Document Report Card
Basic Information
ID: ALA1143897
Journal: Bioorg Med Chem Lett
Title: Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 2: SAR of the amine tether.
Authors: Levy DE, Wang DX, Lu Q, Chen Z, Perumattam J, Xu YJ, Higaki J, Dong H, Liclican A, 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 tether joining the basic amine to the indolyl maleimide core. Key interactions with the kinase ATP site and hinge region, predicted by homology modeling, were confirmed.
CiteXplore: 18334295