| Target Validation Information | |||||
|---|---|---|---|---|---|
| TTD ID | T36483 | ||||
| Target Name | Proteinase activated receptor 1 (F2R) | ||||
| Type of Target |
Successful |
||||
| Drug Potency against Target | Vorapaxar | Drug Info | Ki = 2.7 nM | ||
| SCH-205831 | Drug Info | IC50 = 11 nM | [1] | ||
| Action against Disease Model | Vorapaxar | Drug Info | SCH 530348 inhibited thrombosis in a dose-dependent manner in the Folts model of thrombosis in anesthetized cynomolgus monkeys. In h uMan platelet-rich plasma, SCH 530348 inhibited thrombin induced and TRAP-induced platelet aggregation with IC50 values of 47 and 25 nM, respectively, without affecting the aggregation induced by ADP, thromboxane A2 mimetic U46619, or collagen. | [2] | |
| References | |||||
| REF 1 | Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4509-13. | ||||
| REF 2 | Basic and translational research on proteinase-activated receptors: antagonism of the proteinase-activated receptor 1 for thrombin, a novel approach to antiplatelet therapy for atherothrombotic disease. J Pharmacol Sci. 2008 Dec;108(4):433-8. | ||||
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