Bookmark and Share
BioAssay: AID 2749

Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): luminescence-based cell-based dose response assay for cytotoxic compounds using the IEC-6 intestinal epithelial cell line

Name: Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): luminescence-based cell-based dose response assay for cytotoxic compounds using the IEC-6 intestinal epithelial cell line. ..more
_
   
 Tested Compounds
 Tested Compounds
All(20)
 
 
Inactive(20)
 
 
 Tested Substances
 Tested Substances
All(24)
 
 
Inactive(24)
 
 
 Related BioAssays
 Related BioAssays
AID: 2749
Data Source: The Scripps Research Institute Molecular Screening Center (IEC6CYTOX_INH_LUMI_1536_3XIC50 CSDRUN SAR_Round 0)
BioAssay Type: Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network
Deposit Date: 2010-04-02
Hold-until Date: 2011-03-31
Modify Date: 2011-03-31

Data Table ( Complete ):           All
Tested Compounds:
Depositor Specified Assays
Show more
AIDNameTypeComment
1700Primary cell-based high throughput screening assay to identify inhibitors of kruppel-like factor 5 (KLF5)screeningPrimary Assay (KLF5 inhibition, 1X %INH)
1825Luminescence-based counterscreen assay for KLF5 inhibitors: cell-based high throughput screening assay to identify cytotoxic compounds using the IEC-6 intestinal epithelial cell line.screeningCounterscreen (ICE-6 cytotoxicity, 1X %INH)
1834Luminescence-based confirmation cell-based high throughput screening assay to identify inhibitors of kruppel-like factor 5 (KLF5)screeningConfirmation (KLF5 inhibition, 3X %INH)
1858Summary of probe development efforts to identify inhibitors of kruppel-like factor 5 (KLF5)summarySummary AID
1905Luminescence-based counterscreen assay for KLF5 inhibitors: cell-based high throughput screening assay to identify cytotoxic compounds using the IEC-6 intestinal epithelial cell line in triplicate.screeningCounterscreen (ICE-6 cytotoxicity, 3X %INH)
1973Luminescence-based dose response cell-based high throughput screening assay for inhibitors of kruppel-like factor 5 (KLF5).confirmatoryDose response Assay (KLF5 3X IC50)
1975Luminescence-based counterscreen assay for KLF5 inhibitors: dose response cell-based high throughput screening assay to identify cytotoxic compounds using the IEC-6 intestinal epithelial cell line.confirmatoryDose response Assay (IEC-6 cytotoxicity 3X IC50)
434957Late stage results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): luminescence-based cell-based dose response assay for inhibitors of KLF5 (Round 1)confirmatory
485338Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): luminescence-based cell-based dose response assay for cytotoxic compounds using the DLD-1 cell line (Round 1)confirmatory
588614Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Mitogen-Activated Protein Kinase 1 (MAPK1; ERK1/2) protein levels in DLD1 cellsother
588617Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of KLF5 protein levels in DLD1 cellsother
588640Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of P38 protein levels in HCT116 human colorectal carcinoma cellsother
588643Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Mitogen-Activated Protein Kinase 1 (P-MAPK1; P-ERK1/2) protein levels in HCT116 human colorectal carcinoma cellsother
588646Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of phosphorylated P38 protein levels in HCT116 human colorectal carcinoma cellsother
434956Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): luminescence-based cell-based dose response assay for cytotoxic compounds using the IEC-6 intestinal epithelial cell line (Round 1)confirmatory
588648Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Epidermal Growth Factor Receptor (EGFR) protein levels in HCT116 human colorectal carcinoma cellsother
588654Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Epidermal Growth Factor Receptor (EGFR) protein levels in HT29 human colorectal carcinoma cellsother
588657Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Early Growth Response 1 (EGR1) protein levels in HT29 human colorectal carcinoma cellsother
485336Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of KLF5 protein levelsconfirmatory
588660Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of KLF5 protein levels in HT29 human colorectal carcinoma cellsother
588663Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of phosphorylated P38 protein levels in SW620 human colorectal carcinoma cellsother
