Document Detail


High concentration electrophysiology-based fragment screen: Discovery of novel acid-sensing ion channel 3 (ASIC3) inhibitors.
MedLine Citation:
PMID:  21257308     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
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.
Authors:
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
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2010-12-28
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  -     ISSN:  1464-3405     ISO Abbreviation:  -     Publication Date:  2010 Dec 
Date Detail:
Created Date:  2011-1-24     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier Ltd. All rights reserved.
Affiliation:
Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA.
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