| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1371940 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
Rho Kinase (ROCK) is a serine/threonine kinase whose inhibition could prove beneficial in numerous therapeutic areas. We have developed a promising class of ATP-competitive inhibitors based upon a benzimidazole scaffold, which show excellent potency toward ROCK (IC50 <10 nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
E. Hampton Sessions, Michael Smolinski, Bo Wang, Bozena Frackowiak, Sarwat Chowdhury, Yan Yin, Yen Ting Chen, Claudia Ruiz, Li Lin, Jennifer Pocas, Thomas Schröter, Michael D. Cameron, Philip LoGrasso, Yangbo Feng, Thomas D. Bannister,