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1: Bioorg Med Chem Lett. 2005 Sep 15;15(18):4014-8.Click here to read Links

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

Corbett DF, Heightman TD, Moss SF, Bromidge SM, Coggon SA, Longley MJ, Roa AM, Williams JA, Thomas 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.

PMID: 16002289 [PubMed - indexed for MEDLINE]

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