Benzimidazole- and benzoxazole-based inhibitors of Rho kinase
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Updated: Jun 28, 2026

Identification of Mediators of T-cell Receptor Signaling via the Screening of Chemical Inhibitor Libraries
Published on: January 22, 2019
E Hampton Sessions1, Yan Yin, Thomas D Bannister
1Department of Molecular Therapeutics, The Scripps Research Institute Florida, 130 Scripps Way, #2A1, Jupiter, FL 33458, USA.
Abstract:
Inhibitors of Rho kinase have been developed based on two distinct scaffolds, benzimidazoles, and benzoxazoles. SAR studies and efforts to optimize the initial lead compounds are described. Novel selective inhibitors of ROCK-II with excellent potency in both enzyme and cell-based assays were obtained. These inhibitors possess good microsomal stability, low cytochrome P-450 inhibitions and good oral bioavailability.
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