piperazinyl)-[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
-
IC 50: 3 nM, reversible inhibition
0.000095
(2R)-N-(cyanomethyl)-4-methyl-2-[4'-(4-methylpiperazin-1-yl)biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.000003
(2R)-N-cyano-4-methyl-2-[4'-(piperazin-1-yl)[1,1'-biphenyl]-3-yl]pentanamide
Homo sapiens
pH and temperature not specified in the publication
0.0012
(2S)-2-(biphenyl-2-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
Homo sapiens
-
-
0.00009
(2S)-2-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
Homo sapiens
-
-
0.0001
(2S)-2-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methylpentanamide
Homo sapiens
-
-
0.0000002
(2S)-4,4-dichloro-N-(1-cyanocyclopropyl)-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
Oryctolagus cuniculus
-
above, humanized rabbit cathepsin K
0.0000069
(2S)-4-fluoro-4-methyl-N-(1-(2-(methylsulfonyl)phenyl)-3-oxopiperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000016
(2S)-4-fluoro-4-methyl-N-(1-(methylsulfonyl)-3-oxoazepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000027
(2S)-4-fluoro-4-methyl-N-(1-(methylsulfonyl)-4-oxopyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000018 - 0.000002
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
0.0000057
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)piperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000083
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-phenylpiperidin-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000033
(2S)-4-fluoro-4-methyl-N-(3-oxoazepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000085
(2S)-4-fluoro-4-methyl-N-(4-oxo-1-(pyridin-2-ylsulfonyl)pyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000098
(2S)-4-fluoro-4-methyl-N-(4-oxopyrrolidin-3-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000159
(2S)-N-(1-(benzylsulfonyl)-3-oxoazepan-4-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000042
(2S)-N-(1-acetyl-4-oxopyrrolidin-3-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000029
(2S)-N-(1-benzoyl-4-oxopyrrolidin-3-yl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0000015
(2S)-N-(1-cyanocyclopropyl)-4,4,4-trifluoro-2-([(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]amino)butanamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.000069
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(3-phenoxyphenoxy)pentanamide
Homo sapiens
-
-
0.0006
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-(4-phenoxyphenoxy)pentanamide
Homo sapiens
-
-
0.003
(2S)-N-[2-[(4-methoxyphenyl)amino]ethyl]-4-methyl-2-phenoxypentanamide
Homo sapiens
-
-
0.0000048
(4-[[(2S)-2-([1-[([1,1'-biphenyl]-3-yl)amino]cyclohexane-1-carbonyl]amino)butyl]amino]phenoxy)acetic acid
Homo sapiens
pH and temperature not specified in the publication
0.0000004
(4R)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000003
(4S)-N-(1-cyanocyclopropyl)-5,5,5-trifluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000002
(S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.0062
1,6-dimethyl-1,2-dihydrophenanthro[1,2-b]furan-10,11-dione
Homo sapiens
pH and temperature not specified in the publication
0.000011
1-(3-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
Homo sapiens
-
pH 5.5, 30°C
0.000024
1-(4-chlorophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
Homo sapiens
-
pH 5.5, 30°C
0.000004
1-(4-cyanophenyl)-3-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]urea
Homo sapiens
-
pH 5.5, 30°C
0.000099
1-(4-cyclohexylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.00013
1-(4-ethylphenoxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.02
1-(biphenyl-2-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
value above 20 mM
0.000082
1-(biphenyl-3-ylamino)-N-[(1R)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000039
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]butyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000056
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]pentyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000027
1-(biphenyl-3-ylamino)-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000019
1-(biphenyl-3-ylamino)-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000083
1-(biphenyl-3-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.00032
1-(biphenyl-3-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0001
1-(biphenyl-4-ylamino)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.00019
1-(biphenyl-4-yloxy)-N-[2-[(4-methoxyphenyl)amino]ethyl]cyclohexanecarboxamide
Homo sapiens
-
-
0.00000035
1-benzylcyclopentyl [(1S)-1-formylpentyl]carbamate
Homo sapiens
-
-
0.00000011
1-benzylcyclopentyl [(1S)-1-[(E)-[(2,3-dihydro-1H-indol-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00002
1-cyano-3-azetidinyl cyclohexylmethyl ether
Homo sapiens
-
IC 50: 20 nM
0.000014
1-Isopropyl-2-methylpropyl (1S)-1-cyclohexylmethyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
Homo sapiens
-
IC50: 14 nM
0.000047
1-Isopropyl-2-methylpropyl (1S)-1-isoprpyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
Homo sapiens
-
IC50: 47 nM
0.00036
1-Isopropyl-2-methylpropyl (1S)-1-methyl-2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
Homo sapiens
-
IC50: 360 nM
0.0000051
1-Isopropyl-2-methylpropyl (1S)-1-[(isoxazol-3-ylamino)(oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 5.1 nM
0.000083
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1,3,4-thiadiazol-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 83 nM
0.00004
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1,3-thiazol-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 40 nM
0.00000077 - 0.000013
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
0.0000048
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(isoquinolin-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 4.8 nM
0.000052
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyrazin-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 52 nM
0.000032
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyridin-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 32 nM
0.000095
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(pyridin-3-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 95 nM
0.00025
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(quinolin-2-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 250 nM
0.000015 - 0.00079
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
0.000062 - 0.0012
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
0.000025 - 0.00047
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
0.00000065 - 0.000012
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
0.00000021 - 0.0000018
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
0.0000092
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 9.2 nM
0.000015 - 0.0011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.000022 - 0.0012
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.00002 - 0.0011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.000026 - 0.0015
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.000039 - 0.0027
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.000017 - 0.001
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.00000041 - 0.000011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
0.000032 - 0.0017
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.00000071
1-Isopropyl-2-methylpropyl (1S)-1-[[(3-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.71 nM
0.00000024
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-bromo-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.24 nM
0.00000091
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-cyano-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.91 nM
0.00000026
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-fluoro-1H-indazol-3-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.26 nM
0.00000047 - 0.0000055
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
0.000062 - 0.0016
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
0.000027 - 0.0017
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
0.000027
1-Isopropyl-2-methylpropyl (1S)-2,3-dioxo--1-phenyl-3-[(thien-2-ylmethyl)-amino]propylcarbamate