588666Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Mitogen-Activated Protein Kinase 1 (MAPK1; ERK1/2) protein levels in SW620 human colorectal carcinoma cellsother
588612Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Mitogen-Activated Protein Kinase 1 (P-MAPK1; P-ERK1/2) protein levels in DLD1 cellsother
588667Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Epidermal Growth Factor Receptor (EGFR) protein levels in SW620 human colorectal carcinoma cellsother
588725Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): Radioactivity-based biochemical assay to identify modulators of a panel of 48 kinasesother
588656Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Mitogen-Activated Protein Kinase 1 (MAPK1; ERK1/2) protein levels in HT29 human colorectal carcinoma cellsother
588659Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of P38 protein levels in HT29 human colorectal carcinoma cellsother
588662Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of P38 protein levels in SW620 human colorectal carcinoma cellsother
588665Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Early Growth Response 1 (EGR1) protein levels in SW620 human colorectal carcinoma cellsother
588615Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of P38 protein levels in DLD1 cellsother
588618Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Early Growth Response 1 (EGR1) protein levels in DLD1 cellsother
588644Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Early Growth Response 1 (EGR1) protein levels in HCT116 human colorectal carcinoma cellsother
588650Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Epidermal Growth Factor Receptor (EGFR) protein levels in HCT116 human colorectal carcinoma cellsother
588653Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Epidermal Growth Factor Receptor (EGFR) protein levels in HT29 human colorectal carcinoma cellsother
588610Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Epidermal Growth Factor Receptor (EGFR) protein levels in DLD1 cellsother
588613Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Epidermal Growth Factor Receptor (EGFR) protein levels in DLD1 cells.other
588616Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of phospho-P38 protein levels in DLD1 cellsother
588642Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Mitogen-Activated Protein Kinase 1 (MAPK1; ERK1/2) protein levels in HCT116 human colorectal carcinoma cellsother
588668Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Mitogen-Activated Protein Kinase 1 (P-MAPK1; P-ERK1/2) protein levels in SW620 human colorectal carcinoma cellsother
588677Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Epidermal Growth Factor Receptor (EGFR) protein levels in SW620 human colorectal carcinoma cellsother
588729Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): Absorbance-based cell-based assay to identify modulators of cancer cell viabilityconfirmatory
588539Late stage assay provider counterscreen results for the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): Cell cycle analysis of the DLD-1 cell lineother
588652Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of KLF5 protein levels in HCT116 human colorectal carcinoma cellsother
588655Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of Phosphorylated Mitogen-Activated Protein Kinase 1 (P-MAPK1; P-ERK1/2) protein levels in HT29 human colorectal carcinoma cellsother
588658Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of phosphorylated P38 protein levels in HT29 human colorectal carcinoma cellsother
588661Late stage assay provider counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): chemiluminescence-based western blot assay for inhibitors of KLF5 protein levels in SW620 human colorectal carcinoma cellsother
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center
Affiliation: The Scripps Research Institute, TSRI
Assay Provider: Vincent Yang, Emory University
Network: Molecular Library Probe Production Centers Network (MLPCN)
Grant Proposal Number 1-R03-DA026215-01
Grant Proposal PI: Vincent Yang
External Assay ID: IEC6CYTOX_INH_LUMI_1536_3XIC50 CSDRUN SAR_Round 0

Name: Late stage counterscreen results from the probe development effort to identify inhibitors of kruppel-like factor 5 (KLF5): luminescence-based cell-based dose response assay for cytotoxic compounds using the IEC-6 intestinal epithelial cell line.

