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

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 μM) and 2 (EC 50 =3.9 μM), based on which a focused combinatorial library with a total of 31,372 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.