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BioAssay: AID 720552

qHTS assay for small molecule agonists of the p53 signaling pathway: Summary

p53, a tumor suppressor protein, is activated following cellular insult, including DNA damage and other cellular stresses. The activation of p53 regulates cell fate by inducing DNA repair, cell cycle arrest, apoptosis, or cellular senescence. The activation of p53, therefore, is a good indicator of DNA damage and other cellular stresses. The CellSensor p53RE-bla HCT-116 cell line (Invitrogen) more ..
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 Tested Compounds
 Tested Compounds
All(8119)
 
 
Active(529)
 
 
Inactive(6977)
 
 
Inconclusive(817)
 
 
 Tested Substances
 Tested Substances
All(10488)
 
 
Active(659)
 
 
Inactive(8888)
 
 
Inconclusive(941)
 
 
AID: 720552
Data Source: Tox21 (P53823)
BioAssay Type: Summary, Candidate Probes/Leads with Supporting Evidence
Depositor Category: Other
BioAssay Version:
Deposit Date: 2013-07-29
Modify Date: 2014-08-20

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 529
Related Experiments
AIDNameTypeComment
651631qHTS assay for small molecule agonists of the p53 signaling pathwayConfirmatorydepositor-specified cross reference: P53 activation screen
651633qHTS assay for small molecule agonists of the p53 signaling pathway - cell viabilityConfirmatorydepositor-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:

p53, a tumor suppressor protein, is activated following cellular insult, including DNA damage and other cellular stresses. The activation of p53 regulates cell fate by inducing DNA repair, cell cycle arrest, apoptosis, or cellular senescence. The activation of p53, therefore, is a good indicator of DNA damage and other cellular stresses. The CellSensor p53RE-bla HCT-116 cell line (Invitrogen) contains a stably integrated beta-lactamase (BLA) reporter gene under control of the p53 response elements. The activation of the reporter gene under culture conditions can be detected by fluorescence intensity. This cell line was used to screen the Tox21 compound library in a 1536-well plate format and to identify agonists that activate the p53 signaling pathway. The cytotoxicity of the Tox21 compound library against the p53 RE-bla HCT-116 cell line was tested in parallel by measuring the intra cellular ATP content in the same wells.
Protocol
Please refer to other AIDs, 651631 and 651633, 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 P53 assay (AID 651631) and cell viability counter screen (AID 651633). 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 P53 readout and the cell viability counter screen.String
2Ratio ActivityType of compound activity in the ratio readout of the P53 screen.String
3Ratio Potency (uM)*The concentration of sample yielding half-maximal activation in the ratio readout of the P53 screen.FloatμM
4Ratio Efficacy (%)Percent activation in the ratio readout of the P53 screen.Float%
5530 nm ActivityType of compound activity in the 530 nm readout of the P53 screen.String
6530 nm Potency (uM)he concentration of sample yielding half-maximal activation in the 530 nm readout of the P53 screen.FloatμM
7530 nm Efficacy (%)Type of compound activity in the 530 nm readout of the P53 screen.Float%
8460 nm ActivityType of compound activity in the 460 nm readout of the P53 screen.String
9460 nm Potency (uM)he concentration of sample yielding half-maximal activation in the 460 nm readout of the P53 screen.FloatμM
10460 nm Efficacy (%)Type of compound activity in the 460 nm readout of the P53 screen.Float%
11Viability ActivityType of compound activity in the cell viability counter screen.String
12Viability Potency (uM)The concentration of sample yielding half-maximal inhibition of cell viability.FloatμM
13Viability Efficacy (%)Percent inhibition of cell viability.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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