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BioAssay: AID 493161

Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compounds

Name: Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compounds. ..more
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 Tested Compounds
 Tested Compounds
All(3)
 
 
Inactive(3)
 
 
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 Tested Substances
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Inactive(3)
 
 
 Related BioAssays
 Related BioAssays
AID: 493161
Data Source: The Scripps Research Institute Molecular Screening Center (TCELLCYTOX_INH_ABSORB_4XCC50)
BioAssay Type: Panel, Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
BioAssay Version:
Deposit Date: 2011-02-08
Hold-until Date: 2011-09-01
Modify Date: 2011-09-01

Data Table ( Complete ):           View All Data
Tested Compounds:
Related Experiments
Show more
AIDNameTypeProbeComment
2174Counterscreen for PME1 inhibitors: fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of lysophospholipase 1 (LYPLA1).Screening depositor-specified cross reference: Counterscreen (LYPLA1 inhibitors in singlicate)
2202Summary of probe development efforts to identify inhibitors of lysophospholipase 1 (LYPLA1).Summary2 depositor-specified cross reference: Summary (LYPLA1 inhibitors)
2203Summary of probe development efforts to identify inhibitors of lysophospholipase 2 (LYPLA2).Summary1 depositor-specified cross reference
2233Counterscreen for PME1 inhibitors: fluorescence polarization-based biochemical high throughput confirmation assay for inhibitors of lysophospholipase 1 (LYPLA1).Screening depositor-specified cross reference: Confirmation counterscreen (LYPLA1 inhibitors in triplicate)
504482Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: fluorescence-based cell-based gel-based Activity-Based Protein Profiling (ABPP) IC50 for anti-target ABHD11Confirmatory depositor-specified cross reference
504498Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: LC-MS/MS assay to assess binding of compounds to active site of anti-target ABHD11Other depositor-specified cross reference
504505Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: fluorescence-based cell-based gel-based Activity-Based Protein Profiling (ABPP) percent inhibition for anti-target ABHD11Other depositor-specified cross reference
504507Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: fluorescence-based biochemical gel-based Activity-Based Protein Profiling (ABPP) IC50 for anti-target ABHD11 Set 2Confirmatory depositor-specified cross reference
504510Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compounds set 2Confirmatory depositor-specified cross reference
504520Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: fluorescence-based biochemical gel-based Activity-Based Protein Profiling (ABPP) inhibition and selectivityOther depositor-specified cross reference
504522Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: LC-MS-based cell-based SILAC Activity-Based Protein Profiling (ABPP) for anti-target ABHD11Other depositor-specified cross reference
504892Late stage assay provider results from the probe development effort to identify inhibitors of ABHD11: Fluorescence-based biochemical gel-based Activity-Based Protein Profiling (ABPP) inhibition of the human isoform of ABHD11Other depositor-specified cross reference
651978Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: LCMS-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in vitroOther depositor-specified cross reference
651979Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in situOther depositor-specified cross reference
651980Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in situOther depositor-specified cross reference
651981Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: LCMS-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in vitroOther depositor-specified cross reference
651985Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP evaluation of activity in vivoOther depositor-specified cross reference
651986Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP evaluation of activity in situOther depositor-specified cross reference
651987Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP gel filtration assay to assess binding modeOther depositor-specified cross reference
651988Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition and selectivityOther depositor-specified cross reference
651990Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical dose-response gel-based ABPPConfirmatory depositor-specified cross reference
651991Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compoundsConfirmatory depositor-specified cross reference
651998Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: Substrate-based fluorescence-based biochemical determination of kinetic parametersConfirmatory depositor-specified cross reference
652001Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: Substrate-based fluorescence-based biochemical determination of kinetic parametersConfirmatory depositor-specified cross reference
652003Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: fluorescence-based biochemical dose-response assayConfirmatory depositor-specified cross reference
652004Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: fluorescence-based biochemical dose-response assayConfirmatory depositor-specified cross reference
652018Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: LCMS-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in vitro, Set 2Other depositor-specified cross reference
652029Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibitionOther depositor-specified cross reference
652030Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition and selectivityOther depositor-specified cross reference
743117Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition potency and selectivityOther depositor-specified cross reference
743118Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical dose-response gel-based ABPP in vitroConfirmatory depositor-specified cross reference
743119Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical dose-response gel-based ABPP in situConfirmatory depositor-specified cross reference
743127Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compoundsConfirmatory depositor-specified cross reference
743132Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical dose-response gel-based ABPP in vitro in mouse brainConfirmatory depositor-specified cross reference
743133Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP gel filtration assay to assess inhibitor binding modeOther depositor-specified cross reference
743134Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP assay to assess in vivo activityOther depositor-specified cross reference
743137Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysisOther depositor-specified cross reference
2143Summary of probe development efforts to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).Summary3 same project related to Summary assay
493105Assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition of recombinant and endogenous enzymeOther same project related to Summary assay
493108Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: fluorescence-based cell-based inhibitionOther same project related to Summary assay
493109Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: LC-MS/MS assay to assess binding of compounds to active siteOther same project related to Summary assay
493110Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: Gel-based Activity-Based Protein Profiling (ABPP) IC50 for LYPLA1 and LYPLA2Confirmatory same project related to Summary assay
493111Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition and selectivityOther same project related to Summary assay
493154Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Gel-based Activity-Based Protein Profiling (ABPP) IC50 for off-target ABHD11Confirmatory same project related to Summary assay
2143Summary of probe development efforts to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).Summary3 same project related to Summary assay
2177Counterscreen for PME1 inhibitors: fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of lysophospholipase 2 (LYPLA2).Screening same project related to Summary assay
2232Counterscreen for PME1 inhibitors: fluorescence polarization-based biochemical high throughput confirmation assay to identify inhibitors of lysophospholipase 2 (LYPLA2).Screening same project related to Summary assay
493105Assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition of recombinant and endogenous enzymeOther same project related to Summary assay
493108Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: fluorescence-based cell-based inhibitionOther same project related to Summary assay
493109Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: LC-MS/MS assay to assess binding of compounds to active siteOther same project related to Summary assay
493110Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: Gel-based Activity-Based Protein Profiling (ABPP) IC50 for LYPLA1 and LYPLA2Confirmatory same project related to Summary assay
493111Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition and selectivityOther same project related to Summary assay
493154Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Gel-based Activity-Based Protein Profiling (ABPP) IC50 for off-target ABHD11Confirmatory same project related to Summary assay
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC)
Center Affiliation: The Scripps Research Institute (TSRI)
Assay Provider: Benjamin Cravatt, TSRI
Network: Molecular Libraries Probe Production Centers Network (MLPCN)
Grant Proposal Number: 1 R01 CA132630-01
Grant Proposal PI: Benjamin Cravatt, TSRI
External Assay ID: TCELLCYTOX_INH_ABSORB_4XCC50

