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The development of benzimidazoles as selective rho kinase inhibitors

, : The development of benzimidazoles as selective rho kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 20(6): 1939-1943

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 (IC(50)<10nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).


PMID: 20167489

DOI: 10.1016/j.bmcl.2010.01.124

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