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Literature summary for 3.4.14.5 extracted from

  • Sakashita, H.; Akahoshi, F.; Yoshida, T.; Kitajima, H.; Hayashi, Y.; Ishii, S.; Takashina, Y.; Tsutsumiuchi, R.; Ono, S.
    Lead optimization of [(S)-gamma-(arylamino)prolyl]thiazolidine focused on gamma-substituent: Indoline compounds as potent DPP-IV inhibitors (2007), Bioorg. Med. Chem., 15, 641-655.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl 4-cyanobenzoate
-
Homo sapiens
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl 4-cyanobenzoate
-
Rattus norvegicus
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl benzoate
-
Homo sapiens
(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl benzoate
-
Rattus norvegicus
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
Homo sapiens
(3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
Rattus norvegicus
(3S,5S)-N-(4-methoxyphenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
Homo sapiens
(3S,5S)-N-(4-methoxyphenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
Rattus norvegicus
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
Homo sapiens
(3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
Rattus norvegicus
(3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
Homo sapiens
(3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
Rattus norvegicus
(3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
Homo sapiens
(3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
-
Rattus norvegicus
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
Homo sapiens
1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
Rattus norvegicus
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
Homo sapiens
1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
-
Rattus norvegicus
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
-
Homo sapiens
1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
-
Rattus norvegicus
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Homo sapiens
2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Rattus norvegicus
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
-
Homo sapiens
2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
-
Rattus norvegicus
3-[(2S)-pyrrolidin-2-ylcarbonyl]-1,3-thiazolidine
-
Homo sapiens
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
-
Homo sapiens
4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
-
Rattus norvegicus
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
Homo sapiens
4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
Rattus norvegicus
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
Homo sapiens
4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
Rattus norvegicus
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
Homo sapiens
4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
Rattus norvegicus
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
Homo sapiens
4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
-
Rattus norvegicus
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
Homo sapiens
4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
Rattus norvegicus
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
Homo sapiens
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
Rattus norvegicus
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
Homo sapiens
4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
Rattus norvegicus
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
-
Homo sapiens
4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
-
Rattus norvegicus
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Homo sapiens
5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Rattus norvegicus
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Homo sapiens
5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Rattus norvegicus
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Homo sapiens
5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Rattus norvegicus
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Homo sapiens
5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Rattus norvegicus
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Homo sapiens
5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
-
Rattus norvegicus
6-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]nicotinonitrile
-
Homo sapiens
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
-
Homo sapiens
ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
-
Rattus norvegicus
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
-
Homo sapiens
N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
-
Rattus norvegicus
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
Homo sapiens
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
-
Rattus norvegicus
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
Homo sapiens
N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzenesulfonamide
-
Rattus norvegicus
NVP-DPP728
-
Homo sapiens
NVP-DPP728
-
Rattus norvegicus
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
-
Homo sapiens
[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens P27487
-
-
Rattus norvegicus
-
-
-

Substrates and Products (Substrate)

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

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000005
-
-
Rattus norvegicus 4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.000005
-
-
Homo sapiens 4-([butyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.0000061
-
-
Rattus norvegicus 5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000061
-
-
Homo sapiens 5-methoxy-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000093
-
-
Rattus norvegicus 4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
0.0000093
-
-
Homo sapiens 4,4'-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]imino]dimethanediyl)dibenzonitrile
0.0000101
-
-
Rattus norvegicus 5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000101
-
-
Homo sapiens 5-fluoro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000103
-
-
Rattus norvegicus 5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000103
-
-
Homo sapiens 5-nitro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000107
-
-
Rattus norvegicus 5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000107
-
-
Homo sapiens 5-bromo-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000125
-
-
Rattus norvegicus 4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.0000125
-
-
Homo sapiens 4-([(1-methylethyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.0000134
-
-
Rattus norvegicus 5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000134
-
-
Homo sapiens 5-chloro-2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000136
-
-
Rattus norvegicus 4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.0000136
-
-
Homo sapiens 4-([methyl[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.0000153
-
-
Rattus norvegicus ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
0.0000153
-
-
Homo sapiens ethyl N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]glycinate
0.0000163
-
-
Rattus norvegicus [(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
0.0000163
-
-
Homo sapiens [(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetic acid
0.0000165
-
-
Rattus norvegicus 2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
0.0000165
-
-
Homo sapiens 2-[(4-cyanobenzyl)[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]acetamide
0.0000195
-
-
Rattus norvegicus 2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000195
-
-
Homo sapiens 2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.000021
-
-
Rattus norvegicus (3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.000021
-
-
Homo sapiens (3S,5S)-N-(4-nitrophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.000023
-
-
Rattus norvegicus N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
0.000023
-
-
Homo sapiens N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-b-alanine
0.0000336
-
-
Rattus norvegicus 4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
0.0000336
-
-
Homo sapiens 4-[[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]benzonitrile
0.0000341
-
-
Rattus norvegicus 4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
0.0000341
-
-
Homo sapiens 4-cyano-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
0.0000343
-
-
Rattus norvegicus 4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.0000343
-
-
Homo sapiens 4-([[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]amino]methyl)benzonitrile
0.000039
-
-
Rattus norvegicus 2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.000039
-
-
Homo sapiens 2-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]isoindoline
0.0000549
-
-
Rattus norvegicus (3S,5S)-N-(4-methoxyphenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.0000551
-
-
Rattus norvegicus (3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.0000551
-
-
Homo sapiens (3S,5S)-N-(4-chlorophenyl)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.0000762
-
-
Rattus norvegicus 1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
0.0000762
-
-
Homo sapiens 1-(4-cyanophenyl)-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
0.0000998
-
-
Rattus norvegicus 1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
0.0000998
-
-
Homo sapiens 1-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]-1,2,3,4-tetrahydroquinoline
0.000151
-
-
Rattus norvegicus 1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
0.000151
-
-
Homo sapiens 1-phenyl-3-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]urea
0.000168
-
-
Rattus norvegicus 4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
0.000168
-
-
Homo sapiens 4-cyano-N-(4-cyanobenzyl)-N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
0.000171
-
-
Rattus norvegicus (3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.000171
-
-
Homo sapiens (3S,5S)-N-benzyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.00019
-
-
Rattus norvegicus (3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.00019
-
-
Homo sapiens (3S,5S)-N-phenyl-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-amine
0.000236
-
-
Rattus norvegicus N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide
0.000236
-
-
Homo sapiens N-[(3S,5S)-5-(1,3-thiazolidin-3-ylcarbonyl)pyrrolidin-3-yl]benzamide