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BioAssay: AID 435190

Binding constant for full-length PIP5K1A

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(38)
 
 
Active(8)
 
 
Unspecified(30)
 
 
 Tested Substances
 Tested Substances
All(39)
 
 
Active(9)
 
 
Unspecified(30)
 
 
 Related BioAssays
 Related BioAssays
AID: 435190
Data Source: ChEMBL (586356)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-07-08
Modify Date: 2014-08-23

Data Table ( Complete ):           View Active Data    View All Data
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: 8
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)
Comment
Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
Assay Type: Binding
Target Type: Target is a single protein chain
Assay Data Source: Scientific Literature
Protein Target Class: enzyme kinase
Result Definitions
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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
11Kd activity commentKd activity commentString
12Kd standard flagKd standard flagInteger
13Kd qualifierKd qualifierString
14Kd published valueKd published valueFloatμM
15Kd standard valueKd standard valueFloatnM

* Activity Concentration.

Data Table (Concise)
Data Table ( Complete ):     View Active Data    View All Data
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