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.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2008.02.059 | DOI Listing |
Publication Analysis
Top Keywords
aryl-indolyl maleimides
4
maleimides inhibitors
4
inhibitors camkiidelta
4
camkiidelta sar
4
sar aryl
4
aryl region
4
region family
4
family aryl-substituted
4
aryl-substituted maleimides
4
maleimides prepared
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!