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Identification of a potent and selective oxytocin antagonist, from screening a fully encoded differential release
1Department of Lead Discovery, GlaxoSmithKline Medicines Research Centre, Stevenage, Herts, UK. be0897@gsk.com
Bioorganic & Medicinal Chemistry Letters
|June 8, 2001
Abstract:
A library of 1,296 1,4-benzodiazepines was prepared on 160 microM Tentagel beads. Compounds are attached to the beads using orthogonally cleavable linkers. The library was first screened as pools of 30 beads where 50% of the material is released and screened. GW405212X, a selective oxytocin antagonist, was identified by picking single beads from active pools.