Target Validation Information
Target ID T76198
Target Name Thromboxane A2 receptor
Target Type
Successful
Drug Potency against Target DALTROBAN Drug Info IC50 = 62 nM [527205]
BM-573 Drug Info IC50 = 240 nM [528239]
Ramatroban Drug Info Ki = 4.3 nM [552029]
L-657925 Drug Info IC50 = 1500 nM [529310]
SQ-29548 Drug Info IC50 = 35.8 nM [529310]
U-44069 Drug Info Ki = 16 nM [529789]
LAROPIPRANT Drug Info IC50 = 770 nM [528672]
References
Ref 527205J Med Chem. 1992 Jun 12;35(12):2202-9.Synthesis and thromboxane A2/prostaglandin H2 receptor antagonistic activity of phenol derivatives.
Ref 528239J Med Chem. 2006 Jun 15;49(12):3701-9.Synthesis and pharmacological evaluation of novel nitrobenzenic thromboxane modulators as antiplatelet agents acting on both the alpha and beta isoforms of the human thromboxane receptor.
Ref 552029Antagonism 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.
Ref 529310J Med Chem. 1991 Apr;34(4):1511-4.Novel synthesis and biochemical properties of an [125I]-labeled photoaffinity probe for thromboxane A2/prostaglandin H2 receptors.
Ref 529310J Med Chem. 1991 Apr;34(4):1511-4.Novel synthesis and biochemical properties of an [125I]-labeled photoaffinity probe for thromboxane A2/prostaglandin H2 receptors.
Ref 529789J Med Chem. 2008 Nov 27;51(22):7094-8.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 responses against carrageenan-induced hyperalgesia.
Ref 528672J Med Chem. 2007 Feb 22;50(4):794-806.Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]-acetic acid (MK-0524).

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