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Literature summary for 3.4.14.5 extracted from

  • Nordhoff, S.; Lopez-Canet, M.; Hoffmann-Enger, B.; Bulat, S.; Cerezo-Galvez, S.; Hill, O.; Rosenbaum, C.; Rummey, C.; Thiemann, M.; Matassa, V.G.; Edwards, P.J.; Feurer, A.
    From lead to preclinical candidate: optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV (2009), Bioorg. Med. Chem. Lett., 19, 4818-4823.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3R)-3-amino-1-[(2S)-2-([[2-(trifluoromethyl)pyrimidin-4-yl]oxy]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
Homo sapiens
(3R)-3-amino-1-[(2S)-2-([[4-(trifluoromethyl)pyrimidin-2-yl]amino]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
Homo sapiens
(3R)-3-amino-1-[(2S)-2-([[6-(trifluoromethyl)pyridin-3-yl]amino]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
Homo sapiens
(3R)-3-amino-1-[(2S)-2-[(cyclopropylmethoxy)methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
Homo sapiens
(3R)-3-amino-1-[(2S)-2-[(pyrimidin-2-ylamino)methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
Homo sapiens
(3R)-3-amino-1-[(2S)-2-[[(5-fluoropyridin-2-yl)amino]methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
Homo sapiens
(3R)-3-amino-1-[(2S)-2-[[(5-fluoropyrimidin-2-yl)amino]methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
-
Homo sapiens
2-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methoxy)pyridine-4-carbonitrile
-
Homo sapiens
2-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)amino]pyridine-3-carbonitrile
-
Homo sapiens
6-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methoxy)pyridine-3-carbonitrile
-
Homo sapiens
6-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)(methyl)amino]pyridine-3-carbonitrile
-
Homo sapiens
6-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)amino]pyridine-3-carbonitrile
-
Homo sapiens
alogliptin
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1,1,1-trifluoro-N-methylmethanesulfonamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1,1,1-trifluoromethanesulfonamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1-(trifluoromethyl)cyclopropanecarboxamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2,2-trifluoroethanesulfonamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluoro-N-methylpropanamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluorocyclopropanecarboxamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluoropropanamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-dimethylpropanamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluoro-2-methylpropanamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3,3,3-trifluoropropanamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N,2,2-trimethylpropanamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N-cyclopropyl-1,1,1-trifluoromethanesulfonamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N-methylcyclopropanecarboxamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclobutanecarboxamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclopentanecarboxamide
-
Homo sapiens
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)methanesulfonamide
-
Homo sapiens
saxagliptin
-
Homo sapiens
sitagliptin
-
Homo sapiens
vildagliptin
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase IV
-
Homo sapiens
DPP-4
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000011
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N-methylcyclopropanecarboxamide
0.0000013
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluorocyclopropanecarboxamide
0.0000015
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1,1,1-trifluoro-N-methylmethanesulfonamide
0.000002
-
-
Homo sapiens 6-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methoxy)pyridine-3-carbonitrile
0.0000022
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclobutanecarboxamide
0.0000023
-
-
Homo sapiens 2-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methoxy)pyridine-4-carbonitrile
0.0000027
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1-(trifluoromethyl)cyclopropanecarboxamide
0.0000027
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N-cyclopropyl-1,1,1-trifluoromethanesulfonamide
0.0000032
-
-
Homo sapiens 2-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)amino]pyridine-3-carbonitrile
0.0000035
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3,3,3-trifluoropropanamide
0.0000035
-
-
Homo sapiens 6-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)amino]pyridine-3-carbonitrile
0.0000037
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-dimethylpropanamide
0.0000039
-
-
Homo sapiens (3R)-3-amino-1-[(2S)-2-([[4-(trifluoromethyl)pyrimidin-2-yl]amino]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
0.000004
-
-
Homo sapiens 6-[([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)(methyl)amino]pyridine-3-carbonitrile
0.0000048
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclopentanecarboxamide
0.0000054
-
-
Homo sapiens (3R)-3-amino-1-[(2S)-2-[(pyrimidin-2-ylamino)methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
0.0000056
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2,2-trifluoroethanesulfonamide
0.0000059
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluoropropanamide
0.0000061
-
-
Homo sapiens (3R)-3-amino-1-[(2S)-2-([[2-(trifluoromethyl)pyrimidin-4-yl]oxy]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
0.0000063
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluoro-2-methylpropanamide
0.0000063
-
-
Homo sapiens (3R)-3-amino-1-[(2S)-2-[[(5-fluoropyridin-2-yl)amino]methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
0.0000068
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-N,2,2-trimethylpropanamide
0.0000071
-
-
Homo sapiens (3R)-3-amino-1-[(2S)-2-[[(5-fluoropyrimidin-2-yl)amino]methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
0.0000078
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2,2-difluoro-N-methylpropanamide
0.000008
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
0.000009
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
0.00001
-
-
Homo sapiens (3R)-3-amino-1-[(2S)-2-[(cyclopropylmethoxy)methyl]pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
0.000012
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-1,1,1-trifluoromethanesulfonamide
0.000015
-
-
Homo sapiens (3R)-3-amino-1-[(2S)-2-([[6-(trifluoromethyl)pyridin-3-yl]amino]methyl)pyrrolidin-1-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
0.000027
-
-
Homo sapiens N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)methanesulfonamide