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  • Title: Triazine and pyrimidine based ROCK inhibitors with efficacy in spontaneous hypertensive rat model.
    Author: Ho KK, Beasley JR, Belanger L, Black D, Chan JH, Dunn D, Hu B, Klon A, Kultgen SG, Ohlmeyer M, Parlato SM, Ray PC, Pham Q, Rong Y, Roughton AL, Walker TL, Wright J, Xu K, Xu Y, Zhang L, Webb M.
    Journal: Bioorg Med Chem Lett; 2009 Nov 01; 19(21):6027-31. PubMed ID: 19800787.
    Abstract:
    The profile of a series of triazine and pyrimidine based ROCK inhibitors is described. An initial binding mode was established based on a homology model and the proposed interactions are consistent with the observed SAR. Compounds from the series are potent in a cell migration assay and possess a favorable kinase selectivity. In vivo activity was demonstrated for compound 1A in a spontaneous hypertensive rat model.
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