Aryl-indolyl maleimides as inhibitors of CaMKIIδ. Part 1: SAR of the aryl region

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 7, 2008, Pages 2390-2394

  Levy, Daniel E ^a   Wang, Dan Xiong ^a   Lu, Qing ^a   Chen, Zheng ^a   Perumattam, John ^a   Xu, Yong jin ^a   Liclican, Albert ^a   Higaki, Jeffrey ^a   Dong, Hanmin ^a   Laney, Maureen ^a   Mavunkel, Babu ^a   Dugar, Sundeep ^a  

^a SCIOS INC   (United States)

Author keywords

Calmodulin; Inhibitors; Kinase; Maleimides

Indexed keywords

HYDROGEN; INDOLE DERIVATIVE; MALEIMIDE DERIVATIVE; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; PROTEIN KINASE (CALCIUM,CALMODULIN) II; PROTEIN KINASE INHIBITOR;

ARTICLE; CALCIUM SIGNALING; COMPARATIVE STUDY; DRUG POTENCY; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME INHIBITION; HYDROGEN BOND; HYDROPHOBICITY; MOLECULAR INTERACTION; MOLECULAR MODEL; PREDICTION; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION;

ADENOSINE TRIPHOSPHATE; BENZENE DERIVATIVES; BINDING SITES; CALCIUM-CALMODULIN-DEPENDENT PROTEIN KINASE TYPE 2; DRUG DESIGN; ENZYME INHIBITORS; INDOLES; MALEIMIDES; MODELS, CHEMICAL; STRUCTURE-ACTIVITY RELATIONSHIP; SUBSTRATE SPECIFICITY;

EID: 41149166383     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.02.059     Document Type: Article

References (12)

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9. Compound 1 was obtained from Calbiochem-Novabiochem Corporation, catalog # 203294.
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11. 2, 8.3 μg/ml calmodulin, 25 μM [His 5] Autocamtide-2, 120 nM [g-33P]ATP) and incubated at rt for 3 min. Reactions were terminated by transferring 25 μl to a UNIFILTER 96-well P81microplate (Whatman, UK), pre-wet with 15 μl 1% phosphoric acid. After 10 min, the plate was washed 3 times with 1% phosphoric acid and one time with 95% ethanol on a BiomekFX (Beckman Coulter, CA) equipped with a vacuum manifold. Plates were dried for approximately 60 min, scintillant was added to the wells, and the plates were read on a TopCount NXT Microplate Scintillation and Luminescence Counter (Perkin-Elmer, MA).
12. Compound 14r was obtained from Calbiochem-Novabiochem Corporation, catalog # 557508.