Bookmark and Share
BioAssay: AID 651758

qHTS assay to identify small molecules that stimulate interleukin-8 (IL-8) secretion

Interleukin-8 is a 8 kDa chemokine produced by macrophages and other cells like epithelial cells that is often associated with inflammation. Interleukin-8 secretion is a key parameter in localized inflammation. There is a growing concern for some of environmental chemicals which may contribute the increasing the incidence of inflammation. A homogeneous IL-8 assay using Time Resolved fluorescence (HTRF) technology based on Time Resolved Fluorescent Resonance Energy Transfer (TR-FRET) allows to measure IL-8 secreted from the cells in a 1536-well plate format. ..more
_
   
 Tested Compounds
 Tested Compounds
All(1335)
 
 
Active(38)
 
 
Inactive(390)
 
 
Inconclusive(938)
 
 
 Tested Substances
 Tested Substances
All(1408)
 
 
Active(41)
 
 
Inactive(396)
 
 
Inconclusive(971)
 
 
 Related BioAssays
 Related BioAssays
AID: 651758
Data Source: NCGC (IL8424)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: Other
Deposit Date: 2012-11-07

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 38
Description:
National Center for Advancing Translational Sciences [NCATS]
NIH Chemical Genomics Center [NCGC]
National Institutes of Environmental Health Sciences [NIEHS]
National Toxicology Program [NTP]

Assay Overview:

