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BioAssay: AID 436051

Binding constant for RPS6KA5(Kin.Dom.2 - N-terminal) kinase domain

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(3)
 
 
Unspecified(35)
 
 
 Tested Substances
 Tested Substances
All(38)
 
 
Active(3)
 
 
Unspecified(35)
 
 
 Related BioAssays
 Related BioAssays
AID: 436051
Data Source: ChEMBL (587217)
Depositor Category: Literature, Extracted
BioAssay Version:
Deposit Date: 2010-07-08
Modify Date: 2013-11-16

Data Table ( Complete ):           Active    All
Target
Sequence: RecName: Full=Ribosomal protein S6 kinase alpha-5; Short=S6K-alpha-5; AltName: Full=90 kDa ribosomal protein S6 kinase 5; AltName: Full=Nuclear mitogen- and stress-activated protein kinase 1; AltName: Full=RSK-like protein kinase; Short=RSKL
Description ..   
Protein Family: N-terminal catalytic domain of the Protein Serine/Threonine Kinase, Mitogen and stress-activated kinase 1
Comment ..   

Gene:RPS6KA5     Related Protein 3D Structures     More BioActivity Data..
BioActive Compounds: 3
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
ChEMBL Assay Type: Binding

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 10850

ChEMBL Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Kd*Kd PubChem standard valueFloatμM
2BEIBinding Efficiency Index(nM)Float
3SEISurface 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 binding domainsKd binding domainsString
12Kd activity commentKd activity commentString
13Kd standard flagKd standard flagInteger
14Kd qualifierKd qualifierString
15Kd published valueKd published valueFloatμM
16Kd standard valueKd standard valueFloatnM
17Kd binding domainsKd binding domainsString

* Activity Concentration.

Data Table (Concise)
Classification
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