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BioAssay: AID 624167

Dose Response confirmation of uHTS small molecule Peg3 Promoter Inhibitor hits in a screening assay

Cancer is a progressive disease culminating in the acquisition of metastatic potential by a subset of evolving tumor cells. Although extensively investigated, the precise molecular events underlying tumor development and cancer progression remain unclear. Progression elevated gene-3 (PEG-3), originally identified in rodents, displays elevated expression as cancers become more aggressive. The more ..
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 Tested Compounds
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Active(359)
 
 
Inactive(665)
 
 
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Active(359)
 
 
Inactive(665)
 
 
AID: 624167
Data Source: Burnham Center for Chemical Genomics (SBCCG-A846-PEG3-DMSO-Panel-Assay)
BioAssay Type: Panel, Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2012-05-22

Data Table ( Complete ):           View Active Data    View All Data
Target
BioActive Compounds: 359
Related Experiments
AIDNameTypeComment
588405HTS Assay for Peg3 Promoter InhibitorsScreeningdepositor-specified cross reference
588409Summary Assay for small molecule Peg3 Promoter InhibitorsSummarydepositor-specified cross reference
602417Single concentration confirmation of uHTS hits for Peg3 Promoter Inhibitors via a luciferase reporter assayScreeningsame project related to Summary assay
651549Dose Response confirmation of uHTS small molecule Peg3 Promoter Inhibitor hits in screening - selectivity counter screen assays - Set 2Confirmatorysame project related to Summary assay
651551SAR analysis of small molecule Peg3 Promoter Inhibitors hits in screening - selectivity counter screen assaysConfirmatorysame project related to Summary assay
Description:
Data Source: Sanford-Burnham Center for Chemical Genomics (SBCCG)
Source Affiliation: Sanford-Burnham Medical Research Institute (SBIMR, San Diego, CA)
Network: NIH Molecular Libraries Probe Production Centers Network (MLPCN)
Grant Number: 2R01 GM068385-06
Assay Provider: Paul B. Fisher, M.Ph., Ph.D., Virginia Commonwealth University

Cancer is a progressive disease culminating in the acquisition of metastatic potential by a subset of evolving tumor cells. Although extensively investigated, the precise molecular events underlying tumor development and cancer progression remain unclear. Progression elevated gene-3 (PEG-3), originally identified in rodents, displays elevated expression as cancers become more aggressive. The minimal promoter region controlling PEG-3 expression, PEG-Prom, has been isolated and shown to display elevated expression in a wide range of both human and rodent tumors, with minimal expression in normal cells. The PEG-Prom is transcriptionally activated following transformation by diverse acting oncogenes or as a consequence of unidentified genetic factors mediating cellular transformation. We have determined the mechanism for this selectivity and it involves transcription (gene regulatory) factors, AP-1 and PEA-3, which are expressed at elevated levels in virtually all rodent and human cancers. Moreover, in cases of cancer reversion or blocking expression of specific transforming oncogenes, PEG-Prom activity is decreased. In these contexts, the PEG-Prom represents a valuable predictive tool and readout to identify molecules with potential antitumor activity, without a priori identification of the genetic changes causative of the transformed/tumorigenic phenotype. The primary goal of this screen is to identify chemical inhibitors of the PEG-Promoter generated from high-throughput screening methods. These small molecule chemical probes might have potential anticancer properties and could provide a foundation for the development of novel antitumor drugs.


The primary goal of this project is to identify chemical inhibitors of the PEG-Promoter generated from high-throughput screening methods using HeLa cells stably expressing the PEG-Promoter upstream of firefly luciferase. These small molecule chemical probes might have potential anticancer properties and could provide a foundation for the development of novel antitumor drugs.

The goal of these assays is to confirm hits from "uHTS identification of Peg3 Promoter Inhibitors in a luminescence assay", AID 588405. Cytotoxicity is determined by testing the compounds in in a normal rat embryo fibroblast cell line (CREF). A luciferase reporter assay is used to measure unspecific luciferase reporter activity. Compounds active in either this assay or CREF assay are considered off-target and removed from further consideration.

