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    
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.
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
Related Documents :
9367728 - In vitro effects of secondary plant compounds on germination of blastospores of the ent...
21292858 - Alanine-scanning mutagenesis of selected residues in the n-terminal region alters the f...
7428958 - Possible role of endogenous toxigenic lipids in the carbon tetrachloride poisoned hepat...
7492988 - Direct effect of 12(s)-hydroxyeicosatetraenoic acid on rat crystalline lens is perturba...
7209958 - Cuticle and mucous glands in the oesophagus of an annelid (nereis virens).
22059918 - Partial replacement of sodium chloride with potassium chloride in dry fermented sausage...
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.
Department of Medicinal Chemistry, Merck Research Laboratories, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA.
Export Citation:
APA/MLA Format     Download EndNote     Download BibTex
MeSH Terms

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

Previous Document:  Improved tolerance to bile salts of aggregated Bifidobacterium longum produced during continuous cul...
Next Document:  Discovery of a potent series of non-steroidal non ?-trifluoromethyl carbinol glucocorticoid receptor...