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BioAssay: AID 743063

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

Androgen receptor (AR), a nuclear hormone receptor, plays a critical role in AR-dependent prostate cancer and other androgen related diseases. Endocrine disrupting chemicals (EDCs) and their interactions with steroid hormone receptors like AR may cause disruption of normal endocrine function as well as interfere with metabolic homeostasis, reproduction, developmental and behavioral functions. To more ..
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 Tested Compounds
 Tested Compounds
All(8119)
 
 
Active(549)
 
 
Inactive(6260)
 
 
Inconclusive(1748)
 
 
 Tested Substances
 Tested Substances
All(10486)
 
 
Active(670)
 
 
Inactive(7770)
 
 
Inconclusive(2046)
 
 
AID: 743063
Data Source: Tox21 (ARN170)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: Other
BioAssay Version:
Deposit Date: 2013-11-13
Modify Date: 2014-08-20

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 549
Related Experiments
AIDNameTypeComment
743033qHTS assay to identify small molecule antagonists of the androgen receptor (AR) signaling pathway - cell viability counter screenConfirmatorydepositor-specified cross reference: Cell viability counter screen
743035qHTS assay to identify small molecule antagonists of the androgen receptor (AR) signaling pathwayConfirmatorydepositor-specified cross reference: AR 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:

Androgen receptor (AR), a nuclear hormone receptor, plays a critical role in AR-dependent prostate cancer and other androgen related diseases. Endocrine disrupting chemicals (EDCs) and their interactions with steroid hormone receptors like AR may cause disruption of normal endocrine function as well as interfere with metabolic homeostasis, reproduction, developmental and behavioral functions. To identify the compounds that inhibit AR signaling, GeneBLAzer AR-UAS-bla-GripTite cell line (Invitrogen, Carlsbad, CA, USA) containing a beta-lactamase reporter gene under 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 AR-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, 743035 and 743033, 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 AR antagonist mode assay (AID 743035) and cell viability counter screen (AID 743033). 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 AR antagonist mode screen and the cell viability counter screens.String
2Ratio ActivityType of compound activity in the ratio readout of the AR antagonist mode screen.String
3Ratio Potency (uM)*The concentration of sample yielding half-maximal inhibition in the ratio readout of the AR antagonist mode screen.FloatμM
4Ratio Efficacy (%)Percent inhibition in the ratio readout of the AR antagonist mode screen.Float%
5530 nm ActivityType of compound activity in the 530 nm readout of the AR antagonist mode screen.String
6530 nm Potency (uM)The concentration of sample yielding half-maximal inhibition in the 530 nm readout of the AR antagonist mode screen.FloatμM
7530 nm Efficacy (%)Percent inhibition in the 530 nm readout of the AR antagonist mode screen.Float%
8460 nm ActivityType of compound activity in the 460 nm readout of the AR antagonist mode screen.String
9460 nm Potency (uM)The concentration of sample yielding half-maximal inhibition in the 460 nm readout of the AR antagonist mode screen.FloatμM
10460 nm Efficacy (%)Percent inhibition in the 460 nm readout of the AR 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)
Data Table ( Complete ):     View Active Data    View All Data
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