Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594743 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
Abstract
A benzothiophene containing Rho kinase inhibitor was identified in an ultra high-throughput enzymatic assay. SAR studies led to inhibitors with low nM enzymatic IC50s, low or sub-μM cellular EC50s in a novel label-free assay, and in vivo efficacy in a monkey model of ocular hypertension.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Robert L. Davis, Mehmet Kahraman, Thomas J. Prins, Yan Beaver, Travis G. Cook, Jessica Cramp, Charmagne S. Cayanan, Elisabeth M.M. Gardiner, Marsha A. McLaughlin, Abbot F. Clark, Mark R. Hellberg, Andrew K. Shiau, Stewart A. Noble, Allen J. Borchardt,