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Literature summary for 3.4.14.5 extracted from

  • Pei, Z.; Li, X.; von Geldern, T.W.; Longenecker, K.; Pireh, D.; Stewart, K.D.; Backes, B.J.; Lai, C.; Lubben, T.H.; Ballaron, S.J.; Beno, D.W.; Kempf-Grote, A.J.; Sham, H.L.; Trevillyan, J.M.
    Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors (2007), J. Med. Chem., 50, 1983-1987.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3R)-1-[6-[(3R,4R)-3-amino-4-(2,4,5-trifluorophenyl)piperidin-1-yl]pyrimidin-4-yl]pyrrolidin-3-ol
-
Homo sapiens
(3R,4R)-1-(6-phenylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
(3R,4R)-1-(6-piperidin-1-ylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
(3R,4R)-1-(6-pyrrolidin-1-ylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
(3R,4R)-1-[4-[3-(methylsulfonyl)phenyl]-1,3,5-triazin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
(3R,4R)-1-[6-(3,3-difluoropyrrolidin-1-yl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
(3R,4R)-1-[6-[2-(trifluoromethyl)-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
(3R,4R)-1-[6-[3-(methylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
(3R,4R)-3-amino-N-phenyl-4-(2,4,5-trifluorophenyl)piperidine-1-carboxamide
-
Homo sapiens
(4R,5R)-5-amino-1-(2-phenylethyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
(4R,5R)-5-amino-1-(2-pyridin-4-ylethyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
(4R,5R)-5-amino-1-(3-phenylpropyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
(4R,5R)-5-amino-1-(morpholin-4-ylmethyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
(4R,5R)-5-amino-1-benzyl-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
(4R,5R)-5-amino-1-benzyl-4-(2-chlorophenyl)piperidin-2-one
-
Homo sapiens
(4R,5R)-5-amino-1-[(2S)-2-phenylpropyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
(4R,5R)-5-amino-1-[2-(1,3-benzodioxol-5-yl)ethyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
(4R,5R)-5-amino-1-[2-[3-(methylsulfonyl)phenyl]ethyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
(4R,5R)-5-amino-1-[2-[4-(methylsulfonyl)phenyl]ethyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
(4R,5R)-5-amino-4-(2-chlorophenyl)-1-(cyclohexylmethyl)piperidin-2-one
-
Homo sapiens
(4R,5R)-5-amino-4-(2-chlorophenyl)-1-phenylpiperidin-2-one
-
Homo sapiens
3-[2-[(4R,5R)-5-amino-2-oxo-4-(2,4,5-trifluorophenyl)piperidin-1-yl]ethyl]benzoic acid
-
Homo sapiens
6-[(3R,4R)-3-amino-4-(2,4,5-trifluorophenyl)piperidin-1-yl]-N,N-diethylpyrimidin-4-amine
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P27487
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Gly-Pro-4-methylcoumarin 7-amide + H2O
-
Homo sapiens Gly-Pro + 7-amino-4-methylcoumarin
-
?

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase IV
-
Homo sapiens
DPP4
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000012
-
(3R)-1-[6-[(3R,4R)-3-amino-4-(2,4,5-trifluorophenyl)piperidin-1-yl]pyrimidin-4-yl]pyrrolidin-3-ol
-
Homo sapiens
0.0000016
-
(3R,4R)-1-[6-(3,3-difluoropyrrolidin-1-yl)pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
0.0000023
-
(3R,4R)-1-(6-pyrrolidin-1-ylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
0.000003
-
(3R,4R)-1-[6-[2-(trifluoromethyl)-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
0.0000038
-
3-[2-[(4R,5R)-5-amino-2-oxo-4-(2,4,5-trifluorophenyl)piperidin-1-yl]ethyl]benzoic acid
-
Homo sapiens
0.000004
-
(4R,5R)-5-amino-1-[2-[3-(methylsulfonyl)phenyl]ethyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
0.000004
-
(3R,4R)-1-[6-[3-(methylsulfonyl)phenyl]pyrimidin-4-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
0.0000061
-
(3R,4R)-1-(6-phenylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
0.0000071
-
(4R,5R)-5-amino-1-[2-(1,3-benzodioxol-5-yl)ethyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
0.000011
-
(3R,4R)-1-(6-piperidin-1-ylpyrimidin-4-yl)-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
0.000012
-
(4R,5R)-5-amino-1-[2-[4-(methylsulfonyl)phenyl]ethyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
0.000012
-
6-[(3R,4R)-3-amino-4-(2,4,5-trifluorophenyl)piperidin-1-yl]-N,N-diethylpyrimidin-4-amine
-
Homo sapiens
0.000013
-
(3R,4R)-1-[4-[3-(methylsulfonyl)phenyl]-1,3,5-triazin-2-yl]-4-(2,4,5-trifluorophenyl)piperidin-3-amine
-
Homo sapiens
0.000017
-
(4R,5R)-5-amino-1-(2-phenylethyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
0.000024
-
(4R,5R)-5-amino-1-(2-pyridin-4-ylethyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
0.0000833
-
(4R,5R)-5-amino-1-[(2S)-2-phenylpropyl]-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
0.00014
-
(3R,4R)-3-amino-N-phenyl-4-(2,4,5-trifluorophenyl)piperidine-1-carboxamide
-
Homo sapiens
0.00027
-
(4R,5R)-5-amino-1-(3-phenylpropyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
0.00044
-
(4R,5R)-5-amino-1-benzyl-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
0.00059
-
(4R,5R)-5-amino-1-(morpholin-4-ylmethyl)-4-(2,4,5-trifluorophenyl)piperidin-2-one
-
Homo sapiens
0.00093
-
(4R,5R)-5-amino-4-(2-chlorophenyl)-1-(cyclohexylmethyl)piperidin-2-one
-
Homo sapiens
0.0014
-
(4R,5R)-5-amino-1-benzyl-4-(2-chlorophenyl)piperidin-2-one
-
Homo sapiens
0.0016
-
(4R,5R)-5-amino-4-(2-chlorophenyl)-1-phenylpiperidin-2-one
-
Homo sapiens