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ID: ALA1143885
Journal: Bioorg Med Chem Lett
Title: Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 1: SAR of the aryl region.
Authors: Levy DE, Wang DX, Lu Q, Chen Z, Perumattam J, Xu YJ, Liclican A, Higaki J, Dong H, Laney M, Mavunkel B, Dugar S.
Abstract: A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 34nM to >20microM and were dependant upon both the nature of the aryl group and the hydrogen bond donating potential of the maleimide ring. Key interactions with the kinase ATP site and hinge region were found to be consistent with homology modeling predictions.
CiteXplore: 18334294