Name: Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compounds.

Description:

Protein palmitoylation is an essential post-translational modification necessary for trafficking and localization of regulatory proteins that play key roles in cell growth and signaling. Numerous proteins have been identified as targets of palmitoylation, including cytoskeletal proteins, kinases, receptors, and other proteins involved in various aspects of cellular signaling and homeostasis (1). Using a global chemo-proteomic method for the metabolic incorporation and identification of palmitoylated proteins, we were able to identify hundreds of palmitoylated proteins, revealing palmitoylation as a widespread post-translational modification (PTM) (2). Palmitoylation involves an acyl-thioester linkage to specific cysteines (3,4). Given the labile properties of thioesters, palmitoylation is potentially reversible and may be regulated in a manner analogous to other PTMs (e.g., phosphorylation). As such, identification of proteins responsible for the dynamic modulation of palmitoylation is paramount to understanding its patho/physiological roles. For example, multiple oncogenes, including HRAS and SRC, require palmitoylation for malignant transformation (5), suggesting protein palmitoyl thioesterases may have tumor suppressor activity required to repress aberrant growth signaling. More than a decade ago, the cytosolic serine hydrolase acyl-protein thioesterase 1 (APT1) was identified as an in vitro HRAS palmitoyl thioesterase (6). Initially classified as lysophospholipase 1 (LYPLA1) (7), the enzyme has since been demonstrated to have several hundred-fold higher activity as a protein thioesterase. While the in vitro data (6,8) provided an intriguing clue to its possible role in vivo, prior to our studies, little was known about the in vivo thioesterase activity of LYPLA1. Upon retroviral shRNA knockdown of LYPLA1, we found that HRAS was robustly hyper-palmitoylated, providing the first evidence that the endogenous enzyme is a functional protein palmitoyl thioesterase capable of regulating HRAS palmitoylation in mammalian cells. However, shRNA resulted in only an 80% reduction in LYPLA1 expression (unpublished). LYPLA2 (a.k.a. APT2) is 65% identical to LYPLA1, and also exhibits lysophospholipase activity in vitro, but its potential role as a thioesterase is unknown (9). shRNA knockdown studies of LYPLA2 revealed only partial knockdown of the enzyme, making substrate identification inconclusive (unpublished). A principle goal of post-genomic research is the determination of the molecular and cellular role of uncharacterized enzymes like LYPLA1 and LYPLA2. As such, a dual inhibitor selective for both LYPLA1 and LYPLA2 would greatly aid investigations into the biological function of these related enzymes. Several inhibitors of LYPLA1 have been described (10,11), but none of these agents have proven capable of inhibiting LYPLA1 activity in cells, and no selective inhibitors of LYPLA2 have been reported to date. To comprehensively identify LYPLA1 and LYPLA2 substrates and functionally test the role of these enzymes in dynamic de-palmitoylation and tumorigenesis, development of a high affinity inhibitor, capable of achieving temporal and more complete control over activity, is critical.

