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  • Title: The development of benzimidazoles as selective rho kinase inhibitors.
    Author: Sessions EH, Smolinski M, Wang B, Frackowiak B, Chowdhury S, Yin Y, Chen YT, Ruiz C, Lin L, Pocas J, Schröter T, Cameron MD, LoGrasso P, Feng Y, Bannister TD.
    Journal: Bioorg Med Chem Lett; 2010 Mar 15; 20(6):1939-43. PubMed ID: 20167489.
    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 (IC(50)<10nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).
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