Interleukin-8 is a 8 kDa chemokine produced by macrophages and other cells like epithelial cells that is often associated with inflammation. Interleukin-8 secretion is a key parameter in localized inflammation. There is a growing concern for some of environmental chemicals which may contribute the increasing the incidence of inflammation. A homogeneous IL-8 assay using Time Resolved fluorescence (HTRF) technology based on Time Resolved Fluorescent Resonance Energy Transfer (TR-FRET) allows to measure IL-8 secreted from the cells in a 1536-well plate format.
Protocol
Assay protocol summary:
THP-1 cells were dispensed at 2000 cells/5ul/well in 1536-well white solid plates. After addition of 23 nl of compound, positive controls and DMSO only, the assay plates were incubated at 37 C for 16 hrs, followed by addition of 5 uL of mixture of cryptate labeled and XL665 labeled anti-IL-8 antibodies. After the assay plates were incubated at room temperature for 1-3 hrs, the plates were measured by an EnVision plate reader.
Comment
Compound Ranking:
1. Compounds are first classified as having full titration curves, partial modulation, partial curve (weaker actives), single point activity (at highest concentration only), or inactive. See data field "Curve Description". For this assay, apparent activators are ranked higher than compounds that showed apparent inhibition.
2. For all inactive compounds, PUBCHEM_ACTIVITY_SCORE is 0. For all active compounds, a score range was given for each curve class type given above. Active compounds have PUBCHEM_ACTIVITY_SCORE between 40 and 100. Inconclusive compounds have PUBCHEM_ACTIVITY_SCORE between 1 and 39. Fit_LogAC50 was used for determining relative score and was scaled to each curve class' score range.
Categorized Comment - additional comments and annotations
From ChEMBL:
Assay Type: Functional
Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1PhenotypeIndicates type of activity observed: inhibitor, activator, fluorescent, cytotoxic, inactive, or inconclusive.String
2Potency*Concentration at which compound exhibits half-maximal efficacy, AC50. Extrapolated AC50s also include the highest efficacy observed and the concentration of compound at which it was observed.FloatμM
3EfficacyMaximal efficacy of compound, reported as a percentage of control. These values are estimated based on fits of the Hill equation to the dose-response curves.Float%
4Analysis CommentAnnotation/notes on a particular compound's data or its analysis.String
5W665-Activity_ScoreActivity score.Integer
6W665-Curve_DescriptionA description of dose-response curve quality. A complete curve has two observed asymptotes; a partial curve may not have attained its second asymptote at the highest concentration tested. High efficacy curves exhibit efficacy greater than 80% of control. Partial efficacies are statistically significant, but below 80% of control.String
7W665-Fit_LogAC50The logarithm of the AC50 from a fit of the data to the Hill equation (calculated based on Molar Units).Float
8W665-Fit_HillSlopeThe Hill slope from a fit of the data to the Hill equation.Float
9W665-Fit_R2R^2 fit value of the curve. Closer to 1.0 equates to better Hill equation fit.Float
10W665-Fit_InfiniteActivityThe asymptotic efficacy from a fit of the data to the Hill equation.Float%
11W665-Fit_ZeroActivityEfficacy at zero concentration of compound from a fit of the data to the Hill equation.Float%
12W665-Fit_CurveClassNumerical encoding of curve description for the fitted Hill equation.Float
13W665-Excluded_PointsWhich dose-response titration points were excluded from analysis based on outlier analysis. Each number represents whether a titration point was (1) or was not (0) excluded, for the titration series going from smallest to highest compound concentrations.String
14W665-Max_ResponseMaximum activity observed for compound (usually at highest concentration tested).Float%
15W665-Activity at 0.0005899000 uM (0.0005899μM**)% Activity at given concentration.Float%
16W665-Activity at 0.00295 uM (0.002949μM**)% Activity at given concentration.Float%
17W665-Activity at 0.015 uM (0.01475μM**)% Activity at given concentration.Float%
18W665-Activity at 0.033 uM (0.03297μM**)% Activity at given concentration.Float%
19W665-Activity at 0.074 uM (0.07373μM**)% Activity at given concentration.Float%
20W665-Activity at 0.165 uM (0.1649μM**)% Activity at given concentration.Float%
21W665-Activity at 0.369 uM (0.3687μM**)% Activity at given concentration.Float%
22W665-Activity at 0.824 uM (0.8244μM**)% Activity at given concentration.Float%
23W665-Activity at 1.843 uM (1.843μM**)% Activity at given concentration.Float%
24W665-Activity at 4.122 uM (4.122μM**)% Activity at given concentration.Float%
25W665-Activity at 9.217 uM (9.217μM**)% Activity at given concentration.Float%
26W665-Activity at 20.61 uM (20.61μM**)% Activity at given concentration.Float%
27W665-Activity at 46.08 uM (46.08μM**)% Activity at given concentration.Float%
28W665-Activity at 92.17 uM (92.17μM**)% Activity at given concentration.Float%
29Ratio-Activity_ScoreActivity score.Integer
