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BioAssay: AID 743091

qHTS assay to identify small molecule antagonists of the estrogen receptor alpha (ER-alpha) signaling pathway using the BG1 cell line: Summary

Estrogen receptor (ER), a nuclear hormone receptor, plays an important role in development, metabolic homeostasis and reproduction. Endocrine disrupting chemicals (EDCs) and their interactions with steroid hormone receptors like ER causes disruption of normal endocrine function. Therefore, it is important to understand the effect of environmental chemicals on the ER signaling pathway. To identify more ..
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 Tested Compounds
 Tested Compounds
All(8119)
 
 
Active(398)
 
 
Inactive(6560)
 
 
Inconclusive(1432)
 
 
 Tested Substances
 Tested Substances
All(10486)
 
 
Active(477)
 
 
Inactive(8297)
 
 
Inconclusive(1712)
 
 
AID: 743091
Data Source: Tox21 (BG1N735)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: Other
BioAssay Version:
Deposit Date: 2013-11-20
Modify Date: 2014-08-21

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 398
Related Experiments
AIDNameTypeComment
743080qHTS assay to identify small molecule antagonists of the estrogen receptor alpha (ER-alpha) signaling pathway using the BG1 cell lineConfirmatorydepositor-specified cross reference: ER antagonist mode screen
743081qHTS assay to identify small molecule antagonists of the estrogen receptor alpha (ER-alpha) signaling pathway using the BG1 cell line - 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:

Estrogen receptor (ER), a nuclear hormone receptor, plays an important role in development, metabolic homeostasis and reproduction. Endocrine disrupting chemicals (EDCs) and their interactions with steroid hormone receptors like ER causes disruption of normal endocrine function. Therefore, it is important to understand the effect of environmental chemicals on the ER signaling pathway. To identify ER antagonists, BG1-Luc-4E2 cell line (provided by Dr. Michael Denison from University of California) has been used to screen the Tox21 10K compound library. BG1Luc4E2 cell line endogenously expresses full-length ER-alpha and is stably transfected with a plasmid containing four estrogen responsive elements (ERE) upstream of a luciferase reporter gene. The cytotoxicity of the Tox21 compound library against the BG1-Luc-4E2 cell line was tested in parallel by measuring the cell viability using CellTiter-Fluor assay (Promega, Madison, WI) in the same wells.
Protocol
Please refer to other AIDs, 743080 and 743081, 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 ER antagonist mode assay (AID 743080) and cell viability counter screen (AID 743081). 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 ER antagonist mode readout and the cell viability counter screen.String
2ER ActivityType of compound activity in the ER antagonist mode screen.String
3ER Potency (uM)*The concentration of sample yielding half-maximal inhibition of ER.FloatμM
4ER Efficacy (%)Percent inhibition of ER.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
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