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A comparison of protein kinases inhibitor screening methods using both enzymatic activity and binding affinity determination

Abstract:
Binding assays are increasingly used as a screening method for protein kinase inhibitors; however, as yet only a weak correlation with enzymatic activity-based assays has been demonstrated. We show that the correlation between the two types of assays can be improved using more precise screening conditions. Furthermore a marked improvement in the correlation was found by using kinase constructs containing the catalytic domain in presence of additional domains or subunits.
Publication status:
Published
Peer review status:
Peer reviewed

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Institution:
University of Oxford
Division:
MSD
Department:
NDM
Sub department:
Structural Genomics Consortium
Role:
Author
Publisher:
Public Library of Science
Journal:
PLoS ONE More from this journal
Volume:
9
Issue:
6
Pages:
e98800
Publication date:
2014-06-10
Acceptance date:
2014-04-27
DOI:
EISSN:
1932-6203
ISSN:
1932-6203
Language:
English
Keywords:
UUID:
uuid:8d55f8b2-d046-4af0-a79c-5c4b4a6fd60e
Local pid:
pubs:469645
Source identifiers:
469645
Deposit date:
2014-06-30

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