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Literature summary for 3.4.14.5 extracted from

  • Tsai, T.Y.; Hsu, T.; Chen, C.T.; Cheng, J.H.; Chiou, M.C.; Huang, C.H.; Tseng, Y.J.; Yeh, T.K.; Huang, C.Y.; Yeh, K.C.; Huang, Y.W.; Wu, S.H.; Wang, M.H.; Chen, X.; Chao, Y.S.; Jiaang, W.T.
    Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 1908-1912.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2S)-1-(5-morpholin-4-yl-5-oxo-L-norvalyl)pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-(5-oxo-5-piperidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-(5-oxo-5-pyrrolidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[(2S)-2-amino-4-(1,3-dihydro-2H-isoindol-2-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[(2S)-2-amino-6-(1,3-dihydro-2H-isoindol-2-yl)-6-oxohexanoyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[(2S,3R)-2-amino-3-ethyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]pentanoyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[3-methyl-5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[3-methyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[3-methyl-5-[(2R)-2-methylpyrrolidin-1-yl]-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-oxo-5-(1,3-thiazolidin-3-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-oxo-5-(4-pyridin-4-ylpiperazin-1-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-oxo-5-[4-(trifluoroacetyl)piperazin-1-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-[(2R)-2-(methoxyamino)pyrrolidin-1-yl]-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-[2-(4-fluorophenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-6-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-1-[5-[6,7-dimethoxy-1-(1-methylethyl)-3,4-dihydroisoquinolin-2(1H)-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
-
Rattus norvegicus
(2S)-5-(1,3-dihydro-2H-isoindol-2-yl)-1,5-dioxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine
-
Rattus norvegicus
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxo-N-phenylpentanamide
-
Rattus norvegicus
(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-N-cyclopentyl-5-oxopentanamide
-
Rattus norvegicus
ethyl 4-[(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxopentanoyl]piperazine-1-carboxylate
-
Rattus norvegicus
sitagliptin
-
Rattus norvegicus
vildagliptin
-
Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Rattus norvegicus
-

Synonyms

Synonyms Comment Organism
CD26
-
Rattus norvegicus
dipeptidyl peptidase IV
-
Rattus norvegicus
DPP-IV
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
-
Rattus norvegicus (2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
0.000005
-
-
Rattus norvegicus (2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
0.000005
-
-
Rattus norvegicus (2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
0.000006
-
-
Rattus norvegicus (2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
0.000006
-
-
Rattus norvegicus (2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
0.000007
-
-
Rattus norvegicus (2S)-1-(5-oxo-5-pyrrolidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
0.000007
-
-
Rattus norvegicus (2S)-1-[5-(5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
0.000007
-
-
Rattus norvegicus (2S)-1-[5-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
0.000008
-
-
Rattus norvegicus (2S)-1-[5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
0.000008
-
-
Rattus norvegicus (2S)-1-[5-oxo-5-[4-(trifluoroacetyl)piperazin-1-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
0.000009
-
-
Rattus norvegicus (2S)-1-[5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-norvalyl]pyrrolidine-2-carbonitrile
0.00001
-
-
Rattus norvegicus (2S)-1-[(2S)-2-amino-6-(1,3-dihydro-2H-isoindol-2-yl)-6-oxohexanoyl]pyrrolidine-2-carbonitrile
0.00001
-
-
Rattus norvegicus (2S)-1-[5-oxo-5-(1,3-thiazolidin-3-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
0.000011
-
-
Rattus norvegicus (4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-N-cyclopentyl-5-oxopentanamide
0.000012
-
-
Rattus norvegicus (2S)-1-[3-methyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
0.000012
-
-
Rattus norvegicus (2S)-1-[5-(1,3-dihydro-2H-isoindol-2-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
0.000013
-
-
Rattus norvegicus (2S)-1-[3-methyl-5-[(2R)-2-methylpyrrolidin-1-yl]-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
0.000014
-
-
Rattus norvegicus (2S)-1-[5-[(2R)-2-(methoxyamino)pyrrolidin-1-yl]-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
0.000015
-
-
Rattus norvegicus (2S)-1-(5-oxo-5-piperidin-1-yl-L-norvalyl)pyrrolidine-2-carbonitrile
0.000016
-
-
Rattus norvegicus (2S)-1-[5-(3,4-dihydroisoquinolin-2(1H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
0.000017
-
-
Rattus norvegicus (2S)-1-(5-morpholin-4-yl-5-oxo-L-norvalyl)pyrrolidine-2-carbonitrile
0.000019
-
-
Rattus norvegicus (2S)-1-[5-oxo-5-(4-pyridin-4-ylpiperazin-1-yl)-L-norvalyl]pyrrolidine-2-carbonitrile
0.000022
-
-
Rattus norvegicus (2S)-1-[5-[(2R)-2-(methoxymethyl)pyrrolidin-1-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
0.000025
-
-
Rattus norvegicus (2S)-1-[5-(4,7-dihydrothieno[2,3-c]pyridin-6(5H)-yl)-3-methyl-5-oxo-L-alloisoleucyl]pyrrolidine-2-carbonitrile
0.000031
-
-
Rattus norvegicus (2S)-1-[(2S,3R)-2-amino-3-ethyl-5-oxo-5-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]pentanoyl]pyrrolidine-2-carbonitrile
0.000031
-
-
Rattus norvegicus (2S)-1-[3-methyl-5-oxo-5-[2-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[1,5-a]pyrazin-7(8H)-yl]-L-alloisoleucyl]pyrrolidine-2-carbonitrile
0.000031
-
-
Rattus norvegicus ethyl 4-[(4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxopentanoyl]piperazine-1-carboxylate
0.000035
-
-
Rattus norvegicus (2S)-1-[5-[6,7-dimethoxy-1-(1-methylethyl)-3,4-dihydroisoquinolin-2(1H)-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
0.000037
-
-
Rattus norvegicus (4S)-4-amino-5-[(2S)-2-cyanopyrrolidin-1-yl]-5-oxo-N-phenylpentanamide
0.00004
-
-
Rattus norvegicus (2S)-1-[5-[2-(4-fluorophenyl)-4,5,6,7-tetrahydro-1,3-benzothiazol-6-yl]-5-oxo-L-norvalyl]pyrrolidine-2-carbonitrile
0.000298
-
-
Rattus norvegicus (2S)-1-[(2S)-2-amino-4-(1,3-dihydro-2H-isoindol-2-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
0.0016
-
-
Rattus norvegicus (2S)-5-(1,3-dihydro-2H-isoindol-2-yl)-1,5-dioxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine