Inhibitors | Comment | Organism | Structure |
---|---|---|---|
6-(aminomethyl)-1,3-dimethyl-7-(1-methylpiperazinium)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione | compound exhibits low exposure, high clearance, high selectivity for dipeptidyl peptidase IV over dipeptidyleptidase DPP8 | Homo sapiens | |
6-(aminomethyl)-1,3-dimethyl-7-(morpholin-4-yl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione | compound exhibits excellent exposure, low clearance, high selectivity for dipeptidyl peptidase IV over dipeptidyleptidase DPP8 | Homo sapiens | |
7-amino-6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione | compound exhibits good exposure, moderate clearance, high selctivity for dipeptidyl peptidase IV over dipeptidyleptidase DPP8 | Homo sapiens | |
7-amino-6-(aminomethyl)-5-(2-fluoro-6-methoxyphenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione | compound exhibits good exposure, moderate clearance, high selectivity for dipeptidyl peptidase IV over dipeptidyleptidase DPP8 | Homo sapiens | |
additional information | interactions important for binding are the pi-pi stacking interaction of the pyridopyrimidine-dione ring with Tyr547, its H-bond interaction to the backbone NH of Tyr631 and the OH of Ser630, and polar interactions between the basic amine and Glu205, Glu206 and Tyr662, high selectivity for dipeptidyl peptidase IV over dipeptidyleptidase DPP8 | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P27487 | - |
- |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000046 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 6-(aminomethyl)-1,3-dimethyl-7-(morpholin-4-yl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione | |
0.0000048 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 7-amino-6-(aminomethyl)-5-(2-bromo-5-fluorophenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione | |
0.0000099 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 6-(aminomethyl)-1,3-dimethyl-7-(1-methylpiperazinium)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione | |
0.00002 | - |
pH not specified in the publication, temperature not specified in the publication | Homo sapiens | 7-amino-6-(aminomethyl)-5-(2-fluoro-6-methoxyphenyl)-1,3-dimethylpyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione |