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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