Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T78356 | ||||
Target Name | Thromboxane-A synthase (TBXAS1) | ||||
Type of Target |
Clinical trial |
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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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