Description:

Transcription factors are essential regulators of transcription that bind DNA to control both the rate and frequncy of gene expression (1). Many diseases of cell homeostasis are associated with aberrant transcription factor activity (2). Colon cancer, in particular, is a disease of uncontrolled proliferation of the epithelial cells that line the intestinal crypts. Kruppel-like factor 5 (KLF5) is a zinc finger-containing transcription factor that binds to GC-rich sequnces in promoters of numerous genes (3) including cyclin D1 (4), cyclin B1/Cdc2 (4), and integrin-linked kinase (5). KLF5 is highly expressed in rapidly dividing epithelial cells in intestinal crypts (6). This expression pattern of KLF5, along with studies demonstrating that KLF5 mediates the transforming effects of oncogenic H-Ras (7), and that ectopic expression of KLF5 leads to increased cell proliferation and anchorage-independent growth of cultured intestinal epithelial cells (8, 9), suggest that KLF5 may be involved in colon cancer pathogenesis. Therefore, the identification of selective inhibitors of KLF5 may provide useful tools to elucidate the role of KLF5 as a regulator of cellular proliferation and tumor formation in the intestinal epithelium.

References:

1. Ptashne M. Regulation of transcription: from lambda to eukaryotes. Trends Biochem Sci. 2005 Jun;30(6):275-9.
2. Fre S, Vignjevic D, Schoumacher M, Duffy SL, Janssen KP, Robine S, Louvard D. Adv Cancer Res. 2008;100:85-111. Epithelial morphogenesis and intestinal cancer: new insights in signaling mechanisms.
3. Goldstein BG, Chao HH, Yang Y, Yermolina YA, Tobias JW, Katz JP. Am J Physiol Gastrointest Liver Physiol. 2007 Jun;292(6):G1784-92. Overexpression of Kruppel-like factor 5 in esophageal epithelia in vivo leads to increased proliferation in basal but not suprabasal cells.
4. Ghaleb AM, Nandan MO, Chanchevalap S, Dalton WB, Hisamuddin IM, Yang VW. Kruppel-like factors 4 and 5: the yin and yang regulators of cellular proliferation. Cell Res. 2005 Feb;15(2):92-6.
5. Yang Y, Tetreault MP, Yermolina YA, Goldstein BG, Katz JP. Kruppel-like factor 5 controls keratinocyte migration via the integrin-linked kinase. J Biol Chem. 2008 Jul 4;283(27):18812-20.
6. McConnell BB, Ghaleb AM, Nandan MO, Yang VW. The diverse functions of Kruppel-like factors 4 and 5 in epithelial biology and pathobiology. Bioessays. 2007 Jun;29(6):549-57. Erratum in: Bioessays. 2007 Sep;29(9):946.
7. Nandan MO, Yoon HS, Zhao W, Ouko LA, Chanchevalap S, Yang VW. Kruppel-like factor 5 mediates the transforming activity of oncogenic H-Ras. Oncogene. 2004 Apr 22;23(19):3404-13.
8. Chanchevalap S, Nandan MO, Merlin D, Yang VW. FEBS Lett. 2004 Dec 3;578(1-2):99-105. All-trans retinoic acid inhibits proliferation of intestinal epithelial cells by inhibiting expression of the gene encoding Kruppel-like factor 5.
9. Sun R, Chen X, Yang VW. J Biol Chem. 2001 Mar 9;276(10):6897-900. Intestinal-enriched Kruppel-like factor (Kruppel-like factor 5) is a positive regulator of cellular proliferation.

Keywords:

Late stage, powders, purchased, synthesized, IEC-6, intestinal epithelial cells, cytotoxicity, cell viability, KLF5, BTEB2, kruppel-like factor 5, cancer, dose response, counterscreen, HTS, high throughput screen, 1536, inhibitor, inhibition, luciferase, luminescence, CellTiter Glo, Scripps, Scripps Florida, The Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN.
Protocol
Assay Overview:

