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Literature summary for 3.4.14.5 extracted from

  • Sakashita, H.; Akahoshi, F.; Kitajima, H.; Tsutsumiuchi, R.; Hayashi, Y.
    [(S)-gamma-(Arylamino)prolyl]thiazolidine compounds as a novel series of potent and stable DPP-IV inhibitors (2006), Bioorg. Med. Chem., 14, 3662-3671.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2S)-1-L-prolylpyrrolidine-2-carbonitrile IC50: 2.9 nmol/L Homo sapiens
(2S)-1-L-prolylpyrrolidine-2-carbonitrile IC50: 2.9 nmol/L Rattus norvegicus
3-((2S,4S)-4-anilino-2-pyrrolidinylcarbonyl)-1,3-thiazolidine IC50: 147 nmol/L Homo sapiens
3-((2S,4S)-4-anilino-2-pyrrolidinylcarbonyl)-1,3-thiazolidine IC50: 190 nmol/L Rattus norvegicus
3-L-prolyl-1,3-thiazolidine IC50: 538 nmol/L Homo sapiens
3-L-prolyl-1,3-thiazolidine IC50: 607 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(2-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 18.2 nmol/L Homo sapiens
3-[(2S,4S)-4-(2-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 21.8 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(2-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 24.1 nmol/L Homo sapiens
3-[(2S,4S)-4-(2-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 41.3 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(3,4-dicyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 8.4 nmol/L Homo sapiens
3-[(2S,4S)-4-(3,4-dicyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 10.8 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(3,4-methylenedioxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 29.0 nmol/L Homo sapiens
3-[(2S,4S)-4-(3,4-methylenedioxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 34.5 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(3-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 11.1nmol/L Homo sapiens
3-[(2S,4S)-4-(3-chloro-4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 13.0 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(3-chloro-4-methoxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 19.9 nmol/L Homo sapiens
3-[(2S,4S)-4-(3-chloro-4-methoxyphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 14.8 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(4-aminophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 105 nmol/L Homo sapiens
3-[(2S,4S)-4-(4-aminophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 125 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(4-chlorophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 45.4 nmol/L Homo sapiens
3-[(2S,4S)-4-(4-chlorophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 55.1 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 25.2 nmol/L Homo sapiens
3-[(2S,4S)-4-(4-cyanophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 33.6 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(4-methanesulfonylphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 52.3 nmol/L Homo sapiens
3-[(2S,4S)-4-(4-methanesulfonylphenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 43.8 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(4-nitrophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 19.2 nmol/L Homo sapiens
3-[(2S,4S)-4-(4-nitrophenyl)amino-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 21.0 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(5-cyano-2-pyridyl)amino-2-pyrolidinylcarbonyl]-1,3-thiazolidine IC50: 25.4 nmol/L Homo sapiens
3-[(2S,4S)-4-(5-cyano-2-pyridyl)amino-2-pyrolidinylcarbonyl]-1,3-thiazolidine IC50: 30.4 nmol/L Rattus norvegicus
3-[(2S,4S)-4-(p-anisidino)-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 51.5 nmol/L Homo sapiens
3-[(2S,4S)-4-(p-anisidino)-2-pyrrolidinylcarbonyl]-1,3-thiazolidine IC50: 54.9 nmol/L Rattus norvegicus
6-([(3S,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-3-yl]amino)pyridine-3-carbonitrile IC50: 0.25 nmol/L Homo sapiens
6-([(3S,5S)-5-([(2S)-2-cyanopyrrolidin-1-yl]carbonyl)pyrrolidin-3-yl]amino)pyridine-3-carbonitrile IC50: 0.27 nmol/L Rattus norvegicus
6-([2-((2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl)amino)ethyl]amino)pyridine-3-carbonitrile IC50: 1.4 nmol/L Homo sapiens
6-([2-((2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl)amino)ethyl]amino)pyridine-3-carbonitrile IC50: 2.3 nmol/L Rattus norvegicus
6-[(2-([2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]amino)ethyl)amino]pyridine-3-carbonitrile IC50: 270 nmol/L Homo sapiens
6-[(2-([2-oxo-2-(1,3-thiazolidin-3-yl)ethyl]amino)ethyl)amino]pyridine-3-carbonitrile IC50: 500 nmol/L Rattus norvegicus

Organism

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

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Homo sapiens
-
blood plasma
-
Rattus norvegicus
-

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
-
?
Gly-Pro-4-methylcoumarin 7-amide + H2O
-
Rattus norvegicus Gly-Pro + 7-amino-4-methylcoumarin
-
?