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

Bioorg Med Chem Lett

High-Throughput Chemistry, Discovery Research, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow Essex CM19 5AW, UK.

Published: September 2005

AI Article Synopsis

  • High-throughput screening of biphenylmethylamines, created through solid-phase chemistry, uncovered compounds that strongly bind to the 5-HT5A receptor.
  • The study explored structure-activity relationships, aiding in the refinement of these compounds.
  • A notable finding was the biphenylmethylamine derivative 11, which emerged as a powerful and selective antagonist for the 5-HT5A receptor.

Article 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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http://dx.doi.org/10.1016/j.bmcl.2005.06.024DOI Listing

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