Homo sapiens
-
IC50: 27 nM
0.000024
1-Isopropyl-2-methylpropyl (1S)-3-methyl-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]butylcarbamate
Homo sapiens
-
IC50: 24 nM
0.000087
1-Isopropyl-2-methylpropyl (1S,2S)-2-methyl-1-[oxo[(thien-2-ylmethyl)-amino]acetyl]butylcarbamate
Homo sapiens
-
IC50: 87 nM
0.012
1-Isopropyl-2-methylpropyl 2,3-dioxo-3-[(thien-2-ylmethyl)-amino]propylcarbamate
Homo sapiens
-
IC50: 0.012 mM
0.00013
1-methylethyl (2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazinecarboxylate
Homo sapiens
-
-
0.000026
1-[(1H-imidazol-4-yl)methyl]-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole
Homo sapiens
pH and temperature not specified in the publication
0.000006
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-(3-methylphenyl)urea
Homo sapiens
-
pH 5.5, 30°C
0.000025
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-phenylurea
Homo sapiens
-
pH 5.5, 30°C
0.000023
1-[1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]-3-[3-(trifluoromethyl)phenyl]urea
Homo sapiens
-
pH 5.5, 30°C
0.186
13-methyl-2H,10H-[1,3]benzodioxolo[5,6-c][1,3]dioxolo[4,5-i]phenanthridin-13-ium
Homo sapiens
pH 5.5, 25°C, collagenase activity, 14% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.0088 - 0.02724
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-6-[5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl]-2,3-dihydro-4H-1-benzopyran-4-one
0.01
2-(3-methoxyphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.0035
2-(3-methylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000288
2-(3-tert-butylphenyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000026
2-(4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxoazepan-1-ylsulfonyl)pyridine 1-oxide
Homo sapiens
-
-
0.01
2-(biphenyl-3-yl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.00012
2-(cyclohexylamino)pyrimidine-4-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0011
2-(cyclohexylmethyl)-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00000001 - 0.00001
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
0.000000009
2-cyano-4-(cyclohexylamino)-N-[2-(3-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000022 - 0.000022
2-cyano-4-(cyclohexylamino)-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
0.00000075
2-cyano-4-(cyclohexylamino)-N-[2-(4-pyrrolidin-1-ylphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000047 - 0.000047
2-cyano-4-(cyclohexylamino)-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
0.000009
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000000031
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[3-[2-(1H-imidazol-1-yl)ethoxy]-4-methoxyphenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[3-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000013
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[(1-methylpiperidin-4-yl)oxy]phenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000011
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000003 - 0.000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
0.000000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(3-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
value below 0.000000003 mM
0.000000003 - 0.000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
0.0000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-pyrrolidin-1-ylphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000011
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[3-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000000025 - 0.000025
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
0.000034
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000015
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.00013
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.00017
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000038
2-cycloheptyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
2-cycloheptyl-3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00011
2-cycloheptyl-4-[2-(dimethylamino)ethyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0005
2-cycloheptyl-4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000197
2-cyclohexyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00087
2-cyclopentyl-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.01
2-[3-(hydroxymethyl)phenyl]-3,5-dioxo-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.0000062
2-[[2-cyano-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methyl]-N-cyclohexyl-1,3-dioxo-2,8-diazaspiro[4.5]decane-8-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000042
2-[[2-cyano-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methyl]-N-methyl-1,3-dioxo-2,8-diazaspiro[4.5]decane-8-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.009
3,3'-[(3-carboxy-4-oxocyclohexa-2,5-dien-1-ylidene)methylene]bis(6-hydroxybenzoic acid)
Homo sapiens
pH 5.5, 25°C, collagenase activity, 1.7% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.01
3,5-dioxo-2-phenyl-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.000072
3,5-dioxo-2-[3-(propan-2-yl)phenyl]-4-propyl-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00446
3,5-dioxo-4-(2-phenylethyl)-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.012
3,5-dioxo-4-phenyl-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.01
3,5-dioxo-4-propyl-2-[4-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.000182
3,5-dioxo-4-[2-(piperidin-1-yl)ethyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000038
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(propan-2-yl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000017
3,5-dioxo-4-[3-(piperidin-1-yl)propyl]-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000045
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-2-oxopropylcarbamate
Homo sapiens
-
-
0.000068
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxo-N-(phenylsulfonyl)pyrrolidine-1-carboxamide
Homo sapiens
-
-
0.0000073
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxo-N-phenylpyrrolidine-1-carboxamide
Homo sapiens
-
-
0.0000073
3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxamide
Homo sapiens
-
-
0.0000048
3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoic acid
Homo sapiens
-
-
0.00004
3-(benzyloxy)-1-cyanoazetidine
Homo sapiens
-
IC 50: 40 nM
0.001
3-(cyclohexylamino)benzonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
1
3-amino-4-[(tetrahydro-2-furanylmethyl)amino] benzoic acid
Homo sapiens
-
at pH 5.5 and 28°C
0.0001
3-[(benzyloxy)methyl]-1-cyanopyrrolidine
Homo sapiens
-
IC 50: 100 nM
0.0000045
3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoic acid
Homo sapiens
-
-
0.00039
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.0000002
4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl][1,1'-biphenyl]-4-sulfonic acid
Homo sapiens
pH and temperature not specified in the publication
0.0000002
4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl][1,1'-biphenyl]-4-sulfonic acid
Homo sapiens
pH and temperature not specified in the publication
0.000096
4-(3,4-dimethylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000293
4-(3-cyanophenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000457
4-(3-cyclopentylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000181
4-(3-methylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
4-(3-tert-butylphenyl)-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000009
4-(4-acetylpiperazin-1-yl)-5-amino-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000001 - 0.000004
4-(cyclohexylamino)-6-(piperazin-1-yl)-1,3,5-triazine-2-carbonitrile
0.00017
4-(cyclohexylamino)pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000132
4-(dimethylamino)-N-[1-([(1S)-1-[(5-furan-2-yl-1,3,4-oxadiazol-2-yl)carbonyl]butyl]carbamoyl)cyclohexyl]benzamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.001
4-benzyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0074
4-butyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000084
4-cycloheptyl-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
4-cycloheptyl-6-[3-(piperidin-1-yl)propyl]pyrimidine-2-carbonitrile
0.00068
4-cyclohexyl-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000011
