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Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis
Tao Guo1, Anton E P Adang, Roland E Dolle
1Pharmacopeia, Inc, PO Box 5350, Princeton, NJ 08543-5350, USA.tguo@pharmcop.com
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.
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