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BioAssay: AID 720725

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

The Glucocorticoid receptor (GR) is one of the members of the nuclear receptor family of ligand-dependent transcription factors. GR plays a critical role in carbohydrate, protein and lipid metabolisms and programmed cell death. CellSensor GR-bla HeLa cell line (Invitrogen) contains a beta-lactamase reporter gene under the control of the glucocorticoid response element stably integrated into HeLa more ..
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 Tested Compounds
 Tested Compounds
All(8119)
 
 
Active(384)
 
 
Inactive(6193)
 
 
Inconclusive(1908)
 
 
 Tested Substances
 Tested Substances
All(10486)
 
 
Active(460)
 
 
Inactive(7744)
 
 
Inconclusive(2282)
 
 
AID: 720725
Data Source: Tox21 (GRN811)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: Other
BioAssay Version:
Deposit Date: 2013-11-01
Modify Date: 2014-08-20

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 384
Related Experiments
AIDNameTypeComment
720692qHTS assay to identify small molecule antagonists of the glucocorticoid receptor (GR) signaling pathwayConfirmatorydepositor-specified cross reference: GR antagonist mode screen
720693qHTS assay to identify small molecule antagonists of the glucocorticoid receptor (GR) 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 Glucocorticoid receptor (GR) is one of the members of the nuclear receptor family of ligand-dependent transcription factors. GR plays a critical role in carbohydrate, protein and lipid metabolisms and programmed cell death. CellSensor GR-bla HeLa cell line (Invitrogen) contains a beta-lactamase reporter gene under the control of the glucocorticoid response element stably integrated into HeLa cells, a cervical cancer cell line that expresses glucocorticoid receptor. The activation of the reporter gene under culture conditions can be detected by fluorescence intensity. This cell line has been used to screen the Tox21 10K compound library and to identify the compounds that inhibit the GR signaling. The cytotoxicity of the Tox21 10K compound library against the GR-bla HeLa 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, 720692 and 720693, 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 GR antagonist mode assay (AID 720692) and cell viability counter screen (AID 720693). 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 GR antagonist mode screen and the cell viability counter screens.String
2Ratio ActivityType of compound activity in the ratio readout of the GR antagonist mode screen.String
3Ratio Potency (uM)The concentration of sample yielding half-maximal inhibition in the ratio readout of the GR antagonist mode screen.FloatμM
4Ratio Efficacy (%)Percent inhibition in the ratio readout of the GR antagonist mode screen.Float%
5530 nm ActivityType of compound activity in the 530 nm readout of the GR antagonist mode screen.String
6530 nm Potency (uM)The concentration of sample yielding half-maximal inhibition in the 530 nm readout of the GR antagonist mode screen.FloatμM
7530 nm Efficacy (%)Percent inhibition in the 530 nm readout of the GR antagonist mode screen.Float%
8460 nm ActivityType of compound activity in the 460 nm readout of the GR antagonist mode screen.String
9460 nm Potency (uM)The concentration of sample yielding half-maximal inhibition in the 460 nm readout of the GR antagonist mode screen.FloatμM
10460 nm Efficacy (%)Percent inhibition in the 460 nm readout of the GR 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

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