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  3. Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry

Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry

  • Bioorg Med Chem Lett. 2005 Sep 15;15(18):4014-8. doi: 10.1016/j.bmcl.2005.06.024.
David F Corbett 1,  Tom D Heightman,  Stephen F Moss,  Steven M Bromidge,  Sara A Coggon,  Mark J Longley,  Ana Maria Roa,  Jennifer A Williams,  David R Thomas
Affiliations

Affiliation

  • 1 High-Throughput Chemistry, Discovery Research, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow Essex CM19 5AW, UK. david.f.corbett@gsk.com
PMID: 16002289 DOI: 10.1016/j.bmcl.2005.06.024
Abstract

High-throughput screening of an array of biphenylmethylamines synthesised by high-throughput solid-phase chemistry resulted in the identification of compounds with high-affinity for the 5-ht5A receptor. The structure-activity relationship within this series and further array synthesis led to the identification of the biphenylmethylamine derivative 11, a potent and selective 5-ht5A receptor antagonist.

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