High concentration electrophysiology-based fragment screen: Discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors

Scott E. Wolkenberg,Zhijian Zhao,James J. Mulhearn,Scott T. Harrison,John M. Sanders,Matthew J. Cato,Aneta Jovanovska,Jacqueline Panigel,Sean P. Cook,Darrell A. Henze,Stefanie A. Kane,George D. Hartman,James C. Barrow

Bioorganic & Medicinal Chemistry Letters（2011）

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摘要

The Merck Fragment Library was screened versus acid-sensing ion channel 3 (ASIC3), a novel target for the treatment of pain. Fragment hits were optimized using two strategies, and potency was improved from 0.7mM to 3μM with retention of good ligand efficiency and incorporation of reasonable physical properties, off-target profile, and rat pharmacokinetics.

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关键词

Acid-sensing ion channel 3,Fragment screening,Electrophysiology

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