4-cyclooctyl-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.002
4-cyclopentyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0113 - 0.015
4-dihydrotanshinone
0.0025
4-ethyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000033
4-fluoro-N-(3-oxoazepan-4-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000098
4-fluoro-N-(4-oxopyrrolidin-3-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000083
4-fluoro-N-(5-oxo-2-phenylpiperidin-4-yl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.00029
4-fluoro-N-prop-2-yn-1-yl-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
0.000016
4-fluoro-N-[1-(methylsulfonyl)-3-oxoazepan-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000027
4-fluoro-N-[1-(methylsulfonyl)-4-oxopyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000069
4-fluoro-N-[2-[2-(methylsulfonyl)phenyl]-5-oxopiperidin-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000002
4-fluoro-N-[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000057
4-fluoro-N-[3-oxo-1-(pyridin-2-ylsulfonyl)piperidin-4-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000073
4-fluoro-N-[4-oxo-1-(phenylcarbamoyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000029
4-fluoro-N-[4-oxo-1-(phenylcarbonyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000085
4-fluoro-N-[4-oxo-1-(pyridin-2-ylsulfonyl)pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000068
4-fluoro-N-[4-oxo-1-[(phenylsulfonyl)carbamoyl]pyrrolidin-3-yl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.00478
4-methyl-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000985
4-phenyl-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.004074
4-propyl-6-[2-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000033
4-propyl-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-propyl-6-[4-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000019
4-[(2,2-dimethylpropyl)(4-iodobenzyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000071
4-[(2,2-dimethylpropyl)amino]-5-(3-[4-[(4-methoxyphenyl)sulfonyl]piperazin-1-yl]prop-1-yn-1-yl)pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000086
4-[(2,2-dimethylpropyl)amino]-5-[3-(pyridin-3-yloxy)prop-1-yn-1-yl]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000071
4-[(2,2-dimethylpropyl)amino]-5-[3-[4-(4-methylpiperazin-1-yl)phenyl]prop-1-yn-1-yl]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000048
4-[(2,2-dimethylpropyl)[4-(1H-1,2,4-triazol-1-ylmethyl)benzyl]amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000073
4-[(2,2-dimethylpropyl)[4-(3-piperidin-1-ylprop-1-yn-1-yl)benzyl]amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000086
4-[(2,2-dimethylpropyl)[4-[3-(1H-1,2,4-triazol-1-yl)prop-1-yn-1-yl]benzyl]amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000038
4-[(2,2-dimethylpropyl)[4-[3-(4-methylpiperazin-1-yl)prop-1-yn-1-yl]benzyl]amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00024
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.0000048
4-[2-(4-methylpiperazin-1-yl)-4,5-dihydro-1,3-thiazol-4-yl]-N-(1-[[(3S,4R)-2-oxo-4-phenoxyazetidin-3-yl]carbamoyl]cyclohexyl)benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00081
4-[2-(dimethylamino)ethyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001
4-[2-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
4-[3-(dimethylamino)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000148
4-[3-(methylsulfonyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000112
4-[3-(morpholin-4-yl)propyl]-3,5-dioxo-2-[3-(trifluoromethyl)phenyl]-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
4-[3-(pentan-3-ylamino)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
4-[3-(piperidin-1-yl)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00001
4-[3-(tert-butylamino)propyl]-6-[3-(trifluoromethyl)phenyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000034
4-[4-chloro-3-(trifluoromethyl)phenyl]-6-propylpyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000069
4-[benzyl(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00028
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.0000036
4-[[4-[3-(1,4'-bipiperidin-1'-yl)prop-1-yn-1-yl]benzyl](2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000064
4-[[4-[3-(4-acetylpiperazin-1-yl)prop-1-yn-1-yl]benzyl](2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000037
5-(3-[4-[(3-chloropropyl)sulfonyl]piperazin-1-yl]prop-1-yn-1-yl)-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000032
5-amino-4-(3-hydroxyazetidin-1-yl)-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000002
5-amino-4-(bicyclo[2.2.1]hept-2-ylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000023
5-amino-4-(cyclohexylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000013
5-amino-4-(cyclopentylamino)-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00011
5-amino-4-morpholin-4-yl-6-(phenylamino)pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00034
5-amino-4-morpholin-4-yl-6-(tetrahydrofuran-3-ylamino)pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00006
5-amino-4-morpholin-4-yl-6-piperidin-1-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000022
5-amino-4-morpholin-4-yl-6-pyrrolidin-1-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000014
5-amino-4-[(1,1-dioxidotetrahydrothiophen-3-yl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.00056
5-amino-4-[(1-methylethyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0003
5-amino-4-[(1-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000017
5-amino-4-[(2,2-dimethylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000024
5-amino-4-[(2-methoxyethyl)amino]-6-[(2-methylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000018
5-amino-4-[(2-methylpropyl)amino]-6-morpholin-4-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000006
5-amino-4-[(2-methylpropyl)amino]-6-piperazin-1-ylpyrimidine-2-carbonitrile
Homo sapiens
-
-
0.000062
5-amino-4-[(2-methylpropyl)amino]-6-[(tetrazolidin-5-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0001
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.00001
5-[3-(1,3-dihydro-2H-isoindol-2-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000032
5-[3-(3,4-dihydroisoquinolin-2(1H)-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000072
5-[3-(4,5-dichloro-1H-imidazol-1-yl)prop-1-yn-1-yl]-4-[(2,2-dimethylpropyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.075
6,8-dihydroxy-3-(3,4,5-trihydroxyphenyl)-2,3-dihydro-1,4-benzodioxin-2-yl 3,4,5-trihydroxybenzoate
Homo sapiens
pH 5.5, 25°C, collagenase activity, 12% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.000001
6-(4-chlorobenzyl)-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.001
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.00022 - 0.0022
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.001
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000017
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.0001 - 0.00011
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000001
6-(4-chlorobenzyl)-7-(3,3,3-trifluoropropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.001
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0001
6-(4-chlorobenzyl)-7-(4,4,4-trifluorobutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.0000023
6-(4-chlorobenzyl)-7-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.001
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.001
6-(4-chlorobenzyl)-7-[2-(piperidin-1-yl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.000014
6-(cyclohexylamino)-9-[(2S,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl]-9H-purine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
6-(cyclohexylamino)-9-[2-(4-methylpiperazin-1-yl)ethyl]-9H-purine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.001
6-(cyclohexylamino)pyrazine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.001
6-(cyclohexylamino)pyridine-2-carbonitrile
Homo sapiens
-
IC50 above 0.001 mM, pH and temperature not specified in the publication
0.0000012
6-benzyl-7-(2,2,2-trifluoroethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000015
6-benzyl-7-cyclohexyl-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.002
6-cyano-2-(3-trifluoromethyl-phenyl)-3,5-dioxo-1,2,4-triazine
