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Literature summary for 3.4.14.5 extracted from

  • Kurukulasuriya, R.; Rohde, J.J.; Szczepankiewicz, B.G.; Basha, F.; Lai, C.; Jae, H.S.; Winn, M.; Stewart, K.D.; Longenecker, K.L.; Lubben, T.W.; Ballaron, S.J.; Sham, H.L.; von Geldern, T.W.
    Xanthine mimetics as potent dipeptidyl peptidase IV inhibitors (2006), Bioorg. Med. Chem. Lett., 16, 6226-6230.
    View publication on PubMed
Search for more literature for 3.4.14.5

Inhibitors

Inhibitors Comment Organism Structure
1-(3-benzyl-4-oxido-3H-imidazo[4,5-b]pyridin-2-yl)piperidin-3-aminium
-
 Homo sapiens
1-[1-(2-chlorobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
 Homo sapiens
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
-
 Homo sapiens
1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
-
 Rattus norvegicus
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium potent and selective DPPIV inhibitor, but it showed a significant loss of activity in the presence of plasma Homo sapiens
1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
 Rattus norvegicus
1-[1-(2-cyanobenzyl)-5-methyl-4-oxo-4,5-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
-
 Homo sapiens
1-[1-(2-cyanobenzyl)-6-methyl-7-oxo-3a,6,7,7a-tetrahydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
-
 Homo sapiens
1-[1-(3-cyanobenzyl)-6-methyl-7-oxo-6,7-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
-
 Homo sapiens
1-[1-[3-(cyanomethyl)benzyl]-6-methyl-7-oxo-6,7-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
-
 Homo sapiens
1-[4,9-dioxo-1-[2-(trifluoromethyl)benzyl]-4,9-dihydro-1H-naphtho[2,3-d]imidazol-2-yl]piperidin-3-aminium
-
 Homo sapiens
1-[5-benzyl-1-(3-cyanobenzyl)-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
 Homo sapiens
1-[5-methyl-4,6-dioxo-1-[2-(trifluoromethoxy)benzyl]-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
 Homo sapiens
1-[5-methyl-4,6-dioxo-1-[2-(trifluoromethyl)benzyl]-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
-
 Homo sapiens
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
-
 Homo sapiens
1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
-
 Rattus norvegicus
1-[7-fluoro-6-methoxy-1-[2-(trifluoromethyl)benzyl]-1H-benzimidazol-2-yl]piperidin-3-aminium
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus P14740
-
-

Synonyms

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
-
 Homo sapiens 1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
0.000002
-
 in absence of plasma Rattus norvegicus 1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
0.000002
-
 potent and selective DPPIV inhibitor, but it showed a significant loss of activity in the presence of plasma Homo sapiens 1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
0.000003
-
 in absence of plasma Rattus norvegicus 1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
0.000005
-
-
 Homo sapiens 1-[1-(2-cyanobenzyl)-6-methyl-7-oxo-3a,6,7,7a-tetrahydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
0.000007
-
 in presence of 18% plasma Rattus norvegicus 1-[7-(2-cyanobenzyl)-1,3-dimethyl-2,6-dioxo-2,3,4,5,6,7-hexahydro-1H-purin-8-yl]piperidin-3-aminium
0.000009
-
-
 Homo sapiens 1-[1-(2-chlorobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
0.00001
-
-
 Homo sapiens 1-[5-methyl-4,6-dioxo-1-[2-(trifluoromethyl)benzyl]-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
0.000011
-
-
 Homo sapiens 1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
0.000011
-
-
 Homo sapiens 1-[1-[3-(cyanomethyl)benzyl]-6-methyl-7-oxo-6,7-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
0.000017
-
 in absence of plasma Rattus norvegicus 1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
0.000022
-
-
 Homo sapiens 1-[5-methyl-4,6-dioxo-1-[2-(trifluoromethoxy)benzyl]-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
0.000024
-
 in presence of 18% plasma Rattus norvegicus 1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
0.000025
-
-
 Homo sapiens 1-[4,9-dioxo-1-[2-(trifluoromethyl)benzyl]-4,9-dihydro-1H-naphtho[2,3-d]imidazol-2-yl]piperidin-3-aminium
0.000029
-
-
 Homo sapiens 1-[5-benzyl-1-(3-cyanobenzyl)-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
0.000057
-
-
 Homo sapiens 1-[7-fluoro-6-methoxy-1-[2-(trifluoromethyl)benzyl]-1H-benzimidazol-2-yl]piperidin-3-aminium
0.00026
-
-
 Homo sapiens 1-[1-(2-cyanobenzyl)-5-methyl-4-oxo-4,5-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium
0.0003
-
-
 Homo sapiens 1-(3-benzyl-4-oxido-3H-imidazo[4,5-b]pyridin-2-yl)piperidin-3-aminium
0.00045
-
-
 Homo sapiens 1-[1-(2-cyanobenzyl)-4,5-bis(methylcarbamoyl)-1H-imidazol-2-yl]piperidin-3-aminium
0.0006
-
 in presence of 18% plasma Rattus norvegicus 1-[1-(2-cyanobenzyl)-5-methyl-4,6-dioxo-1,4,5,6-tetrahydropyrrolo[3,4-d]imidazol-2-yl]piperidin-3-aminium
0.0012
-
-
 Homo sapiens 1-[1-(3-cyanobenzyl)-6-methyl-7-oxo-6,7-dihydro-1H-imidazo[4,5-d]pyridazin-2-yl]piperidin-3-aminium