30Ratio-Curve_DescriptionA description of dose-response curve quality. A complete curve has two observed asymptotes; a partial curve may not have attained its second asymptote at the highest concentration tested. High efficacy curves exhibit efficacy greater than 80% of control. Partial efficacies are statistically significant, but below 80% of control.String
31Ratio-Fit_LogAC50The logarithm of the AC50 from a fit of the data to the Hill equation (calculated based on Molar Units).Float
32Ratio-Fit_HillSlopeThe Hill slope from a fit of the data to the Hill equation.Float
33Ratio-Fit_R2R^2 fit value of the curve. Closer to 1.0 equates to better Hill equation fit.Float
34Ratio-Fit_InfiniteActivityThe asymptotic efficacy from a fit of the data to the Hill equation.Float%
35Ratio-Fit_ZeroActivityEfficacy at zero concentration of compound from a fit of the data to the Hill equation.Float%
36Ratio-Fit_CurveClassNumerical encoding of curve description for the fitted Hill equation.Float
37Ratio-Excluded_PointsWhich dose-response titration points were excluded from analysis based on outlier analysis. Each number represents whether a titration point was (1) or was not (0) excluded, for the titration series going from smallest to highest compound concentrations.String
38Ratio-Max_ResponseMaximum activity observed for compound (usually at highest concentration tested).Float%
39Ratio-Activity at 0.0005899000 uM (0.0005899μM**)% Activity at given concentration.Float%
40Ratio-Activity at 0.00295 uM (0.002949μM**)% Activity at given concentration.Float%
41Ratio-Activity at 0.015 uM (0.01475μM**)% Activity at given concentration.Float%
42Ratio-Activity at 0.033 uM (0.03297μM**)% Activity at given concentration.Float%
43Ratio-Activity at 0.074 uM (0.07373μM**)% Activity at given concentration.Float%
44Ratio-Activity at 0.165 uM (0.1649μM**)% Activity at given concentration.Float%
45Ratio-Activity at 0.369 uM (0.3687μM**)% Activity at given concentration.Float%
46Ratio-Activity at 0.824 uM (0.8244μM**)% Activity at given concentration.Float%
47Ratio-Activity at 1.843 uM (1.843μM**)% Activity at given concentration.Float%
48Ratio-Activity at 4.122 uM (4.122μM**)% Activity at given concentration.Float%
49Ratio-Activity at 9.217 uM (9.217μM**)% Activity at given concentration.Float%
50Ratio-Activity at 20.61 uM (20.61μM**)% Activity at given concentration.Float%
51Ratio-Activity at 46.08 uM (46.08μM**)% Activity at given concentration.Float%
52Ratio-Activity at 92.17 uM (92.17μM**)% Activity at given concentration.Float%
53W615-Activity_ScoreActivity score.Integer
54W615-Curve_DescriptionA description of dose-response curve quality. A complete curve has two observed asymptotes; a partial curve may not have attained its second asymptote at the highest concentration tested. High efficacy curves exhibit efficacy greater than 80% of control. Partial efficacies are statistically significant, but below 80% of control.String
55W615-Fit_LogAC50The logarithm of the AC50 from a fit of the data to the Hill equation (calculated based on Molar Units).Float
56W615-Fit_HillSlopeThe Hill slope from a fit of the data to the Hill equation.Float
57W615-Fit_R2R^2 fit value of the curve. Closer to 1.0 equates to better Hill equation fit.Float
58W615-Fit_InfiniteActivityThe asymptotic efficacy from a fit of the data to the Hill equation.Float%
59W615-Fit_ZeroActivityEfficacy at zero concentration of compound from a fit of the data to the Hill equation.Float%
60W615-Fit_CurveClassNumerical encoding of curve description for the fitted Hill equation.Float
61W615-Excluded_PointsWhich dose-response titration points were excluded from analysis based on outlier analysis. Each number represents whether a titration point was (1) or was not (0) excluded, for the titration series going from smallest to highest compound concentrations.String
62W615-Max_ResponseMaximum activity observed for compound (usually at highest concentration tested).Float%
63W615-Activity at 0.0005899000 uM (0.0005899μM**)% Activity at given concentration.Float%
64W615-Activity at 0.00295 uM (0.002949μM**)% Activity at given concentration.Float%
65W615-Activity at 0.015 uM (0.01475μM**)% Activity at given concentration.Float%
66W615-Activity at 0.033 uM (0.03297μM**)% Activity at given concentration.Float%
67W615-Activity at 0.074 uM (0.07373μM**)% Activity at given concentration.Float%
68W615-Activity at 0.165 uM (0.1649μM**)% Activity at given concentration.Float%
69W615-Activity at 0.369 uM (0.3687μM**)% Activity at given concentration.Float%
70W615-Activity at 0.824 uM (0.8244μM**)% Activity at given concentration.Float%
71W615-Activity at 1.843 uM (1.843μM**)% Activity at given concentration.Float%
72W615-Activity at 4.122 uM (4.122μM**)% Activity at given concentration.Float%
73W615-Activity at 9.217 uM (9.217μM**)% Activity at given concentration.Float%
74W615-Activity at 20.61 uM (20.61μM**)% Activity at given concentration.Float%
75W615-Activity at 46.08 uM (46.08μM**)% Activity at given concentration.Float%
76W615-Activity at 92.17 uM (92.17μM**)% Activity at given concentration.Float%
77Compound QCNCGC designation for data stage: 'qHTS', 'qHTS Verification', 'Secondary Profiling'String

* Activity Concentration. ** Test Concentration.

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