Homo sapiens
-
pH and temperature not specified in the publication
0.0000065
6-[(1'-acetyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
6-[(4,5-dichloro-1H-imidazol-1-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000004
6-[(5,5-dimethyl-2,4-dioxo-1,3-oxazolidin-3-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000027
6-[(8-acetyl-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
6-[(8-benzyl-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001
6-[4-[(diethylamino)methyl]benzyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.00029
6-[[4-(4-acetyl-1,4-diazepan-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.0059
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.00165
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.000079
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.0054
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.0000054
6-[[8-(2,4-dimethoxyphenyl)-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl]methyl]-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001 - 0.00003
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
0.000005
7-(2,2-dimethylpropyl)-6-(1H-1,2,3-triazol-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000006
7-(2,2-dimethylpropyl)-6-(1H-imidazol-1-ylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000002
7-(2,2-dimethylpropyl)-6-[(1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[(1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[(1,3-dioxo-2,8-diazaspiro[4.5]decan-2-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
IC50 below 1 nM, pH and temperature not specified in the publication
0.000001 - 0.000076
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000001 - 0.000027
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000001
7-(2,2-dimethylpropyl)-6-[(2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001 - 0.000012
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.0000017
7-(2,2-dimethylpropyl)-6-[(5-fluoro-1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000017 - 0.0000078
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.0000019
7-(2,2-dimethylpropyl)-6-[(5-methoxy-1'-methyl-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001 - 0.000044
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
0.000003
7-(2,2-dimethylpropyl)-6-[(pyridin-4-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[4-(4-methylpiperazin-1-yl)benzyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[4-(morpholin-4-yl)benzyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.0000017
7-(2,2-dimethylpropyl)-6-[[2-oxo-1'-(propan-2-yl)spiro[indole-3,4'-piperidin]-1(2H)-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[[4-(4-fluorophenyl)piperazin-1-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000022
7-(2,2-dimethylpropyl)-6-[[8-(morpholin-4-ylacetyl)-1,3-dioxo-2,8-diazaspiro[4.5]dec-2-yl]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00028
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00025
7-(2-cyclohexylethyl)-6-[(pyridin-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00048
7-(2-cyclohexylethyl)-6-[(pyridin-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.0143
acetyl-strophanthidin
Homo sapiens
pH 5.5, 25°C, collagenase activity, 5.4% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.0000006 - 0.00048
balicatib
0.00004
benzyl 1-cyano-3-pyrrolidinylcarbamate
Homo sapiens
-
IC 50: 40 nM
0.0000006 - 0.000044
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
0.000163 - 0.002106
BML-244
0.000013 - 0.000296
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
0.00066 - 0.00071
carbobenzyloxy-Phe-Phe-CH2F
Homo sapiens
-
pH 5.5, 22°C, recombinant enzyme, dependent on the substrate
0.000181 - 0.00426
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
0.088
ellipticine
Homo sapiens
pH 5.5, 25°C, 4.0% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.0016
ethyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
Homo sapiens
-
-
0.0000016
ethyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
Oryctolagus cuniculus
-
-
0.000054
ethyl 4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxoazepane-1-carboxylate
Homo sapiens
-
-
0.000009
ethyl 4-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-3-oxopiperidine-1-carboxylate
Homo sapiens
-
-
0.000054
ethyl 4-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-3-oxoazepane-1-carboxylate
Oryctolagus cuniculus
-
-
0.000009
ethyl 4-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-5-oxopiperidine-2-carboxylate
Oryctolagus cuniculus
-
-
0.0000017
Ethyl 5-[((3S)-3[[(isopropyl-2-methylpropoxy)carbonyl]amide]-2-oxoheptanoyl)amino]-1H-pyrazole-4-carboxylate
Homo sapiens
-
IC50: 1.7 nM
0.00047
ethyl N-[[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]-b-alaninate
Homo sapiens
-
-
0.00052
ethyl N-[[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]glycinate
Homo sapiens
-
-
0.00879
kushennol F
Homo sapiens
pH and temperature not specified in the publication
0.0000002
L-13006235
Oryctolagus cuniculus
-
-
0.0000002 - 0.004807
L-873724
0.0000043
methyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
Homo sapiens
-
-
0.0000043
methyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
Oryctolagus cuniculus
-
-
0.000001
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-fluoro-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000003
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2,2-trifluoroethyl]biphenyl-4-sulfinate
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000008
methyl 4'-[(1S)-1-([(2S)-1-[(1-cyanocyclopropyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000003
methyl 4'-[(1S)-1-([(2S)-1-[(cyanomethyl)amino]-4-methyl-1-oxopentan-2-yl]amino)-2,2-difluoroethyl]biphenyl-4-sulfinate
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0335 - 0.037
methyl 5-acetoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
Homo sapiens
-
pH 5.5, 22°C, recombinant enzyme, dependent on the substrate
0.000021
methyl 5-hydroxy-7,12-dioxo-7,12-dihydrodinaphtho[1,2-b:2',3'-d]furan-6-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.0215 - 0.028
methyl 5-hydroxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
Homo sapiens
-
pH 5.5, 22°C, recombinant enzyme, dependent on the substrate
0.045 - 0.067
methyl 5-methoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
Homo sapiens
-
pH 5.5, 22°C, recombinant enzyme, dependent on the substrate
0.04 - 0.042
methyl 5-propoxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
Homo sapiens
-
pH 5.5, 22°C, recombinant enzyme, dependent on the substrate
0.000027
methyl N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninate
Homo sapiens
-
-
0.00018
methyl [[(2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazino]carbonyl]carbamate
Homo sapiens
-
-
0.0000023 - 0.000018
Mu-Leu-Hph-fluoromethylketone
0.000023
MV061606
Homo sapiens
-
pH and temperature not specified in the publication
-
0.00000016
N-((S)-4-methyl-1-oxo-1-((S)-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-ylamino)pentan-2-yl)benzofuran-2-carboxamide
Homo sapiens
-
-
0.0000024 - 0.000028
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
0.0000042
N-(1-acetyl-4-oxopyrrolidin-3-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000073
N-(1-carbamoyl-4-oxopyrrolidin-3-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000004
N-(1-cyano-1-methylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000006 - 0.0000051
N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
0.00037
N-(1-cyano-3-pyrrolidinyl)benzamide
Homo sapiens
-
IC 50: 370 nM
0.00029
N-(1-cyano-3-pyrrolidinyl)[1,1'-biphenyl]-4-carboxamide
Homo sapiens
-
IC 50: 290 nM
0.00005
N-(1-cyano-3pyrrolidinyl)benzenesulfonamide
Homo sapiens
-
IC 50: 50 nM
0.0000002
N-(1-cyanocyclopropyl)-4,4-difluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-norvalinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000002
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(1-hydroxycyclopropyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000021
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(1-hydroxycyclopropyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000002
