Fragment-based discovery of 6-substituted isoquinolin-1-amine based ROCK-I inhibitors.


Fragment-based NMR screening of a small literature focused library led to identification of a historical thrombin/FactorXa building block, 17A, that was found to be a ROCK-I inhibitor. In the absence of an X-ray structure, fragment growth afforded 6-substituted isoquinolin-1-amine derivatives which were profiled in the primary ROCK-I IMAP assay. Compounds… (More)
DOI: 10.1016/j.bmcl.2010.11.060

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