Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1359538 | Bioorganic & Medicinal Chemistry Letters | 2014 | 6 Pages |
Abstract
Herein we report the discovery and SAR of an indole-based protease activated receptor-4 (PAR-4) antagonist scaffold derived from a similarity search of the Vanderbilt HTS collection, leading to MLPCN probe ML354 (VU0099704). Using a novel PAC-1 fluorescent αIIbβ3 activation assay this probe molecule antagonist was found to have an IC50 of 140 nM for PAR-4 with 71-fold selectivity versus PAR-1 (PAR-1IC50 = 10 μM).
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Wandong Wen, Summer E. Young, Matthew T. Duvernay, Michael L. Schulte, Kellie D. Nance, Bruce J. Melancon, Julie Engers, Charles W. Locuson II, Michael R. Wood, J. Scott Daniels, Wenjun Wu, Craig W. Lindsley, Heidi E. Hamm, Shaun R. Stauffer,