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2-hydroxypropan-2-yl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000002
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-(4-methyl-4,5-dihydro-1,3-thiazol-2-yl)phenyl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000003
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-(quinolin-6-yl)phenyl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000003
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-[5-(1-hydroxycyclopropyl)pyridin-2-yl]phenyl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000004
N-(1-cyanocyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4-[6-(methylsulfonyl)pyridin-3-yl]phenyl]ethyl]-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000004
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1R)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000004
N-(1-cyanocyclopropyl)-N2-[(1S)-1-[4'-[(1S)-2,2-difluoro-1-hydroxyethyl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-4-fluoro-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000016
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000019
N-(1-cyanocyclopropyl)-N2-[(1S)-2,2-difluoro-1-[4'-(2,2,2-trifluoro-1-hydroxyethyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.026
N-(1-ethynylcyclopropyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
0.000009
N-(2,3-dichlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: 9 nM
0.000006
N-(2-chlorophenyl)triazolyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: 6 nM
0.000047
N-(3-bromoprop-2-yn-1-yl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
0.00014
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000001
N-(4-chlorophenyl)-2-methylalanyl-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-L-leucinamide
Homo sapiens
-
IC50 is below 1 nM
0.000003
N-(5-isopropyl)pyridine-2-carboxyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: less than 3 nM
0.00000057
N-(cyanomethyl)-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
0.000349
N-(cyanomethyl)-4-methyl-2-[3'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.000059
N-(cyanomethyl)-4-methyl-2-[3'-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.000012
N-(cyanomethyl)-4-methyl-2-[4'-(2-piperazin-1-yl-1,3-thiazol-4-yl)biphenyl-3-yl]pentanamide
Homo sapiens
-
IC50: in vitro bone resorption assay
0.0000002
N-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000000005
N-(cyanomethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(piperazin-1-yl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
IC50 below 5 pM, pH and temperature not specified in the publication
0.000006
N-4-benzyloxybenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: 6 nM
0.000003
N-4-isopropylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: less than 3 nM
0.000003
N-4-propylbenzoyl-L-leucine-(2-(4-methoxy)phenylaminoethyl)amide
Homo sapiens
-
IC50: less than 3 nM
0.000015
N-benzyl-3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxamide
Homo sapiens
-
-
0.00035
N-but-3-yn-2-yl-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methanesulfonyl)[1,1'-biphenyl]-4-yl]ethyl]-L-leucinamide
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
0.0000002
N-cyano-N2-[4-[4-(piperazin-1-yl)phenyl]thiophen-3-yl]-L-leucinamide
Homo sapiens
pH and temperature not specified in the publication
0.013
N-[(1-cyano-2-pyrrolidinyl)methyl]benzamide
Homo sapiens
-
IC 50: 0.013 mM
0.012
N-[(1-cyano-2-pyrrolidinyl)methyl]benzenesulfonamide
Homo sapiens
-
IC 50: 0.012 mM
0.00007
N-[(1-cyano-3-azetidinyl)methyl]benzamide
Homo sapiens
-
IC 50: 70 nM
0.00002
N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide
Homo sapiens
-
IC 50: 20 nM
0.000005
N-[(1-cyano-3-azetidinyl)methyl]cyclohexanecarboxamide
Homo sapiens
-
IC 50: 5 nM
0.0002
N-[(1-cyano-3pyrrolidinyl)methyl]benzenesulfonamide
Homo sapiens
-
IC 50: 200 nM
0.000044
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.00019
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(2-methyl-1H-imidazol-1-yl)acetyl]-L-leucinamide
Homo sapiens
-
IC50: 190 nM
0.000084
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(4-phenylpiperidin-1-yl)acetyl]-L-leucinamide
Homo sapiens
-
IC50: 84 nM
0.000009
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(4-pyridin-4-ylpiperazin-1-yl)acetyl]-L-leucinamide
Homo sapiens
-
IC50: 9 nM
0.000024
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[(5-methyl-1H-imidazol-4-yl)acetyl]-L-leucinamide
Homo sapiens
-
IC50: 24 nM
0.000001
N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-N2-[2-(4-chlorophenoxy)-2-methylpropanoyl]-L-leucinamide
Homo sapiens
-
IC50 is below 1 nM
0.000001
N-[(1S)-1-([(1R)-2-(benzyloxy)-1-cyanoethyl]carbamoyl)-3-methylbutyl]-1-methyl-1H-indole-2-carboxamide
Homo sapiens
-
IC50 is below 1 nM
0.00043
N-[(1S)-1-([(1R)-2-(benzyloxy)-1-cyanoethyl]carbamoyl)-3-methylbutyl]-1H-indole-2-carboxamide
Homo sapiens
-
IC50: 430 nM
0.0002
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000151
N-[(1S)-1-carbamoyl-3-(methylsulfonyl)propyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000273
N-[(1S)-1-carbamoyl-3-phenylpropyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.0000006
N-[(1S)-1-cyano-2-phenylethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.0000002
N-[(1S)-1-cyano-3-(methylsulfanyl)propyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.0000009 - 0.0000012
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
0.000041
N-[(1S)-1-[2-(methylsulfanyl)ethyl]-2-oxopropyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000109
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-3-(methylsulfonyl)-L-alaninamide
Homo sapiens
-
-
0.000174
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-alaninamide
Homo sapiens
-
-
0.000013
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methioninamide
Homo sapiens
-
-
0.00012
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-methionine
Homo sapiens
-
-
0.00001
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-L-phenylalaninamide
Homo sapiens
-
-
0.000277
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-(2,2,2-trifluoroethyl)-L-methioninamide
Homo sapiens
-
-
0.000238
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-(methylsulfonyl)-L-methioninamide
Homo sapiens
-
-
0.000087
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-benzyl-L-methioninamide
Homo sapiens
-
-
0.001045
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-dimethyl-L-methioninamide
Homo sapiens
-
-
0.000067
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-N-methyl-L-methioninamide
Homo sapiens
-
-
0.000066
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl-S-methyl-L-cysteinamide
Homo sapiens
-
-
0.000238
N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucylglycinamide
Homo sapiens
-
-
0.0000075
N-[(1S)-3-methyl-1-([(1S)-1-methyl-2-oxo-3-[(pyridin-2-ylsulfonyl)amino]propyl]carbamoyl)butyl]-1-benzofuran-2-carboxamide
Homo sapiens
-
-
0.000016
N-[(1S)-3-methyl-1-[[3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]carbamoyl]butyl]-1-benzofuran-2-carboxamide
Oryctolagus cuniculus
-
-
0.0000068
N-[(2S)-1-[4-(benzyloxy)anilino]butan-2-yl]-N2-(morpholine-4-carbonyl)-L-leucinamide
Homo sapiens
pH and temperature not specified in the publication
0.000003
N-[(2S)-4-methyl-1-([2-[4-(2-methylpropoxy)anilino]ethyl]amino)-1-oxopentan-2-yl]-2,3-dihydro-1-benzofuran-2-carboxamide
Homo sapiens
IC50 below 3 nM, pH and temperature not specified in the publication
0.000015
N-[1-(benzylcarbamoyl)-4-oxopyrrolidin-3-yl]-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.000159
N-[1-(benzylsulfonyl)-3-oxoazepan-4-yl]-4-fluoro-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
-
0.0000014
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide
Homo sapiens
pH and temperature not specified in the publication
0.0000002
N-[1-[(cyanomethyl)carbamoyl]cyclohexyl]-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.011
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-(phenylamino)cyclohexanecarboxamide
Homo sapiens
-
-
0.003
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-phenoxycyclohexanecarboxamide
Homo sapiens
-
-
0.0002
N-[2-[(4-methoxyphenyl)amino]ethyl]-1-[4-(1-methylethyl)phenoxy]cyclohexanecarboxamide
Homo sapiens
-
-
