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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
7
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pubmed:dateCreated |
2008-4-3
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pubmed:abstractText |
A family of aryl-substituted maleimides was prepared and studied for their activity against calmodulin dependant kinase. Inhibitory activities against the enzyme ranged from 10nM 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 of the inhibitors. Key interactions with the kinase ATP site and hinge region, predicted by homology modeling, were confirmed.
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
1464-3405
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pubmed:author |
pubmed-author:BonagaLlorenteL,
pubmed-author:DoStevenS,
pubmed-author:DongHanminH,
pubmed-author:DugarSundeepS,
pubmed-author:HigakiJeffreyJ,
pubmed-author:LaneyMaureenM,
pubmed-author:LevyDaniel EDE,
pubmed-author:LiangWeilingW,
pubmed-author:LiclicanAlbertA,
pubmed-author:LuQingQ,
pubmed-author:MavunkelBabuB,
pubmed-author:PerumattamJohnJ,
pubmed-author:SiderisSteveS,
pubmed-author:WangDan-XiongDX,
pubmed-author:XuYong-JinYJ,
pubmed-author:ZhengChenC
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
18
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2399-403
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pubmed:dateRevised |
2010-11-18
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pubmed:meshHeading |
pubmed-meshheading:18337095-Adenosine Triphosphate,
pubmed-meshheading:18337095-Benzene Derivatives,
pubmed-meshheading:18337095-Binding Sites,
pubmed-meshheading:18337095-Calcium-Calmodulin-Dependent Protein Kinase Type 2,
pubmed-meshheading:18337095-Drug Design,
pubmed-meshheading:18337095-Enzyme Inhibitors,
pubmed-meshheading:18337095-Hydrophobic and Hydrophilic Interactions,
pubmed-meshheading:18337095-Indoles,
pubmed-meshheading:18337095-Maleimides,
pubmed-meshheading:18337095-Models, Chemical,
pubmed-meshheading:18337095-Structure-Activity Relationship,
pubmed-meshheading:18337095-Substrate Specificity
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pubmed:year |
2008
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pubmed:articleTitle |
Aryl-indolyl maleimides as inhibitors of CaMKIIdelta. Part 3: Importance of the indole orientation.
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pubmed:affiliation |
Scios, Inc., 6500 Paseo Padre Parkway, Fremont, CA 94555, USA.
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pubmed:publicationType |
Journal Article
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