Target Validation Information
TTD ID T78356
Target Name Thromboxane-A synthase (TBXAS1)
Type of Target
Clinical trial
Drug Potency against Target CGS-13080 Drug Info IC50 = 3.2 nM [1]
CGS-22652 Drug Info IC50 = 2 nM
ONO-1581 Drug Info IC50 = 3000 nM
Action against Disease Model NV-52 Drug Info NV-52 selectively inhibits TXS in vitro in physiological relevant concentrations, causing a reduction in thromboxane B(2) of </= 40% in association with an increase in prostaglandin E(2). NV-52 is effective in suppressing colonic inflammation in a murine model of inflammatory bowel disease. [2]
References
REF 1 Imidazo[1,5-a]pyridines: a new class of thromboxane A2 synthetase inhibitors. J Med Chem. 1985 Feb;28(2):164-70.
REF 2 Nv-52: a novel thromboxane synthase inhibitor for the treatment of inflammatory bowel disease. Expert Opin Investig Drugs. 2007 Aug;16(8):1255-66.

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