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ID: ALA1147492

Journal: Bioorg Med Chem Lett

Title: Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis.

Authors: Guo T, Adang AE, Dolle RE, Dong G, Fitzpatrick D, Geng P, Ho KK, Kultgen SG, Liu R, McDonald E, McGuinness BF, Saionz KW, Valenzano KJ, van Straten NC, Xie D, Webb ML.

Abstract: High-throughput screening of two million compounds in 37 distinct encoded combinatorial libraries using FSH receptor transfected cells provided small molecule agonists such as 1 (EC(50)=3 microM) and 2 (EC(50)=3.9 microM), based on which a focused combinatorial library with a total of 31372 compounds was designed, synthesized, and screened to reveal 72 novel biaryl FSH receptor agonists such as 8a-c as well as a unique combinatorial SAR.

CiteXplore: 15026056

DOI: 10.1016/j.bmcl.2004.01.042