REFERENCES
1. Su ZZ, Goldstein NI, Jiang H, Wang MN, Duigou GJ, Young CS, Fisher PB. 1999. PEG-3, a nontransforming cancer progression gene, is a positive regulator of cancer aggressiveness and angiogenesis. Proc Natl Acad Sci U S A 96(26):15115-15120.
2. Su ZZ, Emdad L, Sarkar D, Randolph A, Valerie K, Yacoub A, Dent P, Fisher PB. 2005. Potential molecular mechanism for rodent tumorigenesis: mutational generation of progression elevated gene-3 (PEG-3). Oncogene 24(13):2247-2255.
3. Su ZZ, Sarkar D, Emdad L, Duigou GJ, Young CS, Ware J, Randolph A, Valerie K. Fisher PB. 2005. Targeting gene expression selectively in cancer cells using the progression-elevated gene-3 promoter. Proc Natl Acad Sci U S A 102(4):1059-1064.
Panel Information
PEG3
    Data Table(Active)    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescription
ActiveInactive
1IC50_GAPDH_Mean141131RecName: Full=Glyceraldehyde-3-phosphate dehydrogenase; Short=GAPDH; AltName: Full=Peptidyl-cysteine S-nitrosylase GAPDH [gi:120649]
Mean IC50 value
2IC50_1_Range1_GAPDHRecName: Full=Glyceraldehyde-3-phosphate dehydrogenase; Short=GAPDH; AltName: Full=Peptidyl-cysteine S-nitrosylase GAPDH [gi:120649]
IC50 value determined using a sigmoidal dose response equation
3IC50_2_Range1_GAPDHRecName: Full=Glyceraldehyde-3-phosphate dehydrogenase; Short=GAPDH; AltName: Full=Peptidyl-cysteine S-nitrosylase GAPDH [gi:120649]
IC50 value determined using a sigmoidal dose response equation
4IC50_PEG-3_Mean702322protein phosphatase 1 regulatory subunit 15A [Rattus norvegicus] [gi:78486550]
IC50 mean value
5IC50_1_Range1_PEG-3protein phosphatase 1 regulatory subunit 15A [Rattus norvegicus] [gi:78486550]
IC50 value determined using a sigmoidal dose response equation
6IC50_2_Range1_PEG-3protein phosphatase 1 regulatory subunit 15A [Rattus norvegicus] [gi:78486550]
IC50 value determined using a sigmoidal dose response equation
7IC50_Rat fibroblasts (CREF)_Mean282182IC50 value determined using a sigmoidal dose response equation
8IC50_1_Range1_Rat fibroblasts (CREF)IC50 value determined using a sigmoidal dose response equation
9IC50_2_Range1_Rat fibroblasts (CREF)IC50 value determined using a sigmoidal dose response equation

§ Panel component ID.
Protocol
PEG3:
Assay Materials:
PEG-prom-Luc HeLa cells
DMEM 4.5g/l glu w/glu w/o phenol red (Cellgro cat#17-205-CV)
Fetal Bovine Serum (Hyclone Cat# SH30396.03)
L-glutamine (100X ) (Invitrogen Cat#25030081 )
Hygromycin B (CellGro Cat#30-240-CR)
Steady Glo (Promega Cat#E2550)
Assay plate: Aurora 1536 white Solid Bottom Plate

I. Cell Suspension
1- Dispense 4 uL/well of assay media to columns 1-4 using combi dispenser.
2- Dispense 4 uL/well of cells at 3.75X10e5 cells/mL to columns 5-48 using combi Dispenser
3- Spin down plates on Eppendorf centrifuge 5810 at 500 rpm for 1 minute.

II. Compound Addition:
4- Using LabCyte Echo, transfer 2.5 to 40 nL from 10 mM and 2.5 to 40 nl from 0.3125 mM DPI reordered compound source plate into assay plate Columns 5-44 (final concentration of test compounds is 0.195 uM to 99 uM, 1% DMSO), and 40 nL of DMSO to control wells in Columns 1-4 and 45-48.
5- Spin down plates on Vspin at 1000 rpm for 1 minute.
6-Put Kalypsys metal lids on plates, and incubate plates at 37 degrees C with 5% CO2 overnight.

