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BioAssay: AID 720181

Millipore: Percentage of residual kinase activity of GSK3A at 1uM relative to control. Control inhibitor: Staurosporine at 10.0uM. Buffer: 8 mM MOPS pH 7.0, 0.2 mM EDTA

Despite the development of a number of efficacious kinase inhibitors, the strategies for rational design of these compounds have been limited by target promiscuity. In an effort to better understand the nature of kinase inhibition across the kinome, especially as it relates to off-target effects, we screened a well-defined collection of kinase inhibitors using biochemical assays for inhibitory more ..
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 Tested Compounds
 Tested Compounds
All(158)
 
 
Unspecified(158)
 
 
 Tested Substances
 Tested Substances
All(159)
 
 
Unspecified(159)
 
 
 Related BioAssays
 Related BioAssays
AID: 720181
Data Source: ChEMBL (887927)
Depositor Category: Other
BioAssay Version:
Deposit Date: 2013-06-29
Modify Date: 2014-05-26

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Glycogen synthase kinase-3 alpha; Short=GSK-3 alpha; AltName: Full=Serine/threonine-protein kinase GSK3A
Description ..   
Protein Family: Protein Kinases, catalytic domain
Comment ..   

Gene:GSK3A     Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.

Abstract: Despite the development of a number of efficacious kinase inhibitors, the strategies for rational design of these compounds have been limited by target promiscuity. In an effort to better understand the nature of kinase inhibition across the kinome, especially as it relates to off-target effects, we screened a well-defined collection of kinase inhibitors using biochemical assays for inhibitory activity against 234 active human kinases and kinase complexes, representing all branches of the kinome tree. For our study we employed 158 small molecules initially identified in the literature as potent and specific inhibitors of kinases important as therapeutic targets and/or signal transduction regulators. Hierarchical clustering of these benchmark kinase inhibitors on the basis of their kinome activity profiles illustrates how they relate to chemical structure similarities and provides new insights into inhibitor specificity and potential applications for probing new targets. Using this broad dataset, we provide a framework for assessing polypharmacology. We not only discover likely off-target inhibitor activities and recommend specific inhibitors for existing targets, but also identify potential new uses for known small molecules.
Categorized Comment
Assay Type: Binding

Assay Data Source: Millipore Kinase Screening

Assay Test Type: In vitro

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Residual Activity activity commentResidual Activity activity commentString
2Residual Activity standard flagResidual Activity standard flagInteger
3Residual Activity qualifierResidual Activity qualifierString
4Residual Activity published valueResidual Activity published valueFloat%
5Residual Activity standard valueResidual Activity standard valueFloat%

Data Table (Concise)
Classification
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