The purpose of this assay is to determine whether powder samples of compounds identified as active in a previous set of experiments entitled, "Primary cell-based high throughput screening assay to identify inhibitors of kruppel-like factor 5 (KLF5)" (PubChem AID 1700), "Luminescence-based confirmation cell-based high throughput screening assay to identify inhibitors of kruppel-like factor 5 (KLF5)" (AID 1834), "Luminescence-based dose response cell-based high throughput screening assay for inhibitors of kruppel-like factor 5 (KLF5)" (AID 1973), and inactive in a set of experiments entitled, "Luminescence-based counterscreen assay for KLF5 inhibitors: cell-based high throughput screening assay to identify cytotoxic compounds using the IEC-6 intestinal epithelial cell line." (AID 1825), and "Luminescence-based counterscreen assay for KLF5 inhibitors: dose response cell-based high throughput screening assay to identify cytotoxic compounds using the IEC-6 intestinal epithelial cell line)" (AID1975), were nonselective due to IEC6 cell line cytotoxicity. In this assay, rat IEC-6 cells are incubated with test compounds, followed by determination of cell viability. The assay utilizes the CellTiter-Glo luminescent reagent to measure intracellular ATP in viable cells. Luciferase present in the reagent catalyzes the oxidation of beetle luciferin to oxyluciferin and light in the presence of cellular ATP. Well luminescence is directly proportional to ATP levels and cell viability. As designed, compounds that reduce cell viability will reduce ATP levels, luciferin oxidation and light production, resulting in decreased well luminescence. Compounds were tested in triplicate in a 10-point 1:3 dilution series starting at a nominal test concentration of 40 micromolar.

Protocol Summary:

The parental IEC-6 cell line was routinely cultured in T-175 sq cm flasks at 37 degrees C and 95% relative humidity (RH). The growth media consisted of RPMI -1640 supplemented with 10% v/v certified fetal bovine serum, 2 micrograms/ml human recombinant insulin, and 1X antibiotic mix (penicillin, streptomycin, and neomycin).

Prior to the start of the assay 1250 cells in a 5 microliter volume of growth media were dispensed into each well of 1536-well tissue culture-treated microtiter plates. The assay was started immediately by dispensing 20 nL of test compound in DMSO (0.4 % final DMSO concentration), DMSO alone, or doxorubicin (150 micromolar final concentration) to the appropriate wells. Next, the plates were incubated for 48 hours at 37 degrees C (5% CO2, 95% RH). After equilibrating the plates to room temperature for 30 minutes, the assay was stopped by dispensing 5 microliters of CellTiter-Glo reagent to each well, followed by incubation at room temperature for 15 minutes. Well luminescence was measured on the ViewLux plate reader.

The percent inhibition for each compound was calculated as follows:

%Inhibition = ( 1 - ( ( Test_Compound - Median_High_Control ) / ( Median_Low_Control - Median_High_Control ) ) ) * 100

Where:

Test_Compound is defined as wells containing test compound.
Low_Control is defined as wells containing DMSO.
High_Control is defined as wells containing doxorubicin.

For each test compound, percent inhibition was plotted against compound concentration. A four parameter equation describing a sigmoidal dose-response curve was then fitted with adjustable baseline using Assay Explorer software (Symyx Technologies Inc). The reported IC50 values were generated from fitted curves by solving for the X-intercept value at the 50% inhibition level of the Y-intercept value. In cases where the highest concentration tested (i.e. 40 micromolar) did not result in greater than 50% inhibition, the IC50 was determined manually as greater than 40 micromolar. Compounds with an IC50 greater than 10 micromolar were considered inactive. Compounds with an IC50 equal to or less than 10 micromolar were considered active.

PubChem Activity and Score:

Any compound with a percent activity value <50% at all test concentrations was assigned an activity score of zero. Any compound with a percent activity value >50% at any test concentration was assigned an activity score greater than zero. Activity score was then ranked by the potency, with the most potent compounds assigned the highest activity scores.

The PubChem Activity Score range for inactive compounds is 100-1, there are no actives.