III. Reagent Addition
7- Retrieve plates from incubator, remove lids and allow to plates to cool at room temp for 10 minutes
8- Add 4uL/well of Steady-Glo reagent to all wells using Biotek dispenser.
9- Spin down plates without lids on Vspin at 2000 rpm for 2 min
10- Put lid on, and then incubate plates at room temp for 10 minutes.
IV. Reading plates:
11- Read the plate on PerkinElmer-EnVision plate reader luminescence protocol

Cytotoxicity assay for Peg3 Promoter Inhibitors; CREF normal cells.
Assay Materials:
rat embryo fibroblast cell line (CREF).
DMEM 4.5g/l glu w/glu w/o phenol red (Cellgro cat#17-205-CV)
Fetal Bovine Serum (Hyclone Cat# SH30396.03)
L-glutamine (100X ) (Invitrogen Cat#25030081 )
Hygromycin B (CellGro Cat#30-240-CR)
Steady Glo (Promega Cat#E2550)
Assay plate: Aurora 1536 white Solid Bottom Plate

I. Cell Suspension
1- Dispense 4 uL/well of assay media to columns 1-4 using combi dispenser.
2- Dispense 4 uL/well of cells at 7.5X10e5 cells/mL to columns 5-48 using combi Dispenser
3- Spin down plates on Eppendorf centrifuge 5810 at 500 rpm for 1 minute.

II. Compound Addition:
4- Using LabCyte Echo, transfer 2.5 to 40 nL from 10 mM and 2.5 to 40 nl from 0.3125 mM DPI reordered compound source plate into assay plate Columns 5-44 (final concentration of test compounds is 0.195 uM to 99 uM, 1% DMSO), and 40 nL of DMSO to control wells in Columns 1-4 and 45-48.
5- Spin down plates on Vspin at 1000 rpm for 1 minute.
6-Put Kalypsys metal lids on plates, and incubate plates at 37 degrees C with 5% CO2 for 6 hrs.

III. Reagent Addition
7- Retrieve plates from incubator, remove lids and allow to plates to cool at room temp for 10 minutes
8- Add 4uL/well of Steady-Glo reagent to all wells using Biotek dispenser.
9- Spin down plates without lids on Vspin at 2000 rpm for 2 min
10- Put lid on, and then incubate plates at room temp for 10 minutes.
IV. Reading plates:
11- Read the plate on PerkinElmer-EnVision plate reader luminescence protocol


GAPDH luciferase reporter assay.
Protocol:
Assay Materials:
GAPDH reporter transfected HeLa Cells
DMEM 4.5g/l glu w/glu w/o phenol red (Cellgro cat#17-205-CV)
Fetal Bovine Serum (Hyclone Cat# SH30396.03)
L-glutamine (100X ) (Invitrogen Cat#25030081 )
Hygromycin B (CellGro Cat#30-240-CR)
ATP-Lite (Perkin Elmer Cat# 6016739)
Assay plate: Aurora 1536 white Solid Bottom Plate

I. Cell Suspension
1- Dispense 4 uL/well of assay media to columns 1-4 using combi dispenser.
2- Dispense 4 uL/well of cells at 3.75X10e5 cells/mL to columns 5-48 using combi Dispenser
3- Spin down plates on Eppendorf centrifuge 5810 at 500 rpm for 1 minute.

II. Compound Addition:
4- Using LabCyte Echo, transfer 2.5 to 40 nL from 10 mM and 2.5 to 40 nl from 0.3125 mM DPI reordered compound source plate into assay plate Columns 5-44 (final concentration of test compounds is 0.195 uM to 99 uM, 1% DMSO), and 40 nL of DMSO to control wells in Columns 1-4 and 45-48.
5- Spin down plates on Vspin at 1000 rpm for 1 minute.
6-Put Kalypsys metal lids on plates, and incubate plates at 37 degrees C with 5% CO2 overnight.

