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BioAssay: AID 743067

qHTS assay to identify small molecule antagonists of the thyroid receptor (TR) signaling pathway: Summary

Thyroid receptor (TR), a nuclear hormone receptor, plays an important role in development, proliferation, differentiation, metabolism, brain function, and cardiovascular system. TR-interacting compounds have been shown to disrupt thyroid homeostasis. To profile the Tox21 10K compound library in TR signaling, a cell-based GH3-TRE-Luc assay (GH3.TRE-Luc cell line, developed by the laboratory of Dr. more ..
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 Tested Compounds
 Tested Compounds
All(8119)
 
 
Active(378)
 
 
Inactive(5643)
 
 
Inconclusive(2499)
 
 
 Tested Substances
 Tested Substances
All(10486)
 
 
Active(426)
 
 
Inactive(7088)
 
 
Inconclusive(2972)
 
 
AID: 743067
Data Source: Tox21 (TRN190)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: Other
BioAssay Version:
Deposit Date: 2013-11-14
Modify Date: 2014-08-20

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 378
Related Experiments
AIDNameTypeComment
743064qHTS assay to identify small molecule antagonists of the thyroid receptor (TR) signaling pathway - cell viability counter screenConfirmatorydepositor-specified cross reference: Cell viability counter screen
743065qHTS assay to identify small molecule antagonists of the thyroid receptor (TR) signaling pathwayConfirmatorydepositor-specified cross reference: TR antagonist mode 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:

Thyroid receptor (TR), a nuclear hormone receptor, plays an important role in development, proliferation, differentiation, metabolism, brain function, and cardiovascular system. TR-interacting compounds have been shown to disrupt thyroid homeostasis. To profile the Tox21 10K compound library in TR signaling, a cell-based GH3-TRE-Luc assay (GH3.TRE-Luc cell line, developed by the laboratory of Dr. Albertinka J. Murk, Wageningen University) was used to measure the inhibition of TR. GH3 (rat pituitary tumor) cells stably expressing a TR activity sensor consisting of two TR response elements and a luciferase reporter gene. The cytotoxicity of the Tox21 compound library against the GH3.TRE-Luc 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 743065 and 743064 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 TR antagonist mode assay (AID 743065) and cell viability counter screen (AID 743064). 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 TR antagonist mode readout and the cell viability counter screen.String
2TR ActivityType of compound activity in the TR antagonist mode screen.String
3TR Potency (uM)*The concentration of sample yielding half-maximal inhibition of TR.FloatμM
4TR Efficacy (%)Percent inhibition of TR.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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