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  • Title: Hit to lead account of the discovery of bisbenzamide and related ureidobenzamide inhibitors of Rho kinase.
    Author: Morwick T, Büttner FH, Cywin CL, Dahmann G, Hickey E, Jakes S, Kaplita P, Kashem MA, Kerr S, Kugler S, Mao W, Marshall D, Paw Z, Shih CK, Wu F, Young E.
    Journal: J Med Chem; 2010 Jan 28; 53(2):759-77. PubMed ID: 20000469.
    Abstract:
    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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