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Abstract #25783 Published in IGR 12-2
The development of benzimidazoles as selective rho kinase inhibitors
Sessions EH; Smolinski M; Wang B; Frackowiak B; Chowdhury S; Yin Y; Chen YT; Ruiz C; Lin L; Pocas JBioorganic and Medicinal Chemistry Letters 2010; 20: 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) <10 nM). This report details the optimization of selectivity for ROCK over other related kinases such as Protein kinase A (PKA).
T.D. Bannister. Department of Molecular Therapeutics, Translational Research Institute, The Scripps Research Institute, 130 Scripps Way, Jupiter, FL 33458, United States. tbannist@scripps.edu
Classification:
11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)