References:

1. Smotrys, J.E. and Linder, M.E. PALMITOYLATION OF INTRACELLULAR SIGNALING PROTEINS: Regulation and Function. Annual Review of Biochemistry, 2004. 73: 559-587.
2. Martin, B.R. and Cravatt, B.F. Large-scale profiling of protein palmitoylation in mammalian cells. Nat Methods, 2009. 6: 135-138.
3. Magee, A.I., Koyama, A.H., Malfer, C., Wen, D. and Schlesinger, M. J. Release of fatty acids from virus glycoproteins by hydroxylamine. Biochimica et Biophysica Acta (BBA) - General Subjects, 1984. 798: 156-166.
4. Rose, J.K., Adams, G.A. and Gallione, C.J. The presence of cysteine in the cytoplasmic domain of the vesicular stomatitis virus glycoprotein is required for palmitate addition. Proc Natl Acad Sci USA, 1984. 81: 2050-2054.
5. Willumsen, B.M., Cox, A.D., Solski, P.A., Der, C.J. and Buss, J.E. Novel determinants of H-Ras plasma membrane localization and transformation. Oncogene, 1996. 13: 1901-1909.
6. Duncan, J.A. and Gilman, A.G. A Cytoplasmic Acyl-Protein Thioesterase That Removes Palmitate from G Protein alpha Subunits and p21RAS. J Biol Chem, 1998. 273: 15830-15837.
7. Sugimoto, H., Hayashi, H. & Yamashita, S. Purification, cDNA cloning, and regulation of lysophospholipase from rat liver. J Biol Chem, 1996. 271: 7705-7711.
8. Hirano, T. et al. Thioesterase activity and subcellular localization of acylprotein thioesterase 1/lysophospholipase 1. Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, 2009. 1791: 797-805.
9. Toyoda, T., Sugimoto, H. and Yamashita, S. Sequence, expression in Escherichia coli, and characterization of lysophospholipase II. Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, 1999. 1437: 182-193.
10. Biel, M., Deck, P., Giannis, A. and Waldmann, H. Synthesis and Evaluation of Acyl Protein Thioesterase 1 (APT1) Inhibitors. Chemistry - A European Journal, 2006. 12: 4121-4143.
11. Deck, P. et al. Development and Biological Evaluation of Acyl Protein Thioesterase 1 (APT1) Inhibitors. Angewandte Chemie International Edition, 2005. 44: 4975-4980.

Keywords:

late stage, late stage AID, assay provider, powders, LYPLA1, lysophospholipase 1, LYPLA2, lysophospholipase 2, APT1, acyl-protein thioesterase 1, APT2, acyl-protein thioesterase 2, serine hydrolase, palmitoylation, counterscreen, inhibitor, cytotoxicity, CC50, activity-based protein profiling, ABPP, gel-based ABPP, fluorophosphonate rhodamine, FP-Rh, Scripps, Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN
Panel Information
Assays (see Protocol for details).
PID§NameSubstancePanel TargetsDescription
ActiveInactive
1Assay 1: serum-free media3
2Assay 2: media plus FCS3

