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BioAssay: AID 743122

qHTS assay to identify small molecule that activate the aryl hydrocarbon receptor (AhR) signaling pathway: Summary

The Aryl hydrocarbon Receptor (AhR), a member of the family of basic helix-loop-helix transcription factors, is crucial to adaptive responses to environmental changes. AhR mediates cellular responses to environmental pollutants such as aromatic hydrocarbons through induction of phase I and II enzymes but also interacts with other nuclear receptor signaling pathways ..more
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 Tested Compounds
 Tested Compounds
All(8110)
 
 
Active(875)
 
 
Inactive(6407)
 
 
Inconclusive(1357)
 
 
 Tested Substances
 Tested Substances
All(10486)
 
 
Active(1063)
 
 
Inactive(7945)
 
 
Inconclusive(1478)
 
 
AID: 743122
Data Source: Tox21 (AHR641)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: Other
BioAssay Version:
Deposit Date: 2013-11-25
Modify Date: 2014-08-21

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 875
Related Experiments
AIDNameTypeComment
743085qHTS assay to identify small molecule that activate the aryl hydrocarbon receptor (AhR) signaling pathwayConfirmatorydepositor-specified cross reference: AhR agonist mode screen
743086qHTS assay to identify small molecule that activate the aryl hydrocarbon receptor (AhR) signaling pathway - cell viability counter screenConfirmatorydepositor-specified cross reference: Cell viability counter screen
Description:
U.S. Tox21 Program

National Center for Advancing Translational Sciences [NCATS]
NIH Chemical Genomics Center [NCGC]
U.S. Environmental Protection Agency [EPA]
National Institutes of Environmental Health Sciences [NIEHS]
National Toxicology Program [NTP]
U.S. Food and Drug Administration [FDA]

Tox21 Assay Overview:

The Aryl hydrocarbon Receptor (AhR), a member of the family of basic helix-loop-helix transcription factors, is crucial to adaptive responses to environmental changes. AhR mediates cellular responses to environmental pollutants such as aromatic hydrocarbons through induction of phase I and II enzymes but also interacts with other nuclear receptor signaling pathways

A cell based HepG2-AhR-luc assay (HG2L7.5c1 cell line, developed by Dr. Michael S. Denison, University of California at Davis) was used to assess the activation of AhR. HepG2 (human hepatocellular carcinoma) cells were stably transfected with an Ah receptor-responsive firefly luciferase reporter gene plasmid containing 20 dioxin responsive elements and luciferase reporter gene. Increased luciferase activity can be used to identify the compounds that induce AhR activation. The cytotoxicity of the compounds screened against the HepG2-AhR-luc cell line was tested in parallel by measuring the cell viability using CellTiter-Fluor assay in the same wells.
Protocol
Please refer to other AIDs, 743085 and 743086, for detailed assay protocols.
Comment
This summary is written for the purposes of summarizing the compound activities from the project combining the results from both the AhR agonist mode assay (AID 743085) and cell viability counter screen (AID 743086). For all inactive compounds, PUBCHEM_ACTIVITY_SCORE is 0. Active compounds have PUBCHEM_ACTIVITY_SCORE between 40 and 100. Potency and efficacy were used for determining relative score. Inconclusive compounds have PUBCHEM_ACTIVITY_SCORE between 5 and 30 determined by phenotype.
Disclaimer:
Although all reasonable efforts have been made to ensure the accuracy and reliability of the data, caution should be exercised when interpreting the results as artifacts are possible from nonspecific effects such as assay signal interference. The curve fitting and activity calls presented here are based on the NCATS analysis methods. Alternative analysis methods and interpretations of the data are available at EPA (http://actor.epa.gov) and NTP (http://tools.niehs.nih.gov/cebs3/ui/).
Result Definitions
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TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1Activity SummaryType of compound activity based on both the AhR agonist mode readout and the cell viability counter screen.String
2AhR ActivityType of compound activity in the AhR agonist mode screen.String
3AhR Potency (uM)*The concentration of sample yielding half-maximal activation of AhR.FloatμM
4AhR Efficacy (%)Percent activation of AhR.Float%
5Viability ActivityType of compound activity in the cell viability counter screen.String
6Viability Potency (uM)The concentration of sample yielding half-maximal inhibition of cell viability.FloatμM
7Viability Efficacy (%)Percent inhibition of cell viability.Float%
8Sample SourceWhere sample was obtained.String

* Activity Concentration.

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