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Hit to Lead Account of the Discovery of Bisbenzamide and Related Ureidobenzamide Inhibitors of Rho Kinase

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journal contribution
posted on 28.01.2010, 00:00 by Tina Morwick, Frank H. Büttner, Charles L. Cywin, Georg Dahmann, Eugene Hickey, Scott Jakes, Paul Kaplita, Mohammed A. Kashem, Steven Kerr, Stanley Kugler, Wang Mao, Daniel Marshall, Zofia Paw, Cheng-Kon Shih, Frank Wu, Erick Young
A highly selective series of bisbenzamide inhibitors of Rho-associated coiled-coil forming protein kinase (ROCK) and a related ureidobenzamide series, both identified by high throughput screening (HTS), are described. Details of the hit 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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