§ Panel component ID.
Protocol
Assay Overview:
The purpose of this assay is to determine cytotoxicity of inhibitor compounds belonging to the urea triazole scaffold. In this assay, BW5147-derived murine T-cells in either serum-free media (Panel Assay 1) or media containing FCS (Panel Assay 2) are incubated with test compounds, followed by determination of cell viability. The assay utilizes the WST-1 substrate which is converted into colorimetric formazan dye by the metabolic activity of viable cells. The amount of formed formazan directly correlates to the number of metabolically active cells in the culture. As designed, compounds that reduce cell viability will result in decreased absorbance of the dye. Compounds were tested in quadruplicate in a 7-point 1:5 dilution series starting at a nominal test concentration of 50 uM.
Protocol Summary:
This assay was started by dispensing BW5147-derived murine T-cells in RPMI media (100 uL, 10E4 cells/well) into a 96-well plate. Both serum-free media (Assay 1) and media supplemented with fetal calf serum (FCS) (Assay 2) were tested. Compound (5 uL of 0-200 uM in media containing 5% DMSO) was added to each well, giving final compound concentrations of 0-50 uM. Cells were incubated for 48 hours at 37 C in a humidified incubator and cell viability was determined by the WST-1 assay (Roche) according to manufacturer instructions.
The % cell viability for each well was then calculated as follows:
% Cell Viability = ( ABS_Test_Compound - Median_ABS_Low_Control ) / ( Median_ABS_High_Control - Median_ABS_Low_Control ) * 100
Where:
Test_Compound is defined as wells containing cells in the presence of test compound.
High_Control is defined as wells containing cells treated with media only (no compound).
Low_Control is defined as wells containing no cells (media only).
For each test compound, percent cell viability was plotted against the log of the compound concentration. The CC50 is reported as "> X uM" (where X = the highest concentration tested for which less than 50% cell survival was observed).
PubChem Activity Outcome and Score:
The following applies to each panel in this assay:
Compounds with a CC50 value of less than 5 uM were considered active (cytotoxic). Compounds with a CC50 value greater than or equal to 5 uM were considered inactive (non-cytotoxic).
Any compound with a percent activity value less than 50% at all test concentrations was assigned an activity score of zero. Any compound with a percent activity value greater than or equal to 50% at any test concentration was assigned an activity score greater than zero.
Activity score was then ranked by the potency of the compounds with fitted curves, with the most potent compounds assigned the highest activity scores.
Panel Assay 1 Score: The PubChem Activity Score range for inactive compounds is 100-0. There are no active compounds.
Panel Assay 2 Score: The PubChem Activity Score range for inactive compounds is 100-0. There are no active compounds.
Overall Outcome and Score:
The overall outcome was active if the compound was active in at least one panel, inactive otherwise.
The overall score is 0 if the compound was inactive, otherwise the score is taken as the fraction of panels where the compound is active, multiplied by 100.
The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.
List of Reagents:
BW5147-derived murine T-cells (provided by Assay Provider)
RPMI Media (CellGro 10-040-CV)
FCS (Omega Scientific, FB-01)
WST-1 reagent (Roche)
96-well plates (Corning)
Comment
This assay was performed by the assay provider with powder samples of compounds.
Categorized Comment - additional comments and annotations
From PubChem:
Assay Format: Cell-based
Assay Type: Toxicity
Assay Cell Type: BW5147
Result Definitions
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TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Outcome [Assay 1]One of Active, Inactive, or Not Tested1Outcome
2Score [Assay 1]The BioAssay activity ranking score1Integer
3Qualifier [Assay 1]Qualifier identifies if the resultant fold selectivity was determined to be less than or greater than its listed fold selectivity.1String
