Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.
Bioorganic & medicinal chemistry letters 2005 Sep 15; 15(18):4014-8
Corbett D DF, Heightman T TD, Moss S SF, Bromidge S SM, Coggon S SA, Longley M MJ, Roa A AM, Williams J JA, Thomas D DR
High-Throughput Chemistry, Discovery Research, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow Essex CM19 5AW, UK. david.f.corbett@gsk.com
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.