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Literature summary for 3.4.14.5 extracted from

  • Nordhoff, S.; Cerezo-Galvez, S.; Deppe, H.; Hill, O.; Lopez-Canet, M.; Rummey, C.; Thiemann, M.; Matassa, V.G.; Edwards, P.J.; Feurer, A.
    Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV (2009), Bioorg. Med. Chem. Lett., 19, 4201-4203.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
alogliptin
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-(methylsulfonyl)benzamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-2-carboxamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-3-carboxamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-4-carboxamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(3,4,6-trifluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-(methylsulfonyl)benzamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(5-chlorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2,5-dichlorobenzenesulfonamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzenesulfonamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzenesulfonamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-chlorobenzenesulfonamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzenesulfonamide
-
Rattus norvegicus
N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
-
Rattus norvegicus
saxagliptin
-
Rattus norvegicus
sitagliptin
-
Rattus norvegicus
vildagliptin
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase IV
-
Rattus norvegicus
DPP-4
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000038
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-(methylsulfonyl)benzamide
0.000008
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
0.000008
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(5-chlorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
0.000009
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(3,4,6-trifluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
0.000012
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanecarboxamide
0.000014
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
0.00002
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-chlorobenzenesulfonamide
0.000024
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2,5-dichlorobenzenesulfonamide
0.000027
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
0.000027
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-(methylsulfonyl)benzamide
0.000027
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzenesulfonamide
0.00003
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(3-chlorophenyl)butanoyl]pyrrolidin-2-yl]methyl)cyclohexanesulfonamide
0.000034
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)benzenesulfonamide
0.000047
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-2-carboxamide
0.000049
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzamide
0.000053
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-2-fluorobenzenesulfonamide
0.000066
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-4-carboxamide
0.000077
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-(methylsulfonyl)benzamide
0.000087
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)pyridine-3-carboxamide
0.00009
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)benzamide
0.000092
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzamide
0.000092
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(2-fluorophenyl)butanoyl]pyrrolidin-2-yl]methyl)-4-fluorobenzamide
0.000094
-
-
Rattus norvegicus N-([(2S)-1-[(3R)-3-amino-4-(6-fluorocyclohexa-2,4-dien-1-yl)butanoyl]pyrrolidin-2-yl]methyl)-3-fluorobenzenesulfonamide