4CC50 [Assay 1]*The value for concentration at which 50% inhibition is observed; CC50 shown in uM.1FloatμM
5Surviving cells at 0.0032 uM [1, Assay 1] (0.032μM**)Value of % Surviving cells at 0.0032 uM inhibitor concentration; replicate one.1Float%
6Surviving cells at 0.0032 uM [2, Assay 1] (0.032μM**)Value of % Surviving cells at 0.0032 uM inhibitor concentration; replicate two.1Float%
7Surviving cells at 0.0032 uM [3, Assay 1] (0.032μM**)Value of % Surviving cells at 0.0032 uM inhibitor concentration; replicate three.1Float%
8Surviving cells at 0.0032 uM [4, Assay 1] (0.032μM**)Value of % Surviving cells at 0.0032 uM inhibitor concentration; replicate four.1Float%
9Surviving cells at 0.016 uM [1, Assay 1] (0.016μM**)Value of % Surviving cells at 0.016 uM inhibitor concentration; replicate one.1Float%
10Surviving cells at 0.016 uM [2, Assay 1] (0.016μM**)Value of % Surviving cells at 0.016 uM inhibitor concentration; replicate two.1Float%
11Surviving cells at 0.016 uM [3, Assay 1] (0.016μM**)Value of % Surviving cells at 0.016 uM inhibitor concentration; replicate three.1Float%
12Surviving cells at 0.016 uM [4, Assay 1] (0.016μM**)Value of % Surviving cells at 0.016 uM inhibitor concentration; replicate four.1Float%
13Surviving cells at 0.080 uM [1, Assay 1] (0.08μM**)Value of % Surviving cells at 0.080 uM inhibitor concentration; replicate one.1Float%
14Surviving cells at 0.080 uM [2, Assay 1] (0.08μM**)Value of % Surviving cells at 0.080 uM inhibitor concentration; replicate two.1Float%
15Surviving cells at 0.080 uM [3, Assay 1] (0.08μM**)Value of % Surviving cells at 0.080 uM inhibitor concentration; replicate three.1Float%
16Surviving cells at 0.080 uM [4, Assay 1] (0.08μM**)Value of % Surviving cells at 0.080 uM inhibitor concentration; replicate four.1Float%
17Surviving cells at 0.400 uM [1, Assay 1] (0.4μM**)Value of % Surviving cells at 0.400 uM inhibitor concentration; replicate one.1Float%
18Surviving cells at 0.400 uM [2, Assay 1] (0.4μM**)Value of % Surviving cells at 0.400 uM inhibitor concentration; replicate two.1Float%
19Surviving cells at 0.400 uM [3, Assay 1] (0.4μM**)Value of % Surviving cells at 0.400 uM inhibitor concentration; replicate three.1Float%
20Surviving cells at 0.400 uM [4, Assay 1] (0.4μM**)Value of % Surviving cells at 0.400 uM inhibitor concentration; replicate four.1Float%
21Surviving cells at 2 uM [1, Assay 1] (2μM**)Value of % Surviving cells at 2 uM inhibitor concentration; replicate one.1Float%
22Surviving cells at 2 uM [2, Assay 1] (2μM**)Value of % Surviving cells at 2 uM inhibitor concentration; replicate two.1Float%
23Surviving cells at 2 uM [3, Assay 1] (2μM**)Value of % Surviving cells at 2 uM inhibitor concentration; replicate three.1Float%
24Surviving cells at 2 uM [4, Assay 1] (2μM**)Value of % Surviving cells at 2 uM inhibitor concentration; replicate four.1Float%
25Surviving cells at 10 uM [1, Assay 1] (10μM**)Value of % Surviving cells at 10 uM inhibitor concentration; replicate one.1Float%
26Surviving cells at 10 uM [2, Assay 1] (10μM**)Value of % Surviving cells at 10 uM inhibitor concentration; replicate two.1Float%
27Surviving cells at 10 uM [3, Assay 1] (10μM**)Value of % Surviving cells at 10 uM inhibitor concentration; replicate three.1Float%
28Surviving cells at 10 uM [4, Assay 1] (10μM**)Value of % Surviving cells at 10 uM inhibitor concentration; replicate four.1Float%
29Surviving cells at 50 uM [1, Assay 1] (50μM**)Value of % Surviving cells at 50 uM inhibitor concentration; replicate one.1Float%
30Surviving cells at 50 uM [2, Assay 1] (50μM**)Value of % Surviving cells at 50 uM inhibitor concentration; replicate two.1Float%
31Surviving cells at 50 uM [3, Assay 1] (50μM**)Value of % Surviving cells at 50 uM inhibitor concentration; replicate three.1Float%
32Surviving cells at 50 uM [4, Assay 1] (50μM**)Value of % Surviving cells at 50 uM inhibitor concentration; replicate four.1Float%
33Outcome [Assay 2]One of Active, Inactive, or Not Tested2Outcome
34Score [Assay 2]The BioAssay activity ranking score2Integer
35Qualifier [Assay 2]Qualifier identifies if the resultant fold selectivity was determined to be less than or greater than its listed fold selectivity.2String