III. Reagent Addition
7- Retrieve plates from incubator, remove lids and allow to plates to cool at room temp for 10 minutes
8- Add 4uL/well of ATP-Lite reagent to all wells using Biotek dispenser.
9- Spin down plates without lids on Vspin at 2000 rpm for 2 min
10- Put lid on, and then incubate plates at room temp for 10 minutes.
IV. Reading plates:
11- Read the plate on PerkinElmer-EnVision plate reader luminescence protocol
Comment
Compounds that were active in the PEG3 assay but not in the counter screens are defined as active in this assay.

For the individual assays:

Peg3: Compounds that demonstrated IC50_Mean <= 20 are defined as active.
CREF: Compounds that demonstrated IC50_Mean <= 50 are defined as active.
GAPDH: Compounds that demonstrated IC50_Mean <= 30 are defined as active.

To simplify the distinction between the inactives of the primary screen and of the confirmatory screening stage, the Tiered Activity Scoring System was developed and implemented.

Activity Scoring
Activity scoring rules were devised to take into consideration compound efficacy, its potential interference with the assay and the screening stage that the data was obtained. Details of the Scoring System will be published elsewhere. Briefly, the outline of the scoring system utilized for the assay is as follows:

1) First tier (0-40 range) is reserved for primary screening data is not applicable in this assay.

2) Second tier (41-80 range) is reserved for dose-response confirmation data

a. Inactive compounds of the confirmatory stage are assigned a score value equal 41.
b. The score is linearly correlated with a compound's potency and, in addition, provides a measure of the likelihood that the compound is not an artifact based on the available information.
c. The Hill coefficient is taken as a measure of compound behavior in the assay via an additional scaling factor QC:
QC = 2.6*[exp(-0.5*nH^2) - exp(-1.5*nH^2)]

This empirical factor prorates the likelihood of target- or pathway-specific compound effect vs. its non-specific behavior in the assay. This factor is based on expectation that a compound with a single mode of action that achieved equilibrium in the assay demonstrates the Hill coefficient value of 1. Compounds deviating from that behavior are penalized proportionally to the degree of their deviation.
d. Summary equation that takes into account all the items discussed above is
Score = 44 + 6*(pIC50-3)*QC,
Where pIC50 is a negative log(10) of the IC50 value expressed in mole/L concentration units. This equation results in the Score values above 50 for compounds that demonstrate high potency and predictable behavior. Compounds that are inactive in the assay or whose concentration-dependent behavior are likely to be an artifact of that assay will generally have lower Score values.

3) Third tier (81-100 range) is reserved for resynthesized true positives and their analogues and is not applicable in this assay
Categorized Comment - additional comments and annotations
From PubChem:
Assay Cell Type: HeLa
Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1Outcome_b-galactosidase_GAPDH1RecName: Full=Glyceraldehyde-3-phosphate dehydrogenase; Short=GAPDH; AltName: Full=Peptidyl-cysteine S-nitrosylase GAPDHOutcome
2PUBCHEM_ACTIVITY_SCORE_GAPDH1Integer
3IC50_GAPDH_Mean_QualifierThis qualifier is to be used with the next TID, IC50_Mean. If the qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that value1String
4IC50_GAPDH_MeanIC50 value determined using a sigmoidal dose response equation1FloatμM
5Outcome_PEG-34protein phosphatase 1 regulatory subunit 15A [Rattus norvegicus]Outcome
6PUBCHEM_ACTIVITY_SCORE_PEG-34Integer
7IC50_PEG-3_Mean_QualifierThis qualifier is to be used with the next TID, IC50_Mean. If the qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that value4String
8IC50_PEG-3_Mean*IC50 value determined using a sigmoidal dose response equation4FloatμM
9Outcome_Rat fibroblasts (CREF)7Outcome
10PUBCHEM_ACTIVITY_SCORE_Rat fibroblasts (CREF)4protein phosphatase 1 regulatory subunit 15A [Rattus norvegicus]Integer
11IC50_Rat fibroblasts (CREF)_Mean_QualifierThis qualifier is to be used with the next TID, IC50_Mean. If the qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that value8String
12IC50_Rat fibroblasts (CREF)_MeanIC50 value determined using a sigmoidal dose response equation8FloatμM
13IC50_Qualifier_1_Range1_GAPDHThis qualifier is to be used with the next TID, . If the qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that value2RecName: Full=Glyceraldehyde-3-phosphate dehydrogenase; Short=GAPDH; AltName: Full=Peptidyl-cysteine S-nitrosylase GAPDHString
14IC50_1_Range1_GAPDHIC50 value determined using a sigmoidal dose response equation2FloatμM
15Std.Err(IC50)_1_Range1_GAPDHStandard Error of the IC50 value2FloatμM
16nH_1_Range1_GAPDHHill coefficient determined using sigmoidal dose response equation2Float
17Excluded_Points_first_point_Range1_GAPDHFlags to indicate which of the first dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.2String
18% Activity at 100 uM_first_point_Range1_GAPDH (100μM**)% Activity at the test concentration2Float%
19% Activity at 50 uM_first_point_Range1_GAPDH (50μM**)% Activity at the test concentration2Float%
20% Activity at 25 uM_first_point_Range1_GAPDH (25μM**)% Activity at the test concentration2Float%
21% Activity at 12.5 uM_first_point_Range1_GAPDH (12.5μM**)% Activity at the test concentration2Float%
22% Activity at 6.25 uM_first_point_Range1_GAPDH (6.25μM**)% Activity at the test concentration2Float%
23% Activity at 3.125 uM_first_point_Range1_GAPDH (3.125μM**)% Activity at the test concentration2Float%
24% Activity at 1.5625 uM_first_point_Range1_GAPDH (1.5625μM**)% Activity at the test concentration2Float%
25% Activity at 0.78125 uM_first_point_Range1_GAPDH (0.78125μM**)% Activity at the test concentration2Float%
26% Activity at 0.390625 uM_first_point_Range1_GAPDH (0.390625μM**)% Activity at the test concentration2Float%
27% Activity at 0.1953125 uM_first_point_Range1_GAPDH (0.195312μM**)% Activity at the test concentration2Float%
28IC50_Qualifier_2_Range1_GAPDHThis qualifier is to be used with the next TID, . If the qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that value3RecName: Full=Glyceraldehyde-3-phosphate dehydrogenase; Short=GAPDH; AltName: Full=Peptidyl-cysteine S-nitrosylase GAPDHString
29IC50_2_Range1_GAPDHIC50 value determined using a sigmoidal dose response equation3FloatμM
30Std.Err(IC50)_2_Range1_GAPDHStandard Error of the IC50 value3FloatμM
31nH_2_Range1_GAPDHHill coefficient determined using sigmoidal dose response equation3Float
32Excluded_Points_second_point_Range1_GAPDHFlags to indicate which of the second dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.3String
33% Activity at 100 uM_second_point_Range1_GAPDH (100μM**)% Activity at the test concentration3Float%
34% Activity at 50 uM_second_point_Range1_GAPDH (50μM**)% Activity at the test concentration3Float%
35% Activity at 25 uM_second_point_Range1_GAPDH (25μM**)% Activity at the test concentration3Float%
36% Activity at 12.5 uM_second_point_Range1_GAPDH (12.5μM**)% Activity at the test concentration3Float%
37% Activity at 6.25 uM_second_point_Range1_GAPDH (6.25μM**)% Activity at the test concentration3Float%
38% Activity at 3.125 uM_second_point_Range1_GAPDH (3.125μM**)% Activity at the test concentration3Float%
39% Activity at 1.5625 uM_second_point_Range1_GAPDH (1.5625μM**)% Activity at the test concentration3Float%
40% Activity at 0.78125 uM_second_point_Range1_GAPDH (0.78125μM**)% Activity at the test concentration3Float%
41% Activity at 0.390625 uM_second_point_Range1_GAPDH (0.390625μM**)% Activity at the test concentration3Float%
42% Activity at 0.1953125 uM_second_point_Range1_GAPDH (0.195312μM**)% Activity at the test concentration3Float%
43IC50_Qualifier_1_Range1_PEG-3This qualifier is to be used with the next TID, . If the qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that value5protein phosphatase 1 regulatory subunit 15A [Rattus norvegicus]String
44IC50_1_Range1_PEG-3IC50 value determined using a sigmoidal dose response equation5FloatμM
45Std.Err(IC50)_1_Range1_PEG-3Standard Error of the IC50 value5FloatμM
46nH_1_Range1_PEG-3Hill coefficient determined using sigmoidal dose response equation5Float
47Excluded_Points_first_point_Range1_PEG-3Flags to indicate which of the first dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.5String
48% Activity at 100 uM_first_point_Range1_PEG-3 (100μM**)% Activity at the test concentration5Float%
49% Activity at 50 uM_first_point_Range1_PEG-3 (50μM**)% Activity at the test concentration5Float%
50% Activity at 25 uM_first_point_Range1_PEG-3 (25μM**)% Activity at the test concentration5Float%
51% Activity at 12.5 uM_first_point_Range1_PEG-3 (12.5μM**)% Activity at the test concentration5Float%
52% Activity at 6.25 uM_first_point_Range1_PEG-3 (6.25μM**)% Activity at the test concentration5Float%
53% Activity at 3.125 uM_first_point_Range1_PEG-3 (3.125μM**)% Activity at the test concentration5Float%
54% Activity at 1.5625 uM_first_point_Range1_PEG-3 (1.5625μM**)% Activity at the test concentration5Float%
55% Activity at 0.78125 uM_first_point_Range1_PEG-3 (0.78125μM**)% Activity at the test concentration5Float%
56% Activity at 0.390625 uM_first_point_Range1_PEG-3 (0.390625μM**)% Activity at the test concentration5Float%
57% Activity at 0.1953125 uM_first_point_Range1_PEG-3 (0.195312μM**)% Activity at the test concentration5Float%
58IC50_Qualifier_2_Range1_PEG-3This qualifier is to be used with the next TID, . If the qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that value6protein phosphatase 1 regulatory subunit 15A [Rattus norvegicus]String
59IC50_2_Range1_PEG-3IC50 value determined using a sigmoidal dose response equation6FloatμM
60Std.Err(IC50)_2_Range1_PEG-3Standard Error of the IC50 value6FloatμM
61nH_2_Range1_PEG-3Hill coefficient determined using sigmoidal dose response equation6Float
62Excluded_Points_second_point_Range1_PEG-3Flags to indicate which of the second dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.6String
63% Activity at 100 uM_second_point_Range1_PEG-3 (100μM**)% Activity at the test concentration6Float%
64% Activity at 50 uM_second_point_Range1_PEG-3 (50μM**)% Activity at the test concentration6Float%
65% Activity at 25 uM_second_point_Range1_PEG-3 (25μM**)% Activity at the test concentration6Float%
66% Activity at 12.5 uM_second_point_Range1_PEG-3 (12.5μM**)% Activity at the test concentration6Float%
67% Activity at 6.25 uM_second_point_Range1_PEG-3 (6.25μM**)% Activity at the test concentration6Float%
68% Activity at 3.125 uM_second_point_Range1_PEG-3 (3.125μM**)% Activity at the test concentration6Float%
69% Activity at 1.5625 uM_second_point_Range1_PEG-3 (1.5625μM**)% Activity at the test concentration6Float%
70% Activity at 0.78125 uM_second_point_Range1_PEG-3 (0.78125μM**)% Activity at the test concentration6Float%
71% Activity at 0.390625 uM_second_point_Range1_PEG-3 (0.390625μM**)% Activity at the test concentration6Float%
72% Activity at 0.1953125 uM_second_point_Range1_PEG-3 (0.195312μM**)% Activity at the test concentration6Float%
