title: 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 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.
authors.affiliation: Pharmacopeia, Inc, PO Box 5350, Princeton, NJ 08543-5350, USA.tguo@pharmcop.com
authors.forename: Tao
authors.initials: T
authors.lastname: Guo
authors.forename: Anton E P
authors.initials: AE
authors.lastname: Adang
authors.forename: Roland E
authors.initials: RE
authors.lastname: Dolle
authors.forename: Guizhen
authors.initials: G
authors.lastname: Dong
authors.forename: Dan
authors.initials: D
authors.lastname: Fitzpatrick
authors.forename: Peng
authors.initials: P
authors.lastname: Geng
authors.forename: Koc-Kan
authors.initials: KK
authors.lastname: Ho
authors.forename: Steven G
authors.initials: SG
authors.lastname: Kultgen
authors.forename: Ruiyan
authors.initials: R
authors.lastname: Liu
authors.forename: Edward
authors.initials: E
authors.lastname: McDonald
authors.forename: Brian F
authors.initials: BF
authors.lastname: McGuinness
authors.forename: Kurt W
authors.initials: KW
authors.lastname: Saionz
authors.forename: Kenneth J
authors.initials: KJ
authors.lastname: Valenzano
authors.forename: Nicole C R
authors.initials: NC
authors.lastname: van Straten
authors.forename: Dan
authors.initials: D
authors.lastname: Xie
authors.forename: Maria L
authors.initials: ML
authors.lastname: Webb
mesh_terms: D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D011962:Receptors, FSH / Q000819:agonists* / Q000737:chemistry / Q000378:metabolism
chemical_list: D011962:Receptors, FSH