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BioAssay: AID 720835

GSK_PKIS: Inhibition of Firefly Luciferase (Data from PubChem: AID 652016) [NIH NCATS]

A library of 367 protein kinase inhibitors, the GSK Published Kinase Inhibitor Set (PKIS), which has been annotated for protein kinase family activity and is available for public screening efforts, was assayed against the commonly used luciferase reporter enzymes from the firefly, Photinus pyralis (FLuc) and marine sea pansy, Renilla reniformis (RLuc). A total of 22 compounds (#6% of the library) more ..
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 Tested Compounds
 Tested Compounds
All(366)
 
 
Unspecified(366)
 
 
 Tested Substances
 Tested Substances
All(366)
 
 
Unspecified(366)
 
 
 Related BioAssays
 Related BioAssays
AID: 720835
Data Source: ChEMBL (933383)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Other
BioAssay Version:
Deposit Date: 2013-11-07
Modify Date: 2014-05-26

Data Table ( Complete ):           All
Target
Sequence: RecName: Full=Luciferin 4-monooxygenase; Short=Luciferase
Description ..   
Protein Family: Firefly luciferase of light emitting insects and 4-Coumarate-CoA Ligase (4CL)
Comment ..   

Related Protein 3D Structures     More BioActivity Data..
Tested Compounds:
Description:
Title: Profile of the GSK published protein kinase inhibitor set across ATP-dependent and-independent luciferases: implications for reporter-gene assays.

Abstract: A library of 367 protein kinase inhibitors, the GSK Published Kinase Inhibitor Set (PKIS), which has been annotated for protein kinase family activity and is available for public screening efforts, was assayed against the commonly used luciferase reporter enzymes from the firefly, Photinus pyralis (FLuc) and marine sea pansy, Renilla reniformis (RLuc). A total of 22 compounds (#6% of the library) were found to inhibit FLuc with 10 compounds showing potencies #1 microM. Only two compounds were found to inhibit RLuc, and these showed relatively weak potency values (#10 microM). An inhibitor series of the VEGFR2/TIE2 protein kinase family containing either an aryl oxazole or benzimidazole-urea core illustrate the different structure activity relationship profiles FLuc inhibitors can display for kinase inhibitor chemotypes. Several FLuc inhibitors were broadly active toward the tyrosine kinase and CDK families. These data should aid in interpreting the results derived from screens employing the GSK PKIS in cell-based assays using the FLuc reporter. The study also underscores the general need for strategies such as the use of orthogonal reporters to identify kinase or non-kinase mediated cellular responses.
Categorized Comment
Assay Type: Binding

Assay Data Source: GSK Published Kinase Inhibitor Set

Assay Test Type: In vitro

BAO: Assay Format: biochemical format

Target Type: Target is a single protein chain

Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1AC50*AC50 PubChem standard valueFloatμM
3BEIBinding Efficiency Index(nM)Float
2SEISurface Efficiency Index(nM)Float
4LELigand EfficiencyFloat
5LLELipophilic Ligand EfficiencyFloat
6AC50 activity commentAC50 activity commentString
7AC50 standard flagAC50 standard flagInteger
8AC50 qualifierAC50 qualifierString
9AC50 published valueAC50 published valueFloatμM
10AC50 standard valueAC50 standard valueFloatnM
11AC50 binding domainsAC50 binding domainsString

* Activity Concentration.

Data Table (Concise)
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