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The development of benzimidazoles as selective rho kinase inhibitors |
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| 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 |
| Affiliation: | Department of Molecular Therapeutics and Translational Research Institute, The Scripps Research Institute, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, USA |
| 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). |
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