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BioAssay: AID 624824

Binding constant for PIP5K1A kinase domain

We tested the interaction of 72 kinase inhibitors with 442 kinases covering >80% of the human catalytic protein kinome. Our data show that, as a class, type II inhibitors are more selective than type I inhibitors, but that there are important exceptions to this trend. The data further illustrate that selective inhibitors have been developed against the majority of kinases targeted by the more ..
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 Tested Compounds
 Tested Compounds
All(72)
 
 
Active(20)
 
 
Unspecified(52)
 
 
 Tested Substances
 Tested Substances
All(72)
 
 
Active(20)
 
 
Unspecified(52)
 
 
AID: 624824
Data Source: ChEMBL (774304)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2012-09-09
Modify Date: 2014-05-26

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Phosphatidylinositol 4-phosphate 5-kinase type-1 alpha; Short=PIP5K1-alpha; Short=PtdIns(4)P-5-kinase 1 alpha; AltName: Full=68 kDa type I phosphatidylinositol 4-phosphate 5-kinase alpha; AltName: Full=Phosphatidylinositol 4-phosphate 5-kinase type I alpha; Short=PIP5KIalpha
Description ..   
Protein Family: PIPKc
Comment ..   

Gene:PIP5K1A     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 20
Description:
Title: Comprehensive analysis of kinase inhibitor selectivity.

Abstract: We tested the interaction of 72 kinase inhibitors with 442 kinases covering >80% of the human catalytic protein kinome. Our data show that, as a class, type II inhibitors are more selective than type I inhibitors, but that there are important exceptions to this trend. The data further illustrate that selective inhibitors have been developed against the majority of kinases targeted by the compounds tested. Analysis of the interaction patterns reveals a class of 'group-selective' inhibitors broadly active against a single subfamily of kinases, but selective outside that subfamily. The data set suggests compounds to use as tools to study kinases for which no dedicated inhibitors exist. It also provides a foundation for further exploring kinase inhibitor biology and toxicity, as well as for studying the structural basis of the observed interaction patterns. Our findings will help to realize the direct enabling potential of genomics for drug development and basic research about cellular signaling.
(PMID: 22037378)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Categorized Comment
Assay Type: Binding

Assay Data Source: Scientific Literature

Assay Test Type: In vitro

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Protein Target Class: enzyme kinase

Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Kd*Kd PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6Kd activity commentKd activity commentString
7Kd standard flagKd standard flagInteger
8Kd qualifierKd qualifierString
9Kd published valueKd published valueFloatnM
10Kd standard valueKd standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Classification
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