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Literature summary for 3.4.13.18 extracted from

  • Jiaang, W.T.; Chen, Y.S.; Hsu, T.; Wu, S.H.; Chien, C.H.; Chang, C.N.; Chang, S.P.; Lee, S.J.; Chen, X.
    Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8 (2005), Bioorg. Med. Chem. Lett., 15, 687-691.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(1S)-1-cyclohexyl-2-(1,3-dihydro-2H-isoindol-2-yl)-2-oxoethanamine IC50: 24 nM Homo sapiens
(1S)-1-cyclohexyl-2-(3,4-dihydroisoquinolin-2(1H)-yl)-2-oxoethanamine IC50: 3016 nM Homo sapiens
(1S)-1-cyclohexyl-2-oxo-2-piperidin-1-ylethanamine IC50: 1448 nM Homo sapiens
(1S)-1-cyclohexyl-2-oxo-2-pyrrolidin-1-ylethanamine IC50: 78 nM Homo sapiens
(2S)-1-[(2S)-2-amino-4-(3,4-dihydroisoquinolin-2(1H)-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile IC50: 19 nM Homo sapiens
(2S)-1-[(2S)-2-amino-4-(4-[bis(4-fluorophenyl)methyl]piperazin-1-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile IC50: 16 nM Homo sapiens
(2S)-2-amino-2-cyclohexyl-1-[(2R)-2-(iminomethyl)cyclopentyl]ethanone IC50: 27 nM Homo sapiens
(2S,3S)-3-methyl-1-oxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine IC50: 364 nM Homo sapiens
1-(1,3-dihydro-2H-isoindol-2-yl)-4-(3,4-dihydroisoquinolin-2(1H)-yl)-1,4-dioxobutan-2-amine IC50: 555 nM Homo sapiens
1-(1,3-dihydro-2H-isoindol-2-yl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-1,4-dioxobutan-2-amine IC50: 150 nM Homo sapiens
4-(4-[bis(4-fluorophenyl)methyl]piperazin-1-yl)-1-(1,3-dihydro-2H-isoindol-2-yl)-1,4-dioxobutan-2-amine IC50: 14 nM Homo sapiens
6-([2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)ethyl]amino)nicotinonitrile IC50: 4574 nM Homo sapiens
NVP LAF237 i.e.vildagliptin, IC50: 14219 nM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
DPP8
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000014
-
IC50: 14 nM Homo sapiens 4-(4-[bis(4-fluorophenyl)methyl]piperazin-1-yl)-1-(1,3-dihydro-2H-isoindol-2-yl)-1,4-dioxobutan-2-amine
0.000016
-
IC50: 16 nM Homo sapiens (2S)-1-[(2S)-2-amino-4-(4-[bis(4-fluorophenyl)methyl]piperazin-1-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
0.000019
-
IC50: 19 nM Homo sapiens (2S)-1-[(2S)-2-amino-4-(3,4-dihydroisoquinolin-2(1H)-yl)-4-oxobutanoyl]pyrrolidine-2-carbonitrile
0.000024
-
IC50: 24 nM Homo sapiens (1S)-1-cyclohexyl-2-(1,3-dihydro-2H-isoindol-2-yl)-2-oxoethanamine
0.000027
-
IC50: 27 nM Homo sapiens (2S)-2-amino-2-cyclohexyl-1-[(2R)-2-(iminomethyl)cyclopentyl]ethanone
0.000078
-
IC50: 78 nM Homo sapiens (1S)-1-cyclohexyl-2-oxo-2-pyrrolidin-1-ylethanamine
0.00015
-
IC50: 150 nM Homo sapiens 1-(1,3-dihydro-2H-isoindol-2-yl)-4-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)-1,4-dioxobutan-2-amine
0.000364
-
IC50: 364 nM Homo sapiens (2S,3S)-3-methyl-1-oxo-1-(1,3-thiazolidin-3-yl)pentan-2-amine
0.000555
-
IC50: 555 nM Homo sapiens 1-(1,3-dihydro-2H-isoindol-2-yl)-4-(3,4-dihydroisoquinolin-2(1H)-yl)-1,4-dioxobutan-2-amine
0.001448
-
IC50: 1448 nM Homo sapiens (1S)-1-cyclohexyl-2-oxo-2-piperidin-1-ylethanamine
0.003016
-
IC50: 3016 nM Homo sapiens (1S)-1-cyclohexyl-2-(3,4-dihydroisoquinolin-2(1H)-yl)-2-oxoethanamine
0.004574
-
IC50: 4574 nM Homo sapiens 6-([2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)ethyl]amino)nicotinonitrile
0.014219
-
i.e.vildagliptin, IC50: 14219 nM Homo sapiens NVP LAF237