Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T76198 | ||||
Target Name | Thromboxane A2 receptor (TBXA2R) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Ramatroban | Drug Info | Ki = 4.3 nM | [6] | |
BM-573 | Drug Info | IC50 = 240 nM | [2] | ||
DALTROBAN | Drug Info | IC50 = 62 nM | [1] | ||
L-657925 | Drug Info | IC50 = 1500 nM | [4] | ||
LAROPIPRANT | Drug Info | IC50 = 770 nM | [3] | ||
SQ-29548 | Drug Info | IC50 = 35.8 nM | [4] | ||
U-44069 | Drug Info | Ki = 16 nM | [5] | ||
References | |||||
REF 1 | Synthesis and thromboxane A2/prostaglandin H2 receptor antagonistic activity of phenol derivatives. J Med Chem. 1992 Jun 12;35(12):2202-9. | ||||
REF 2 | Synthesis and pharmacological evaluation of novel nitrobenzenic thromboxane modulators as antiplatelet agents acting on both the alpha and beta iso... J Med Chem. 2006 Jun 15;49(12):3701-9. | ||||
REF 3 | Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydroc... J Med Chem. 2007 Feb 22;50(4):794-806. | ||||
REF 4 | Novel synthesis and biochemical properties of an [125I]-labeled photoaffinity probe for thromboxane A2/prostaglandin H2 receptors. J Med Chem. 1991 Apr;34(4):1511-4. | ||||
REF 5 | cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain... J Med Chem. 2008 Nov 27;51(22):7094-8. | ||||
REF 6 | Antagonism of the prostaglandin D2 receptors DP1 and CRTH2 as an approach to treat allergic diseases. Nat Rev Drug Discov. 2007 Apr;6(4):313-25. | ||||
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