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Updated: Nov 28, 2025

RhoC GTPase Activation Assay
Published on: August 22, 2010
ROCK inhibitors 4: Structure-activity relationship studies of 7-azaindole-based rho kinase (ROCK) inhibitors
Upul K Bandarage1, John Court1, Huai Gao1
1Vertex Pharmaceuticals Incorporated, 50 Northern Avenue, Boston, MA 02210, USA.
Abstract:
Rho kinase (ROCK) inhibitors are of therapeutic value for the treatment of disorders such as hypertension and glaucoma, and potentially of wider use against diseases such as cancer and multiple sclerosis. We previously reported a series of potent and selective ROCK inhibitors based on a substituted 7-azaindole scaffold. Here we extend the SAR exploration of the 7-azaindole series to identify leads for further evaluation. New compounds such as 16, 17, 19, 21 and 22 showed excellent ROCK potency and protein kinase A (PKA) selectivity, combined with microsome and hepatocyte stability.
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