| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T36483 | ||||
| Target Name | Thrombin receptor | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | Vorapaxar | Drug Info | Ki = 2.7 nM | ||
| SCH-205831 | Drug Info | IC50 = 11 nM | [528902] | ||
| Action against Disease Model | Vorapaxar | 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. | [552904] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | Studies in proteinase-activated receptor-1(PAR(1)) knockout mice have shown that this receptor plays a major role in orchestrating the interplay between coagulation, inflammation and lung fibrosis. This review will focus on our current understanding of excessive procoagulant signalling in acute and chronic lung injury and will highlight the novel opportunities that this may present for therapeutic intervention. | ||||
| References | |||||
| Ref 552904 | 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. | ||||
| Ref 528902 | Bioorg Med Chem Lett. 2007 Aug 15;17(16):4509-13. Epub 2007 Jun 15.Himbacine derived thrombin receptor (PAR-1) antagonists: SAR of the pyridine ring. | ||||
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