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BioAssay: AID 436056

Selectivity for CDK2 as proportion of 290 kinases in screen with similar potency; non-selective = 1 highly selective = 0

Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity are poorly defined, and an important step toward understanding the relationship between selectivity, efficacy and safety is the exploration of how inhibitors interact with the human kinome. We present interaction maps for 38 kinase inhibitors across more ..
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 Tested Compounds
 Tested Compounds
All(4)
 
 
Unspecified(4)
 
 
 Tested Substances
 Tested Substances
All(4)
 
 
Unspecified(4)
 
 
 Related BioAssays
 Related BioAssays
AID: 436056
Data Source: ChEMBL (587222)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-07-08
Modify Date: 2013-11-16

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Cyclin-dependent kinase 2; AltName: Full=Cell division protein kinase 2; AltName: Full=p33 protein kinase
Description ..   
Protein Family: Catalytic domain of the Serine/Threonine Kinases, Cyclin-Dependent protein Kinase 2 and 3
Comment ..   

Gene:CDK2     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: A quantitative analysis of kinase inhibitor selectivity.

Abstract: Kinase inhibitors are a new class of therapeutics with a propensity to inhibit multiple targets. The biological consequences of multi-kinase activity are poorly defined, and an important step toward understanding the relationship between selectivity, efficacy and safety is the exploration of how inhibitors interact with the human kinome. We present interaction maps for 38 kinase inhibitors across a panel of 317 kinases representing >50% of the predicted human protein kinome. The data constitute the most comprehensive study of kinase inhibitor selectivity to date and reveal a wide diversity of interaction patterns. To enable a global analysis of the results, we introduce the concept of a selectivity score as a general tool to quantify and differentiate the observed interaction patterns. We further investigate the impact of panel size and find that small assay panels do not provide a robust measure of selectivity.
(PMID: 18183025)
Categorized Comment
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 11678

ChEMBL Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Selectivity activity commentSelectivity activity commentString
2Selectivity standard flagSelectivity standard flagInteger
3Selectivity qualifierSelectivity qualifierString
4Selectivity published valueSelectivity published valueFloat
5Selectivity standard valueSelectivity standard valueFloat

Data Table (Concise)
Classification
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