Application | Comment | Organism |
---|---|---|
pharmacology | inhibitor N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate dose-dependently inhibits thrombus formation in a rabbit thrombosis model | Oryctolagus cuniculus |
pharmacology | inhibitor N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate dose-dependently inhibits thrombus formation in a rat thrombosis model. Bleeding time in rats is not significantly prolonged at an antithrombotic dose | Rattus norvegicus |
pharmacology | presence of inhibitor N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate prolongs the activated partial thromboplastin time, prothrombin time and thrombin time in plasma. It does not impair human platelet aggregation induced by ADP or thromboxane A2 receptor agonist U46619. Thrombin-induced platelet aggregation is inhibited with IC50 value of 2.9 microM | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate | i.e. DU-176b. Presence prolongs the activated partial thromboplastin time, prothrombin time and thrombin time in plasma. It does not impair human platelet aggregation induced by ADP or thromboxane A2 receptor agonist U46619. Thrombin-induced platelet aggregation is inhibited with IC50 value of 2.9 microM | Homo sapiens | |
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate | i.e. DU-176b. Dose-dependently inhibits thrombus formation in a rabbit thrombosis model | Oryctolagus cuniculus | |
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate | i.e. DU-176b dose-dependently inhibits thrombus formation in a rat thrombosis model. Bleeding time in rats is not significantly prolonged at an antithrombotic dose | Rattus norvegicus |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Oryctolagus cuniculus | - |
- |
- |
Rattus norvegicus | - |
- |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
benzoyl-Ile-Glu(gamma-O-methyl)-Gly-Arg-4-nitroanilide + N-benzoyl-Ile-Glu-Gly-Arg-4-nitroanilide + H2O | mixed substrate | Homo sapiens | benzoyl-Ile-Glu(gamma-O-methyl)-Gly-Arg + N-benzoyl-Ile-Glu-Gly-Arg + 4-nitroaniline | - |
? | |
benzoyl-Ile-Glu(gamma-O-methyl)-Gly-Arg-4-nitroanilide + N-benzoyl-Ile-Glu-Gly-Arg-4-nitroanilide + H2O | mixed substrate | Rattus norvegicus | benzoyl-Ile-Glu(gamma-O-methyl)-Gly-Arg + N-benzoyl-Ile-Glu-Gly-Arg + 4-nitroaniline | - |
? | |
benzoyl-Ile-Glu(gamma-O-methyl)-Gly-Arg-4-nitroanilide + N-benzoyl-Ile-Glu-Gly-Arg-4-nitroanilide + H2O | mixed substrate | Oryctolagus cuniculus | benzoyl-Ile-Glu(gamma-O-methyl)-Gly-Arg + N-benzoyl-Ile-Glu-Gly-Arg + 4-nitroaniline | - |
? |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.000000561 | - |
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate | pH 7.4, 30°C | Homo sapiens | |
0.000000715 | - |
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate | pH 7.4, 30°C | Oryctolagus cuniculus | |
0.000007 | - |
N-(5-chloropyridin-2-yl)-N'-[(1S,2R,4S)-4-(N,N-dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)-cyclohexyl]ethanediamine 4-toluenesulfonate monohydrate | pH 7.4, 30°C | Rattus norvegicus |