0.000016
N-[cyano(dicyclobutyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000003
N-[cyano(dicyclopropyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000006
N-[cyano(phenyl)methyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.00006
N2-(3-cyclohexylphenyl)-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000011
N2-biphenyl-3-yl-N-[(1S)-1-[([4-[2-(1H-tetrazol-5-yl)ethoxy]phenyl]amino)methyl]propyl]-L-leucinamide
Homo sapiens
-
-
0.0000038
N2-biphenyl-3-yl-N-[(1S)-1-[[(4-methoxyphenyl)amino]methyl]propyl]-L-leucinamide
Homo sapiens
-
-
0.00001
N2-biphenyl-3-yl-N-[(1S)-2-[(4-methoxyphenyl)amino]-1-methylethyl]-L-leucinamide
Homo sapiens
-
-
0.00004
N2-biphenyl-3-yl-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
Homo sapiens
-
-
0.0000003
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000003
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)-2'-fluorobiphenyl-4-yl]-2,2-difluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.0000005
N2-[(1S)-1-[4'-(1-carbamoylcyclopropyl)biphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000002
N2-[(1S)-1-[4'-(2-amino-2-oxoethyl)[1,1'-biphenyl]-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Homo sapiens
pH and temperature not specified in the publication
0.0000002
N2-[(1S)-1-[4'-[(2S)-1-amino-1-oxopropan-2-yl]biphenyl-4-yl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000002
N2-[(1S)-1-[4-[5-(1-carbamoylcyclopropyl)pyridin-2-yl]phenyl]-2,2,2-trifluoroethyl]-N-(1-cyanocyclopropyl)-4-fluoro-L-leucinamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000043
N2-[(benzyloxy)carbonyl]-N-((1S)-1-cyano-2-[4-(trifluoromethyl)phenyl]ethyl)-L-leucinamide
Homo sapiens
-
IC50: 43 nM
0.000009
N2-[(benzyloxy)carbonyl]-N-[(1R)-2-(benzyloxy)-1-cyanoethyl]-L-leucinamide
Homo sapiens
-
IC50: 9 nM
0.00024
N2-[(benzyloxy)carbonyl]-N-[(1R)-2-tert-butoxy-1-cyanoethyl]-L-leucinamide
Homo sapiens
-
IC50: 240 nM
0.00012
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(3-methylphenyl)ethyl]-L-leucinamide
Homo sapiens
-
IC50: 120 nM
0.000063
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(4-methoxyphenyl)ethyl]-L-leucinamide
Homo sapiens
-
IC50: 63 nM
0.000048
N2-[(benzyloxy)carbonyl]-N-[(1S)-1-cyano-2-(4-methylphenyl)ethyl]-L-leucinamide
Homo sapiens
-
IC50: 48 nM
0.000398
N2-[(benzyloxy)carbonyl]-N-[(1S)-2-(4-tert-butoxyphenyl)-1-cyanoethyl]-L-leucinamide
Homo sapiens
-
IC50: 398 nM
0.00009
N2-[(benzyloxy)carbonyl]-N-[2-[(4-methoxyphenyl)amino]ethyl]-L-leucinamide
Homo sapiens
-
-
0.000064
Nalpha-4-methoxybenzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
Oryctolagus cuniculus
-
IC50: 64 nM
0.00047
Nalpha-benzyloxycarbonyl-L-leucine(2-phenylaminoethyl)amide
Oryctolagus cuniculus
-
IC50: 470 nM
0.000046 - 0.000319
NC-2300
0.08
NSC13345
Homo sapiens
at pH 5.5 and 25°C
0.0000002 - 0.00105
odanacatib
0.000047
Phe-Phe-fluoromethylketone
Homo sapiens
pH and temperature not specified in the publication
0.5
piperidin-2-yl-[2-(trifluoromethyl)-6-[4-(trifluoromethyl)phenyl]pyridin-4-yl] methanol
Homo sapiens
-
at pH 5.5 and 28°C
0.0000007 - 0.000066
relacatib
0.00083
S-(1-methylethyl) (2E)-2-[(2S)-2-[(tert-butoxycarbonyl)amino]hexylidene]hydrazinecarbothioate
Homo sapiens
-
-
0.08
S-[2-[2-(dihydroxymethyl)anilino]-2-oxoethyl] carbamothioate
Homo sapiens
pH and temperature not specified in the publication
0.0093
sclareol
Homo sapiens
pH 5.5, 25°C, 3.7% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.0000345
sodium (2S,3S)-3-[[(2S)-4-methyl-1-(2-methylpropoxy)pentan-2-yl]amino]oxirane-2-carboxylate
Homo sapiens
pH and temperature not specified in the publication
0.0272
sophoraflavanone G
Homo sapiens
pH and temperature not specified in the publication
0.005
suramin
Homo sapiens
pH 5.5, 25°C, 16.0% inhibition of activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin as substrate, no inhibition with gelatin as substrate
0.000055
tert-butyl ([1-[(2-cyanotetrahydropyridazin-1(2H)-yl)carbonyl]-2-methylpropyl]carbamoyl)carbamate
Homo sapiens
-
pH 5.5, 30°C
0.0000039
tert-butyl 3-((S)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamido)-4-oxopyrrolidine-1-carboxylate
Homo sapiens
-
-
0.0000048
tert-butyl 3-(4-[[(2S)-2-([[1-(biphenyl-3-ylamino)cyclohexyl]carbonyl]amino)butyl]amino]phenoxy)propanoate
Homo sapiens
-
-
0.0000039
tert-butyl 3-[(4-fluoro-N-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucyl)amino]-4-oxopyrrolidine-1-carboxylate
Oryctolagus cuniculus
-
-
0.0000064
tert-butyl 3-[4-([(2S)-2-[(N-biphenyl-3-yl-L-leucyl)amino]butyl]amino)phenoxy]propanoate
Homo sapiens
-
-
0.000051
tert-butyl [(1S)-1-formylpentyl]carbamate
Homo sapiens
-
-
0.00047
tert-butyl [(1S)-1-[(E)-(4,5-dihydro-1,3-thiazol-2-ylhydrazono)methyl]pentyl]carbamate
Homo sapiens
-
-
0.033
tert-butyl [(1S)-1-[(E)-(carbamimidoylhydrazono)methyl]pentyl]carbamate
Homo sapiens
-
-
0.00035
tert-butyl [(1S)-1-[(E)-(carbamoylhydrazono)methyl]pentyl]carbamate
Homo sapiens
-
-
0.000048
tert-butyl [(1S)-1-[(E)-[(2,3-dihydro-1H-indol-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000093
tert-butyl [(1S)-1-[(E)-[(3,4-dihydroisoquinolin-2(1H)-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000059
tert-butyl [(1S)-1-[(E)-[(3,4-dihydroquinolin-1(2H)-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.0002
tert-butyl [(1S)-1-[(E)-[(3-methylbutanoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
IC50: 0.00016 mM (after addition of the semicarbazide in 15fold excess at pH 5.5) 0.011 mM (after addition of the semicarbazide in 15fold excess at pH 7.0)
0.00041
tert-butyl [(1S)-1-[(E)-[(benzylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00004
tert-butyl [(1S)-1-[(E)-[(diethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
IC50: 0.000047 mM (after addition of the semicarbazide in 15fold excess at pH 5.5) 0.0018 mM (after addition of the semicarbazide in 15fold excess at pH 7.0)
0.000072
tert-butyl [(1S)-1-[(E)-[(dimethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000072
tert-butyl [(1S)-1-[(E)-[(dimethylsulfamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
IC50: 0.00022 mM (after addition of the semicarbazide in 15fold excess at pH 5.5) 0.0019 mM (after addition of the semicarbazide in 15fold excess at pH 7.0)
0.00049
tert-butyl [(1S)-1-[(E)-[(ethylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
IC50: 0.0009 mM (after addition of the semicarbazide in 15fold excess at pH 5.5) above 0.013 mM (after addition of the semicarbazide in 15fold excess at pH 7.0)
0.00028
tert-butyl [(1S)-1-[(E)-[(methylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000035
tert-butyl [(1S)-1-[(E)-[(morpholin-4-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
IC50: 0.00005 mM (after addition of the semicarbazide in 15fold excess at pH 5.5) 0.0021 mM (after addition of the semicarbazide in 15fold excess at pH 7.0)
0.0004
tert-butyl [(1S)-1-[(E)-[(phenylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00022
tert-butyl [(1S)-1-[(E)-[(phenylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000058
tert-butyl [(1S)-1-[(E)-[(piperidin-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000036
tert-butyl [(1S)-1-[(E)-[(pyrrolidin-1-ylcarbonyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00016
tert-butyl [(1S)-1-[(E)-[(tert-butylcarbamoyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000024
tert-butyl [(1S)-1-[(E)-[(trifluoroacetyl)hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.011
tert-butyl [(1S)-1-[(E)-[methyl[(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00052
tert-butyl [(1S)-1-[(E)-[methyl[methyl(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00017
tert-butyl [(1S)-1-[(E)-[[(1-methylethyl)carbamothioyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00017
tert-butyl [(1S)-1-[(E)-[[(1-methylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.00026
tert-butyl [(1S)-1-[(E)-[[(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.0011
tert-butyl [(1S)-1-[(E)-[[(morpholin-4-ylcarbonyl)oxy]imino]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000045
tert-butyl [(1S)-1-[(E)-[[methyl(2-phenylethyl)carbamoyl]hydrazono]methyl]pentyl]carbamate
Homo sapiens
-
-
0.000001
[1-(2-cyano-tetrahydro-pyridazine-1-carbonyl)-2-methyl-propyl]-carbamic acid benzyl ester
Homo sapiens
-
pH 5.5, 30°C
additional information
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetic acid
0.0000005
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000005
(1R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000009
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
Homo sapiens
-
-
0.000009
(1R,2R)-2-[1-benzyl-5-[4-(methylsulfanyl)phenyl]-1H-1,2,3-triazol-4-yl]-N-(cyanomethyl)-5,5-difluorocyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000002
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
Homo sapiens
-
-
0.000002
(1R,2R)-N-(cyanomethyl)-2-(4-[4-[(difluoromethyl)sulfanyl]phenyl]pyridin-3-yl)-5,5-difluorocyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000004
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000004
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.00000041
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[1-methyl-4-[4-(methylsulfanyl)phenyl]-1H-pyrazol-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-methyl-4-[4-(methylsulfanyl)phenyl]-1,3-thiazol-5-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[2-[4-(methylsulfanyl)phenyl]pyridin-3-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000005
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000005
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-1-oxidopyridin-4-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000006
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000008
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000001
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[3-[4-(methylsulfanyl)phenyl]pyridin-4-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000003
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.0000003
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.00000032
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[4'-(methylsulfanyl)biphenyl-2-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.000004
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
Homo sapiens
-
-
0.000005
(1R,2R)-N-(cyanomethyl)-5,5-difluoro-2-[5-[4-(methylsulfanyl)phenyl]-2-oxo-1,2-dihydropyridin-4-yl]cyclohexanecarboxamide
Oryctolagus cuniculus
-
-
0.0000018
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
-
0.000002
(2S)-4-fluoro-4-methyl-N-(3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
Homo sapiens
-
racemate
0.00000077
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.77 nM
0.000013
1-Isopropyl-2-methylpropyl (1S)-1-[oxo(1H-pyrazol-5-ylamino)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 13 nM
0.000015
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 15 nM
0.00079
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 790 nM
0.000062
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 62 nM
0.0012
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-2-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0012 mM
0.000025
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 25 nM
0.00047
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(1-pyridin-4-yl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 470 nM
0.00000065
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.65 nM
0.000012
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(3-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 12 nM
0.00000021
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.21 nM
0.0000018
1-Isopropyl-2-methylpropyl (1S)-1-[oxo[(4-phenyl-1H-pyrazol-5-yl)amino]acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 1.8 nM
0.000015
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 15 nM
0.0011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0011 mM
0.000022
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 22 nM
0.0012
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclohexyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0012 mM
0.00002
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 20 nM
0.0011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-cyclopentyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0011 mM
0.000026
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 26 nM
0.0015
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-ethyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0015 mM
0.000039
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 39 nM
0.0027
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isobutyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0027 mM
0.000017
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 17 nM
0.001
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-isopropyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.001 mM
0.00000041
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.41 nM
0.000011
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-3-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 11 nM
0.000032
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 32 nM
0.0017
1-Isopropyl-2-methylpropyl (1S)-1-[[(1-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0017 mM
0.00000047
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 0.47 nM
0.0000055
1-Isopropyl-2-methylpropyl (1S)-1-[[(4-methyl-1H-pyrazol-5-yl)amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 5.5 nM
0.000062
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 62 nM
0.0016
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(3,3-dimethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0016 mM
0.000027
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
Homo sapiens
-
IC50: 27 nM
0.0017
1-Isopropyl-2-methylpropyl (1S)-1-[[[1-(cyclopropylmethyl)-1H-pyrazol-5-yl]amino](oxo)acetyl]pentylcarbamate
Rattus norvegicus
-
IC50: 0.0017 mM
0.0088
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-6-[5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl]-2,3-dihydro-4H-1-benzopyran-4-one
Homo sapiens
pH and temperature not specified in the publication
0.02724
2-(2,4-dihydroxyphenyl)-5,7-dihydroxy-6-[5-methyl-2-(prop-1-en-2-yl)hex-4-en-1-yl]-2,3-dihydro-4H-1-benzopyran-4-one
Homo sapiens
pH and temperature not specified in the publication
0.00000001
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.00001
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition is determined by a fluorometric assay with recombinant Cat K
0.000000022
2-cyano-4-(cyclohexylamino)-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000022
2-cyano-4-(cyclohexylamino)-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000000047
2-cyano-4-(cyclohexylamino)-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000047
2-cyano-4-(cyclohexylamino)-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-(2-[4-[2-(1H-imidazol-1-yl)ethoxy]phenyl]ethyl)pyrimidine-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
value below 0.000000003 mM
0.000003
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-(4-methoxyphenyl)ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
IC50 less than 0.000003 mM, pH and temperature not specified in the publication
0.000000025
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
-
0.000025
2-cyano-4-[(2,2-dimethylpropyl)amino]-N-[2-[4-(4-methylpiperazin-1-yl)phenyl]ethyl]pyrimidine-5-carboxamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
4-(cyclohexylamino)-6-(piperazin-1-yl)-1,3,5-triazine-2-carbonitrile
Homo sapiens
pH and temperature not specified in the publication
0.000004
4-(cyclohexylamino)-6-(piperazin-1-yl)-1,3,5-triazine-2-carbonitrile
Homo sapiens
pH and temperature not specified in the publication
0.0001
4-cycloheptyl-6-[3-(piperidin-1-yl)propyl]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
4-cycloheptyl-6-[3-(piperidin-1-yl)propyl]pyrimidine-2-carbonitrile
Homo sapiens
pH and temperature not specified in the publication
0.0113
4-dihydrotanshinone
Homo sapiens
with elastin as substrate, at pH 5.5 and 37°C
0.015
4-dihydrotanshinone
Homo sapiens
with collagen type I as substrate, at pH 5.5 and 37°C
0.00022
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0022
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000017
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000017
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0001
