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BioAssay: AID 436057

Selectivity for ERBB2 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(1)
 
 
Unspecified(1)
 
 
 Tested Substances
 Tested Substances
All(1)
 
 
Unspecified(1)
 
 
 Related BioAssays
 Related BioAssays
AID: 436057
Data Source: ChEMBL (587223)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-07-08
Modify Date: 2014-05-24

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Receptor tyrosine-protein kinase erbB-2; AltName: Full=Metastatic lymph node gene 19 protein; Short=MLN 19; AltName: Full=Proto-oncogene Neu; AltName: Full=Proto-oncogene c-ErbB-2; AltName: Full=Tyrosine kinase-type cell surface receptor HER2; AltName: Full=p185erbB2; AltName: CD_antigen=CD340; Flags: Precursor
Description ..   
Protein Family: Catalytic domain of the Protein Tyrosine Kinase, HER2
Comment ..   

Gene:ERBB2     Related Protein 3D Structures     More BioActivity Data..
Tested Compound:
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
Assay Type: Binding

Assay Data Source: Scientific Literature

BAO: Assay Format: biochemical format

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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