Identification of a potent and selective oxytocin antagonist, from screening a fully encoded differential release combinatorial chemical library

Authors
Evans, B Pipe, A Clark, L Banks, M
Citation
B. Evans et al., Identification of a potent and selective oxytocin antagonist, from screening a fully encoded differential release combinatorial chemical library, BIOORG MED, 11(10), 2001, pp. 1297-1300
Citations number
12
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
10
Year of publication
2001
Pages
1297 - 1300
Database
ISI
SICI code
0960-894X(20010521)11:10<1297:IOAPAS>2.0.ZU;2-L
Abstract
A library of 1296 1,4-benzodiazepines was prepared on 160 muM Tentagel bead s. Compounds are attached to the beads using orthogonally cleavable linkers . The library was first screened as pools of 30 beads where 50% of the mate rial is released and screened. GW405212X, a selective oxytocin antagonist, was identified by picking single beads from active pools. (C) 2001 Elsevier Science Ltd. All rights reserved.