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BioAssay: AID 743139

qHTS assay to identify aromatase inhibitors: Summary

Endocrine disrupting chemicals (EDCs) interfere with the biosynthesis and normal functions of steroid hormones including estrogen and androgen in the body. Aromatase catalyzes the conversion of androgen to estrogen and plays a key role in maintaining the androgen and estrogen balance in many of the EDC-sensitive organs. MCF-7 aro ERE cell line (provided by Dr. Shiuan Chen at Beckman Research more ..
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 Tested Compounds
 Tested Compounds
All(8121)
 
 
Active(327)
 
 
Inactive(6128)
 
 
Inconclusive(2100)
 
 
 Tested Substances
 Tested Substances
All(10496)
 
 
Active(381)
 
 
Inactive(7563)
 
 
Inconclusive(2552)
 
 
 Related BioAssays
 Related BioAssays
AID: 743139
Data Source: Tox21 (AROS634)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: Other
Deposit Date: 2013-11-26

Data Table ( Complete ):           Active    All
Target
BioActive Compounds: 327
Depositor Specified Assays
AIDNameTypeComment
743083qHTS assay to identify aromatase inhibitorsconfirmatoryAromatase antagonist mode screen
743084qHTS assay to identify aromatase inhibitors - 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:

Endocrine disrupting chemicals (EDCs) interfere with the biosynthesis and normal functions of steroid hormones including estrogen and androgen in the body. Aromatase catalyzes the conversion of androgen to estrogen and plays a key role in maintaining the androgen and estrogen balance in many of the EDC-sensitive organs. MCF-7 aro ERE cell line (provided by Dr. Shiuan Chen at Beckman Research Institute of the City of Hope) was used to screen the Tox21 10K compound library collection for identification of aromatase inhibitors. MCF-7 aro ERE is human breast carcinoma cell line that was stably transfected with a promoter plasmid, pGL3-Luc, containing three repeats of estrogen responsive element (ERE). The cytotoxicity of the Tox21 compound library against the MCF-7 aro ERE 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, 743083 and 743084, 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 aromatase antagonist mode assay (AID 743083) and cell viability counter screen (AID 743084). 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 aromatase antagonist mode readout and the cell viability counter screen.String
2Antagonist ActivityType of compound activity in the aromatase antagonist mode screen.String
3Antagonist Potency (uM)The concentration of sample yielding half-maximal inhibition of aromatase.FloatμM
4Antagonist Efficacy (%)Percent inhibition of aromatase.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

Data Table (Concise)
Classification
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