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Literature summary for 3.4.14.5 extracted from

  • Tsai, T.Y.; Coumar, M.S.; Hsu, T.; Hsieh, H.P.; Chien, C.H.; Chen, C.T.; Chang, C.N.; Lo, Y.K.; Wu, S.H.; Huang, C.Y.; Huang, Y.W.; Wang, M.H.; Wu, H.Y.; Lee, H.J.; Chen, X.; Chao, Y.S.; Jiaang, W.T.
    Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors (2006), Bioorg. Med. Chem. Lett., 16, 3268-3272.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R)-4-(3-methyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
-
Homo sapiens
(2S)-1-[(4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-5,5-dimethyl-L-prolyl]pyrrolidine-2-carbonitrile
-
Homo sapiens
(2S)-1-[N-[3-(1,3-dihydro-2H-isoindol-2-yl)-1,1-dimethyl-3-oxopropyl]glycyl]pyrrolidine-2-carbonitrile
-
Homo sapiens
(2S)-1-[[(2S,4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
-
Homo sapiens
(2S)-1-[[(2S,4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile in vivo plasma DPP-IV inhibition in Wistar rats Rattus norvegicus
(2S)-1-[[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile
-
Homo sapiens
(3S,5S)-N-(2-phenylethyl)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide
-
Homo sapiens
(3S,5S)-N-benzyl-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide
-
Homo sapiens
(3S,5S)-N-phenyl-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide
-
Homo sapiens
2-([(3S,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]carbonyl)isoindoline
-
Homo sapiens
2-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
Homo sapiens
2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]-5-(trifluoromethyl)isoindoline
-
Homo sapiens
2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
Homo sapiens
2-[[(3S,5S)-5-[[(3R)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]carbonyl]isoindoline
-
Homo sapiens
2-[[(3S,5S)-5-[[(3S)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]carbonyl]isoindoline
-
Homo sapiens
5,6-dichloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
Homo sapiens
5-chloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
Homo sapiens
5-chloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline in vivo plasma DPP-IV inhibition in Wistar rats Rattus norvegicus
5-fluoro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
Homo sapiens
5-methyl-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
Wistar
-
Rattus norvegicus Wistar
-
Wistar
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Gly-Pro-p-nitroanilide + H2O
-
Homo sapiens Gly-Pro + p-nitroaniline
-
?
Gly-Pro-p-nitroanilide + H2O
-
Rattus norvegicus Gly-Pro + p-nitroaniline
-
?
Gly-Pro-p-nitroanilide + H2O
-
Rattus norvegicus Wistar Gly-Pro + p-nitroaniline
-
?

Synonyms

Synonyms Comment Organism
dipeptidyl peptidase IV
-
Homo sapiens
dipeptidyl peptidase IV
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000017
-
-
Homo sapiens (2S)-1-[[(2S,4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)pyrrolidin-2-yl]carbonyl]pyrrolidine-2-carbonitrile
0.000015
-
-
Homo sapiens (2S)-1-[N-[3-(1,3-dihydro-2H-isoindol-2-yl)-1,1-dimethyl-3-oxopropyl]glycyl]pyrrolidine-2-carbonitrile
0.00003
-
-
Homo sapiens (2R)-4-(3-methyl-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-oxo-1-(2,4,5-trifluorophenyl)butan-2-amine
0.00005
-
-
Homo sapiens 5-chloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
0.000051
-
-
Homo sapiens (2S)-1-[[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile
0.000072
-
-
Homo sapiens 5-methyl-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
0.000073
-
-
Homo sapiens 2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]-5-(trifluoromethyl)isoindoline
0.000073
-
-
Homo sapiens 5-fluoro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
0.000084
-
-
Homo sapiens 2-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
0.000109
-
-
Homo sapiens 2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
0.000129
-
-
Homo sapiens 2-([(3S,5S)-5-[(3,3-difluoropyrrolidin-1-yl)carbonyl]pyrrolidin-3-yl]carbonyl)isoindoline
0.000144
-
-
Homo sapiens 5,6-dichloro-2-[[(3S,5S)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidin-3-yl]carbonyl]isoindoline
0.000228
-
-
Homo sapiens 2-[[(3S,5S)-5-[[(3R)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]carbonyl]isoindoline
0.000245
-
-
Homo sapiens 2-[[(3S,5S)-5-[[(3S)-3-fluoropyrrolidin-1-yl]carbonyl]pyrrolidin-3-yl]carbonyl]isoindoline
0.000984
-
-
Homo sapiens (2S)-1-[(4S)-4-(1,3-dihydro-2H-isoindol-2-ylcarbonyl)-5,5-dimethyl-L-prolyl]pyrrolidine-2-carbonitrile
0.001957
-
-
Homo sapiens (3S,5S)-N-benzyl-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide
0.002587
-
-
Homo sapiens (3S,5S)-N-(2-phenylethyl)-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide
0.00413
-
-
Homo sapiens (3S,5S)-N-phenyl-5-(pyrrolidin-1-ylcarbonyl)pyrrolidine-3-carboxamide