Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.
JOURNAL OF MEDICINAL CHEMISTRY(2010)
Abstract
A highly selective series of bisbenzamide inhibitors of Rho-associated coiled-coil forming protein kinase (ROCK) and a related ureidoberizamide series, both identified by high throughput screening (HTS), are described. Details of the lilt validation and lead generation process, Including structure-activity relationship (SAR) studies, a selectivity assessment, target-independent profiling (TIP) results, and an analysis of functional activity using a rat aortic ring assay are discussed.
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Key words
rho kinase
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