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.00011
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000006
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.000001
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.00003
7-(2,2-dimethyl-propyl)-6-(1,3-dioxo-2,8-diaza-spiro[4.5]dec-2-ylmethyl)-7H-pyrrolo[2,3-d] pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000076
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-3-propyl-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000027
7-(2,2-dimethylpropyl)-6-[(2,4-dioxo-8-propyl-1,3,8-triazaspiro[4.5]dec-3-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.000001
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000012
7-(2,2-dimethylpropyl)-6-[(3-methyl-2,4-dioxo-1,3,8-triazaspiro[4.5]dec-8-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.0000017
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
-
0.0000017
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
pH and temperature not specified in the publication
0.0000078
7-(2,2-dimethylpropyl)-6-[(5-fluoro-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.000001
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
below
0.000001
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 less than 0.000001 mM, pH and temperature not specified in the publication
0.000044
7-(2,2-dimethylpropyl)-6-[(5-methoxy-2-oxospiro[indole-3,4'-piperidin]-1(2H)-yl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
-
0.0000006
balicatib
Homo sapiens
-
isolated Cat K
0.000001
balicatib
Oryctolagus cuniculus
-
-
0.0000014
balicatib
Homo sapiens
-
pH and temperature not specified in the publication
0.000056
balicatib
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000061
balicatib
Homo sapiens
-
Hep-G2 cell based assay
0.00048
balicatib
Mus musculus
-
pH and temperature not specified in the publication
0.0000006
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
Homo sapiens
-
pH and temperature not specified in the publication
0.000035
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000044
benzyl [(2S)-1-{2-[(2-{(2S)-2-[(2-amino-3-phenylpropanoyl)amino]-4-methylpentanoyl}hydrazinyl)carbonyl]hydrazinyl}-4-methyl-1-oxopentan-2-yl]carbamate
Mus musculus
-
pH and temperature not specified in the publication
0.000163
BML-244
Homo sapiens
-
pH and temperature not specified in the publication
0.000748
BML-244
Mus musculus
-
pH and temperature not specified in the publication
0.002106
BML-244
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000013
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
Homo sapiens
-
pH and temperature not specified in the publication
0.000269
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000296
Boc-Phe-Leu-NHNH-CO-NHNH-Leu-Z
Mus musculus
-
pH and temperature not specified in the publication
0.000181
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
Homo sapiens
-
pH and temperature not specified in the publication
0.002588
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00426
dibenzyl [(2-oxopropane-1,3-diyl)bis{imino[(2S)-4-methyl-1-oxopentane-1,2-diyl]}]biscarbamate
Mus musculus
-
pH and temperature not specified in the publication
0.0000019
E-64
Homo sapiens
pH and temperature not specified in the publication
0.0117
E-64
Homo sapiens
at pH 5.5 and 25°C
0.000053
K4b
Homo sapiens
-
pH and temperature not specified in the publication
0.000145
K4b
Mus musculus
-
pH and temperature not specified in the publication
0.000239
K4b
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0000002
L-873724
Oryctolagus cuniculus
-
-
0.0000002
L-873724
Homo sapiens
-
isolated Cat K
0.0000002
L-873724
Homo sapiens
-
pH and temperature not specified in the publication
0.0000002
L-873724
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.00002
L-873724
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000043
L-873724
Mus musculus
-
pH and temperature not specified in the publication
0.004807
L-873724
Homo sapiens
-
Hep-G2 cell based assay
0.0000023
Mu-Leu-Hph-fluoromethylketone
Homo sapiens
-
pH and temperature not specified in the publication
0.0000076
Mu-Leu-Hph-fluoromethylketone
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000018
Mu-Leu-Hph-fluoromethylketone
Mus musculus
-
pH and temperature not specified in the publication
0.0000024
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
Mus musculus
-
recombinant cathepsin K
0.000028
N-(1-([(cyanomethyl)amino]carbonyl)cyclohexyl)-4-[2-(4-methylpiperazin-1-yl)-1,3-thiazol-4-yl]benzamide
Homo sapiens
-
at the cellular level in human osteoclasts
0.0000006
N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000051
N-(1-cyano-2-phenylethyl)-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.0000009
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Homo sapiens
-
-
0.0000012
N-[(1S)-1-cyanoethyl]-N2-[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl]-L-leucinamide
Oryctolagus cuniculus
-
humanized rabbit cathepsin K
0.000046
NC-2300
Homo sapiens
-
pH and temperature not specified in the publication
0.000102
NC-2300
Mus musculus
-
pH and temperature not specified in the publication
0.000319
NC-2300
Rattus norvegicus
-
pH and temperature not specified in the publication
0.0000002
odanacatib
Oryctolagus cuniculus
-
-
0.0000002
odanacatib
Homo sapiens
-
isolated Cat K
0.0000002
odanacatib
Homo sapiens
-
pH and temperature not specified in the publication
0.0000002
odanacatib
Oryctolagus cuniculus
-
pH and temperature not specified in the publication
0.00000056
odanacatib
Homo sapiens
50 mM MES pH 5.5, 25 mM EDTA and 2.5 mM DTT. 0.05% Tween20 (v/v), 37°C
0.000034
odanacatib
Homo sapiens
-
pH and temperature not specified in the publication
0.000108
odanacatib
Mus musculus
-
pH and temperature not specified in the publication
0.000112
odanacatib
Rattus norvegicus
-
pH and temperature not specified in the publication
0.00105
odanacatib
Homo sapiens
-
Hep-G2 cell based assay
0.0000007
relacatib
Homo sapiens
-
pH and temperature not specified in the publication
0.0000027
relacatib
Oryctolagus cuniculus
-
-
0.000014
relacatib
Homo sapiens
-
Hep-G2 cell based assay
0.000051
relacatib
Rattus norvegicus
-
pH and temperature not specified in the publication
0.000066
relacatib
Mus musculus
-
pH and temperature not specified in the publication
additional information
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetic acid
Homo sapiens
-
KI value is above 5 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.003 mM, inhibition is determined by a fluorometric assay with recombinant Cat K
additional information
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.003 mM, inhibition is determined by a fluorometric assay with recombinant Cat K
additional information
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.001 mM, inhibition is determined by a fluorometric assay with recombinant Cat K
additional information
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzoic acid
Homo sapiens
-
KI value is above 2 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is below 1 nM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(2-piperidin-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is below 1 nM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
IC50 is above 0.01 mM, Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)-3-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 is above 1 M, with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 is above 2 M, with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
IC50 is above 0.01 mM, Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1.5 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
IC50 is above 0.01 mM, Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 is above 1 M, with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
additional information
Mus musculus
-
Ulmus diviana stem bral extracts show an IC50 of 0.0875 mg/ml
-
additional information
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)propanamide
Homo sapiens
-
KI value is above 1.5 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
additional information
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 not detected
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.