73IC50_Qualifier_1_Range1_Rat fibroblasts (CREF)This qualifier is to be used with the next TID, . If the qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that value8String
74IC50_1_Range1_Rat fibroblasts (CREF)IC50 value determined using a sigmoidal dose response equation8FloatμM
75Std.Err(IC50)_1_Range1_Rat fibroblasts (CREF)Standard Error of the IC50 value8FloatμM
76nH_1_Range1_Rat fibroblasts (CREF)Hill coefficient determined using sigmoidal dose response equation8Float
77Excluded_Points_first_point_Range1_Rat fibroblasts (CREF)Flags to indicate which of the first dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.8String
78% Activity at 100 uM_first_point_Range1_Rat fibroblasts (CREF) (100μM**)% Activity at the test concentration8Float%
79% Activity at 50 uM_first_point_Range1_Rat fibroblasts (CREF) (50μM**)% Activity at the test concentration8Float%
80% Activity at 25 uM_first_point_Range1_Rat fibroblasts (CREF) (25μM**)% Activity at the test concentration8Float%
81% Activity at 12.5 uM_first_point_Range1_Rat fibroblasts (CREF) (12.5μM**)% Activity at the test concentration8Float%
82% Activity at 6.25 uM_first_point_Range1_Rat fibroblasts (CREF) (6.25μM**)% Activity at the test concentration8Float%
83% Activity at 3.125 uM_first_point_Range1_Rat fibroblasts (CREF) (3.125μM**)% Activity at the test concentration8Float%
84% Activity at 1.5625 uM_first_point_Range1_Rat fibroblasts (CREF) (1.5625μM**)% Activity at the test concentration8Float%
85% Activity at 0.78125 uM_first_point_Range1_Rat fibroblasts (CREF) (0.78125μM**)% Activity at the test concentration8Float%
86% Activity at 0.390625 uM_first_point_Range1_Rat fibroblasts (CREF) (0.390625μM**)% Activity at the test concentration8Float%
87% Activity at 0.1953125 uM_first_point_Range1_Rat fibroblasts (CREF) (0.195312μM**)% Activity at the test concentration8Float%
88IC50_Qualifier_2_Range1_Rat fibroblasts (CREF)This qualifier is to be used with the next TID, . If the qualifier is "=", the IC50 result equals the value in that column. If the qualifier is ">", the IC50 result is greater than that value. If the qualifier is "<", the IC50 result is smaller than that value9String
89IC50_2_Range1_Rat fibroblasts (CREF)IC50 value determined using a sigmoidal dose response equation9FloatμM
90Std.Err(IC50)_2_Range1_Rat fibroblasts (CREF)Standard Error of the IC50 value9FloatμM
91nH_2_Range1_Rat fibroblasts (CREF)Hill coefficient determined using sigmoidal dose response equation9Float
92Excluded_Points_second_point_Range1_Rat fibroblasts (CREF)Flags to indicate which of the second dose-response points were excluded from analysis. (1) means the titration point was excluded and (0) means the point was not excluded.9String
93% Activity at 100 uM_second_point_Range1_Rat fibroblasts (CREF) (100μM**)% Activity at the test concentration9Float%
94% Activity at 50 uM_second_point_Range1_Rat fibroblasts (CREF) (50μM**)% Activity at the test concentration9Float%
95% Activity at 25 uM_second_point_Range1_Rat fibroblasts (CREF) (25μM**)% Activity at the test concentration9Float%
96% Activity at 12.5 uM_second_point_Range1_Rat fibroblasts (CREF) (12.5μM**)% Activity at the test concentration9Float%
97% Activity at 6.25 uM_second_point_Range1_Rat fibroblasts (CREF) (6.25μM**)% Activity at the test concentration9Float%
98% Activity at 3.125 uM_second_point_Range1_Rat fibroblasts (CREF) (3.125μM**)% Activity at the test concentration9Float%
99% Activity at 1.5625 uM_second_point_Range1_Rat fibroblasts (CREF) (1.5625μM**)% Activity at the test concentration9Float%
100% Activity at 0.78125 uM_second_point_Range1_Rat fibroblasts (CREF) (0.78125μM**)% Activity at the test concentration9Float%
101% Activity at 0.390625 uM_second_point_Range1_Rat fibroblasts (CREF) (0.390625μM**)% Activity at the test concentration9Float%
102% Activity at 0.1953125 uM_second_point_Range1_Rat fibroblasts (CREF) (0.195312μM**)% Activity at the test concentration9Float%

* Activity Concentration. ** Test Concentration. § Panel component ID.
Additional Information
Grant Number: 2R01 GM068385-06

Classification
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