Protein Information

Name Factor Xa
Synonyms Coagulation factor X; F10; Fx; Coagulation factor X precursor; FXA; Factor Xa; Prothrombinase; Stuart factor…

Compound Information

Name biphenyl
CAS 1,1′-biphenyl

Reference List

PubMed Abstract RScore(About this table)
18550370 Qiao JX, Cheney DL, Alexander RS, Smallwood AM, King SR, He K, Rendina AR, Luettgen JM, Knabb RM, Wexler RR, Lam PY: Achieving structural diversity using the perpendicular conformation of alpha-substituted phenylcyclopropanes to mimic the bioactive conformation of ortho-substituted biphenyl P4 moieties: discovery of novel, highly potent inhibitors of Factor Xa. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4118-23. Epub 2008 May 29.
82(1,1,1,2) Details
19721266 Jia ZJ, Scarborough RM, Zhang P, Halfon S, Arfsten AE, Sinha U, Zhu BY: Design, synthesis and discovery of 1-(2-(6-Chloro-3-methylsulfonyl)-naphthyl)-1H-pyrazole-5-carboxylamides as highly potent factor Xa inhibitors. Chem Pharm Bull. 2009 Sep;57(9):1004-7.

Based upon the biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides reported in our previous communications, we designed and discovered 2-(6-chloro-3-methylsulfonyl)-naphthyl as an optimal factor Xa S1 binding element.
63(0,2,2,3) Details
19193009 de Candia M, Liantonio F, Carotti A, De Cristofaro R, Altomare C: Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: inhibitors of factor Xa and platelet aggregation. J Med Chem. 2009 Feb 26;52(4):1018-28.

Two congeners of N-{[3-(1,1'-biphenyl-4-yl) methoxy] phenyl}piperidine-4-carboxamide (7m and 7p) proved to be potent FXa-selective inhibitors (K (i) = 130 and 57 nM, respectively) and antiplatelet agents and were identified as leads for developing new dual function antithrombotic drugs.
2(0,0,0,2) Details