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
  • 1. High-Throughput Chemistry, Discovery Research, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow Essex CM19 5AW, UK. [email protected]
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.

Products