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

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.

Graphical abstractA series of biphenylmethylamines with affinity for the 5-ht5A receptor was identified by high-throughput screening of array 1, synthesised by high-throughput solid-phase chemistry. Compound 11 was identified as the most potent and selective 5-ht5A receptor antagonist from this series.Figure optionsDownload full-size imageDownload as PowerPoint slide