| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374333 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
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 0.7 mM to 3 μM with retention of good ligand efficiency and incorporation of reasonable physical properties, off-target profile, and rat pharmacokinetics.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
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,