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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