36CC50 [Assay 2]*The value for concentration at which 50% inhibition is observed; CC50 shown in uM.2FloatμM
37Surviving cells at 0.0032 uM [1, Assay 2] (0.032μM**)Value of % Surviving cells at 0.0032 uM inhibitor concentration; replicate one.2Float%
38Surviving cells at 0.0032 uM [2, Assay 2] (0.032μM**)Value of % Surviving cells at 0.0032 uM inhibitor concentration; replicate two.2Float%
39Surviving cells at 0.0032 uM [3, Assay 2] (0.032μM**)Value of % Surviving cells at 0.0032 uM inhibitor concentration; replicate three.2Float%
40Surviving cells at 0.0032 uM [4, Assay 2] (0.032μM**)Value of % Surviving cells at 0.0032 uM inhibitor concentration; replicate four.2Float%
41Surviving cells at 0.016 uM [1, Assay 2] (0.016μM**)Value of % Surviving cells at 0.016 uM inhibitor concentration; replicate one.2Float%
42Surviving cells at 0.016 uM [2, Assay 2] (0.016μM**)Value of % Surviving cells at 0.016 uM inhibitor concentration; replicate two.2Float%
43Surviving cells at 0.016 uM [3, Assay 2] (0.016μM**)Value of % Surviving cells at 0.016 uM inhibitor concentration; replicate three.2Float%
44Surviving cells at 0.016 uM [4, Assay 2] (0.016μM**)Value of % Surviving cells at 0.016 uM inhibitor concentration; replicate four.2Float%
45Surviving cells at 0.080 uM [1, Assay 2] (0.08μM**)Value of % Surviving cells at 0.080 uM inhibitor concentration; replicate one.2Float%
46Surviving cells at 0.080 uM [2, Assay 2] (0.08μM**)Value of % Surviving cells at 0.080 uM inhibitor concentration; replicate two.2Float%
47Surviving cells at 0.080 uM [3, Assay 2] (0.08μM**)Value of % Surviving cells at 0.080 uM inhibitor concentration; replicate three.2Float%
48Surviving cells at 0.080 uM [4, Assay 2] (0.08μM**)Value of % Surviving cells at 0.080 uM inhibitor concentration; replicate four.2Float%
49Surviving cells at 0.400 uM [1, Assay 2] (0.4μM**)Value of % Surviving cells at 0.400 uM inhibitor concentration; replicate one.2Float%
50Surviving cells at 0.400 uM [2, Assay 2] (0.4μM**)Value of % Surviving cells at 0.400 uM inhibitor concentration; replicate two.2Float%
51Surviving cells at 0.400 uM [3, Assay 2] (0.4μM**)Value of % Surviving cells at 0.400 uM inhibitor concentration; replicate three.2Float%
52Surviving cells at 0.400 uM [4, Assay 2] (0.4μM**)Value of % Surviving cells at 0.400 uM inhibitor concentration; replicate four.2Float%
53Surviving cells at 2 uM [1, Assay 2] (2μM**)Value of % Surviving cells at 2 uM inhibitor concentration; replicate one.2Float%
54Surviving cells at 2 uM [2, Assay 2] (2μM**)Value of % Surviving cells at 2 uM inhibitor concentration; replicate two.2Float%
55Surviving cells at 2 uM [3, Assay 2] (2μM**)Value of % Surviving cells at 2 uM inhibitor concentration; replicate three.2Float%
56Surviving cells at 2 uM [4, Assay 2] (2μM**)Value of % Surviving cells at 2 uM inhibitor concentration; replicate four.2Float%
57Surviving cells at 10 uM [1, Assay 2] (10μM**)Value of % Surviving cells at 10 uM inhibitor concentration; replicate one.2Float%
58Surviving cells at 10 uM [2, Assay 2] (10μM**)Value of % Surviving cells at 10 uM inhibitor concentration; replicate two.2Float%
59Surviving cells at 10 uM [3, Assay 2] (10μM**)Value of % Surviving cells at 10 uM inhibitor concentration; replicate three.2Float%
60Surviving cells at 10 uM [4, Assay 2] (10μM**)Value of % Surviving cells at 10 uM inhibitor concentration; replicate four.2Float%
61Surviving cells at 50 uM [1, Assay 2] (50μM**)Value of % Surviving cells at 50 uM inhibitor concentration; replicate one.2Float%
62Surviving cells at 50 uM [2, Assay 2] (50μM**)Value of % Surviving cells at 50 uM inhibitor concentration; replicate two.2Float%
63Surviving cells at 50 uM [3, Assay 2] (50μM**)Value of % Surviving cells at 50 uM inhibitor concentration; replicate three.2Float%
64Surviving cells at 50 uM [4, Assay 2] (50μM**)Value of % Surviving cells at 50 uM inhibitor concentration; replicate four.2Float%

* Activity Concentration. ** Test Concentration. § Panel component ID.
Additional Information
Grant Number: 1 R01 CA132630

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