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BioAssay: AID 743078

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

Estrogen receptor (ER), a nuclear hormone receptor, plays an important role in development, metabolic homeostasis and reproduction. Two subtypes of ER, ER-alpha and ER-beta have similar expression patterns with some uniqueness in both types. Endocrine disrupting chemicals (EDCs) and their interactions with steroid hormone receptors like ER causes disruption of normal endocrine function. To more ..
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 Tested Compounds
 Tested Compounds
All(8121)
 
 
Active(389)
 
 
Inactive(6414)
 
 
Inconclusive(1766)
 
 
 Tested Substances
 Tested Substances
All(10496)
 
 
Active(435)
 
 
Inactive(7998)
 
 
Inconclusive(2063)
 
 
AID: 743078
Data Source: Tox21 (ERN743)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: Other
Deposit Date: 2013-11-18

Data Table ( Complete ):           Active    All
Target
BioActive Compounds: 389
Depositor Specified Assays
AIDNameTypeComment
743069qHTS assay to identify small molecule antagonists of the estrogen receptor alpha (ER-alpha) signaling pathwayconfirmatoryER-alpha antagonist mode screen
743074qHTS assay to identify small molecule antagonists of the estrogen receptor alpha (ER-alpha) signaling pathway - cell viability counter screenconfirmatoryCell 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. Two subtypes of ER, ER-alpha and ER-beta have similar expression patterns with some uniqueness in both types. Endocrine disrupting chemicals (EDCs) and their interactions with steroid hormone receptors like ER causes disruption of normal endocrine function. To identify the compounds that inhibit ER-alpha signaling, an ER-alpha-UAS-bla GripTiteTM cell line (Invitrogen, Carlsbad, CA, USA) containing a beta-lactamase reporter gene under the control of an Upstream Activator Sequence (UAS) stably integrated into HEK293 cells was used to screen the Tox21 10K compound library. The cytotoxicity of the Tox21 compound library against the ERalpha-bla cell line was tested in parallel by measuring the cell viability using CellTiter-Glo assay in the same wells.
Protocol
Please refer to other AIDs, 743069 and 743074, 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-alpha antagonist mode assay (AID 743069) and cell viability counter screen (AID 743074). 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
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1Activity SummaryType of compound activity based on both the ER-alpha antagonist mode screen and the cell viability counter screens.String
2Ratio ActivityType of compound activity in the ratio readout of the ER-alpha antagonist mode screen.String
3Ratio Potency (uM)*The concentration of sample yielding half-maximal inhibition in the ratio readout of the ER-alpha antagonist mode screen.FloatμM
4Ratio Efficacy (%)Percent inhibition in the ratio readout of the ER-alpha antagonist mode screen.Float%
5530 nm ActivityType of compound activity in the 530 nm readout of the ER-alpha antagonist mode screen.String
6530 nm Potency (uM)The concentration of sample yielding half-maximal inhibition in the 530 nm readout of the ER-alpha antagonist mode screen.FloatμM
7530 nm Efficacy (%)Percent inhibition in the 530 nm readout of the ER-alpha antagonist mode screen.Float%
8460 nm ActivityType of compound activity in the 460 nm readout of the ER-alpha antagonist mode screen.String
9460 nm Potency (uM)The concentration of sample yielding half-maximal inhibition in the 460 nm readout of the ER-alpha antagonist mode screen.FloatμM
10460 nm Efficacy (%)Percent inhibition in the 460 nm readout of the ER-alpha antagonist mode screen.Float%
11Viability ActivityType of compound activity in the cell viability counter screens.String
12Viability Potency (uM)The concentration of sample yielding half-maximal inhibition in the cell viability counter screen.FloatμM
13Viability Efficacy (%)Percent inhibition in the cell viability counter screen.Float%
14Sample SourceWhere sample was obtained.String

* Activity Concentration.

Data Table (Concise)
Classification
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