List of Reagents:

IEC-6 cell line (provided by Assay Provider)
DMEM medium (Invitrogen, part 11995-065)
100X Penicillin-Streptomycin-Neomycin mix (Invitrogen, part 15640-055)
Human, recombinant insulin (Invitrogen, part 12585-014)
Trypsin-EDTA solution (Invitrogen, part 25200-056)
Fetal Bovine Serum (Invitrogen, part 16000-044)
Cell Titer Glo (Promega, part G75729)
Doxorubicin (Sigma Chemical, part D1515)
T-175 tissue culture flasks (Corning, part 431080)
1536-well plates (Greiner, part 789173)
Comment
This assay may have been run as two or more separate campaigns, each campaign testing a unique set of compounds. In this assay doxorubicin had an IC50 of approximately 100 nM. All data reported were normalized on a per-plate basis. Possible artifacts of this assay can include, but are not limited to: dust or lint located in or on wells of the microtiter plate, compounds that modulate well fluorescence. All test compound concentrations reported above and below are nominal; the specific test concentration(s) for a particular compound may vary based upon the actual sample provided.
Result Definitions
Show more
TIDNameDescriptionHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1QualifierActivity Qualifier identifies if the resultant data IC50 came from a fitted curve or was determined manually to be less than or greater than its listed IC50 concentration.String
2IC50*The concentration at which 50 percent of the activity in the inhibitor assay is observed; (IC50) shown in micromolar.FloatμM
3LogIC50Log10 of the qualified IC50 (IC50) from the inhibitor assay in M concentration.Float
4Hill SlopeThe variable HillSlope describes the steepness of the curve. This variable is called the Hill slope, the slope factor, or the Hill coefficient. If it is positive, the curve increases as X increases. If it is negative, the curve decreases as X increases. A standard sigmoid dose-response curve (previous equation) has a Hill Slope of 1.0. When HillSlope is less than 1.0, the curve is more shallow. When HillSlope is greater than 1.0, the curve is steeper. The Hill slope has no units.Float
5Hill S0Y-min of the curve.Float
6Hill SinfY-max of the curve.Float
7Hill dSThe range of Y.Float
8Chi SquareA measure for the 'goodness' of a fit. The chi-square test (Snedecor and Cochran, 1989) is used to test if a sample of data came from a population with a specific distribution.Float
9RsquareThis statistic measures how successful the fit explains the variation of the data; R-square is the square of the correlation between the response values and the predicted response values.Float
10Number of DataPointsOverall number of data points of normalized percent inhibition that was used for calculations (includes all concentration points); in some cases a data point can be excluded as outlier.Integer
11Inhibition at 2.0 nM (0.002μM**)Value of %inhibition at 2.0 nanomolar inhibitor concentration; average of triplicate measurement.Float%
12Inhibition at 6.1 nM (0.0061μM**)Value of %inhibition at 6.1 nanomolar inhibitor concentration; average of triplicate measurement.Float%
13Inhibition at 18.2 nM (0.0182μM**)Value of %inhibition at 18.2 nanomolar inhibitor concentration; average of triplicate measurement.Float%
14Inhibition at 54.7 nM (0.0547μM**)Value of %inhibition at 54.7 nanomolar inhibitor concentration; average of triplicate measurement.Float%
15Inhibition at 164.0 nM (0.164μM**)Value of %inhibition at 164.0 nanomolar inhibitor concentration; average of triplicate measurement.Float%
16Inhibition at 491.9 nM (0.4919μM**)Value of %inhibition at 491.9 nanomolar inhibitor concentration; average of triplicate measurement.Float%
17Inhibition at 1.5 uM (1.5μM**)Value of %inhibition at 1.5 micromolar inhibitor concentration; average of triplicate measurement.Float%
18Inhibition at 4.4 uM (4.4μM**)Value of %inhibition at 4.4 micromolar inhibitor concentration; average of triplicate measurement.Float%
19Inhibition at 13.3 uM (13.3μM**)Value of %inhibition at 13.3 micromolar inhibitor concentration; average of triplicate measurement.Float%
20Inhibition at 39.8 uM (39.8μM**)Value of %inhibition at 39.8 micromolar inhibitor concentration; average of triplicate measurement.Float%

* Activity Concentration. ** Test Concentration.
Additional Information
Grant Number: 1-R03-DA026215-01

Data Table (Concise)
PageFrom: