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BioAssay: AID 651991

Late 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 compounds

Name: Late 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 compounds. ..more
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 Tested Compounds
 Tested Compounds
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Inactive(4)
 
 
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 Related BioAssays
 Related BioAssays
AID: 651991
Data Source: The Scripps Research Institute Molecular Screening Center (HEK293T_INH_ABS_6XCC50)
BioAssay Type: Panel, Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
BioAssay Version:
Deposit Date: 2013-01-23
Hold-until Date: 2013-10-18
Modify Date: 2013-10-18

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: Primary screen (LYPLA1 inhibitors in singlicate)
2177Counterscreen for PME1 inhibitors: fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of lysophospholipase 2 (LYPLA2).Screening depositor-specified cross reference: Primary screen (LYPLA2 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: Summary (LYPLA2 inhibitors)
2232Counterscreen for PME1 inhibitors: fluorescence polarization-based biochemical high throughput confirmation assay to identify inhibitors of lysophospholipase 2 (LYPLA2).Screening depositor-specified cross reference: Confirmation screen (LYPLA2 inhibitors in triplicate)
2233Counterscreen for PME1 inhibitors: fluorescence polarization-based biochemical high throughput confirmation assay for inhibitors of lysophospholipase 1 (LYPLA1).Screening depositor-specified cross reference: Confirmation screen (LYPLA1 inhibitors in triplicate)
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 depositor-specified cross reference: Confirmation screen (LYPLA1 and LYPLA2 inhibitors in singlicate)
493108Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: fluorescence-based cell-based inhibitionOther depositor-specified cross reference: Late stage screen (LYPLA1 and LYPLA2 inhibitors in singlicate)
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 depositor-specified cross reference: Late stage LCMS assay (LYPLA1)
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 depositor-specified cross reference: Late stage dose response (LYPLA1 and LYPLA2 inhibitors in triplicate)
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 depositor-specified cross reference: Late stage screen (LYPLA1 and LYPLA2 inhibitors in singlicate)
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 depositor-specified cross reference: Late stage dose response counterscreen (ABHD11 inhibitors in triplicate)
493161Late 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 compoundsConfirmatory depositor-specified cross reference: Late stage dose response counterscreen (T-cell cytotoxicity in quadruplicate)
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: Late stage dose repsonse (ABHD11 inhibitors in triplicate)
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: Late stage MOA assay (ABDH11 LCMS)
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: Late stage screen (ABHD11 inhibitors in singlicate, in situ)
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: Late stage dose response (ABHD11 inhibitors in triplicate)
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: Late stage dose repsonse counterscreen (T-cell cytotoxicity in quadruplicate)
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: Late stage screen (LYPLA1 and LYPLA2 inhibitors in singlicate)
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: Late stage panel screen (ABHD11 SILAC ratio)
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: Late stage counterscreen (ABHD11 inhibitors in singlicate)
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
743137 On Hold
2143Summary of probe development efforts to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).Summary3 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
652003Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: fluorescence-based biochemical dose-response assayConfirmatory same project related to Summary assay
652004Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: fluorescence-based biochemical dose-response assayConfirmatory 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
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
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 same project related to Summary assay
652003Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: fluorescence-based biochemical dose-response assayConfirmatory same project related to Summary assay
652004Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: fluorescence-based biochemical dose-response assayConfirmatory 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
Grant Proposal PI: Benjamin Cravatt, TSRI
External Assay ID: HEK293T_INH_ABS_6XCC50

Name: Late 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 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, selective inhibitors of LYPLA1 or LYPLA2 would greatly aid investigations into the biological function of these 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 high affinity inhibitors, capable of achieving temporal and more complete control over activity, is critical.

References:

1. Dekker, F.J., et al., Small-molecule inhibition of APT1 affects Ras localization and signaling. Nat. Chem. Biol., 2010. 6(6): p. 449-56.
2. Duncan, J.A. and A.G. Gilman, A cytoplasmic acyl-protein thioesterase that removes palmitate from G protein alpha subunits and p21(RAS). J. Biol. Chem., 1998. 273(25): p. 15830-7.
3. Sugimoto, H., H. Hayashi, and S. Yamashita, Purification, cDNA cloning, and regulation of lysophospholipase from rat liver. J. Biol. Chem., 1996. 271(13): p. 7705-11.
4. Toyoda, T., H. Sugimoto, and S. Yamashita, Sequence, expression in Escherichia coli, and characterization of lysophospholipase II. Biochim. Biophys. Acta, 1999. 1437(2): p. 182-93.
5. Biel, M., et al., Synthesis and evaluation of acyl protein thioesterase 1 (APT1) inhibitors. Chemistry, 2006. 12(15): p. 4121-43.
6. Deck, P., et al., Development and biological evaluation of acyl protein thioesterase 1 (APT1) inhibitors. Angew. Chem. Int. Ed. Engl., 2005. 44(31): p. 4975-80.
7. Jessani, N., et al., Enzyme activity profiles of the secreted and membrane proteome that depict cancer cell invasiveness. Proc. Natl. Acad. Sci. U. S. A., 2002. 99(16): p. 10335-40.
8. Leung, D., et al., Discovering potent and selective reversible inhibitors of enzymes in complex proteomes. Nat. Biotechnol., 2003. 21(6): p. 687-91.
9. Bachovchin, D.A., et al., Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes. Nat. Biotechnol., 2009. 27(4): p. 387-94.
10. Forner, F., et al., Quantitative proteomic comparison of rat mitochondria from muscle, heart, and liver. Mol. Cell. Proteomics, 2006. 5(4): p. 608-19.
11. Schubert, C., The genomic basis of the Williams-Beuren syndrome. Cell. Mol. Life Sci., 2009. 66(7): p. 1178-97.

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, protein palmitoylation, counterscreen, dose response, viability, cytotoxicity, CC50, HEK293T cells, WST-1, formazan dye, Scripps, Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN
Panel Information
Assays
PID§NameSubstancePanel TargetsDescription
ActiveInactive
1Serum-free medium4
2Serum-supplemented medium4

§ Panel component ID.
Protocol
Assay Overview:

The purpose of this assay is to determine cytotoxicity of powder samples of test compounds. In this assay, HEK293T cells in either serum-free medium or medium containing fetal calf serum (FCS) 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.

Protocol Summary:

This assay was started by dispensing HEK293T in DMEM medium supplemented with 10% FCS (100 uL, 15,000 cells/well) into a 96-well plate. Cells were incubated for 24 hours at 37 C in a humidified incubator, medium was removed, and 100 uL of fresh, serum-free medium or medium supplemented with 10% FCS was added. Compound (10 uL of 11x stocks in medium containing 10% DMSO) or an equal volume medium containing 10% DMSO only was added to each well. 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. CC50 values were determined from dose-response curves from six replicates at each inhibitor concentration.

The % cell viability for each well was calculated as follows:

%_Cell_Viability = ( ABS_Test_Compound - MedianABS_Low_Control ) / ( MedianABS_High_Control - MedianABS_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).

The CC50 value for each test compound was determined by plotting percent surviving cells against the log of the compound concentration. A three parameter equation describing a sigmoidal dose-response curve was then fitted using GraphPad Prism (GraphPad Software Inc), and the software-generated CC50 values are reported. In the event that the highest test concentration did not result in at least 50% cell death, the CC50 value is reported as being greater than the highest test concentration.

PubChem Activity Outcome and Score:

The following applies to each panel in this assay:

Compounds with CC50 values less than or equal to 10 uM were considered active (cytotoxic). Compounds with CC50 values greater than 10 uM were considered inactive (non-cytotoxic).

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 of the compounds with fitted curves, with the most potent compounds assigned the highest activity scores.

Serum-free Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.
Serum-supplemented Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

Overall Outcome and Score:

Compounds were considered active if they were active in either panel. Compounds were considered inactive if they were inactive in both panel or active in both panels.

The PubChem Activity Score is assigned a value of 100 for active compounds, and 0 for inactive compounds.

The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

List of Reagents:

HEK293T cells (provided by the Assay Provider)
DMEM Medium (CellGro 10-017-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 test compounds.
Categorized Comment
Assay: Dictionary: Version: 0.1

Assay: CurveFit [1]: Equation: =[Baseline Response] + ( [Maximal Response] - [Baseline Response] ) / ( 1 + 10^( ( log( [Concentration] ) - [LogCC50] ) ) )

Assay: CurveFit [2]: Equation: =[Baseline Response] + ( [Maximal Response] - [Baseline Response] ) / ( 1 + 10^( ( log( [Concentration] ) - [LogCC50] ) ) )

Result Definitions
Show more
TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1Outcome [Serum-free]One of Active, Inactive, or Not Tested1Outcome
2Score [Serum-free]The BioAssay Activity Score1Integer
3Qualifier [Serum-free]Qualifier identifies if the resultant CC50 was determined manually to be greater than its listed CC50.1String
4CC50 [Serum-free]*The value for the concentration at which 50% of surviving cells are observed in serum-free medium; CC50 shown in micromolar.1FloatμM
5LogCC50 [Serum-free]log of CC501Float
6Baseline Response [Serum-free]Adjustable baseline of the curve fit, minimal response value.1Float
7Maximal Response [Serum-free]The maximal or asymptotic response above the baseline as concentration increases without bound.1Float
8Surviving Cells at 50 uM [Serum-free] [1] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-free medium; replicate [1]1Float%
9Surviving Cells at 50 uM [Serum-free] [2] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-free medium; replicate [2]1Float%
10Surviving Cells at 50 uM [Serum-free] [3] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-free medium; replicate [3]1Float%
11Surviving Cells at 50 uM [Serum-free] [4] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-free medium; replicate [4]1Float%
12Surviving Cells at 50 uM [Serum-free] [5] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-free medium; replicate [5]1Float%
13Surviving Cells at 50 uM [Serum-free] [6] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-free medium; replicate [6]1Float%
14Surviving Cells at 10 uM [Serum-free] [1] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-free medium; replicate [1]1Float%
15Surviving Cells at 10 uM [Serum-free] [2] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-free medium; replicate [2]1Float%
16Surviving Cells at 10 uM [Serum-free] [3] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-free medium; replicate [3]1Float%
17Surviving Cells at 10 uM [Serum-free] [4] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-free medium; replicate [4]1Float%
18Surviving Cells at 10 uM [Serum-free] [5] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-free medium; replicate [5]1Float%
19Surviving Cells at 10 uM [Serum-free] [6] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-free medium; replicate [6]1Float%
20Surviving Cells at 2 uM [Serum-free] [1] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-free medium; replicate [1]1Float%
21Surviving Cells at 2 uM [Serum-free] [2] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-free medium; replicate [2]1Float%
22Surviving Cells at 2 uM [Serum-free] [3] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-free medium; replicate [3]1Float%
23Surviving Cells at 2 uM [Serum-free] [4] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-free medium; replicate [4]1Float%
24Surviving Cells at 2 uM [Serum-free] [5] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-free medium; replicate [5]1Float%
25Surviving Cells at 2 uM [Serum-free] [6] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-free medium; replicate [6]1Float%
26Surviving Cells at 0.4 uM [Serum-free] [1] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-free medium; replicate [1]1Float%
27Surviving Cells at 0.4 uM [Serum-free] [2] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-free medium; replicate [2]1Float%
28Surviving Cells at 0.4 uM [Serum-free] [3] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-free medium; replicate [3]1Float%
29Surviving Cells at 0.4 uM [Serum-free] [4] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-free medium; replicate [4]1Float%
30Surviving Cells at 0.4 uM [Serum-free] [5] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-free medium; replicate [5]1Float%
31Surviving Cells at 0.4 uM [Serum-free] [6] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-free medium; replicate [6]1Float%
32Surviving Cells at 0.08 uM [Serum-free] [1] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-free medium; replicate [1]1Float%
33Surviving Cells at 0.08 uM [Serum-free] [2] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-free medium; replicate [2]1Float%
34Surviving Cells at 0.08 uM [Serum-free] [3] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-free medium; replicate [3]1Float%
35Surviving Cells at 0.08 uM [Serum-free] [4] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-free medium; replicate [4]1Float%
36Surviving Cells at 0.08 uM [Serum-free] [5] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-free medium; replicate [5]1Float%
37Surviving Cells at 0.08 uM [Serum-free] [6] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-free medium; replicate [6]1Float%
38Surviving Cells at 0.016 uM [Serum-free] [1] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-free medium; replicate [1]1Float%
39Surviving Cells at 0.016 uM [Serum-free] [2] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-free medium; replicate [2]1Float%
40Surviving Cells at 0.016 uM [Serum-free] [3] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-free medium; replicate [3]1Float%
41Surviving Cells at 0.016 uM [Serum-free] [4] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-free medium; replicate [4]1Float%
42Surviving Cells at 0.016 uM [Serum-free] [5] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-free medium; replicate [5]1Float%
43Surviving Cells at 0.016 uM [Serum-free] [6] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-free medium; replicate [6]1Float%
44Surviving Cells at 0.0032 uM [Serum-free] [1] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-free medium; replicate [1]1Float%
45Surviving Cells at 0.0032 uM [Serum-free] [2] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-free medium; replicate [2]1Float%
46Surviving Cells at 0.0032 uM [Serum-free] [3] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-free medium; replicate [3]1Float%
47Surviving Cells at 0.0032 uM [Serum-free] [4] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-free medium; replicate [4]1Float%
48Surviving Cells at 0.0032 uM [Serum-free] [5] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-free medium; replicate [5]1Float%
49Surviving Cells at 0.0032 uM [Serum-free] [6] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-free medium; replicate [6]1Float%
50Outcome [Serum-supplemented]One of Active, Inactive, or Not Tested2Outcome
51Score [Serum-supplemented]The BioAssay Activity Score2Integer
52Qualifier [Serum-supplemented]Qualifier identifies if the resultant CC50 was determined manually to be greater than its listed CC50.2String
53CC50 [Serum-supplemented]*The value for the concentration at which 50% of surviving cells are observed in serum-containing medium; CC50 shown in micromolar.2FloatμM
54LogCC50 [Serum-supplemented]log of CC502Float
55Baseline Response [Serum-supplemented]Adjustable baseline of the curve fit, minimal response value.2Float
56Maximal Response [Serum-supplemented]The maximal or asymptotic response above the baseline as concentration increases without bound.2Float
57Surviving Cells at 50 uM [Serum-supplemented] [1] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-supplemented medium; replicate [1]2Float%
58Surviving Cells at 50 uM [Serum-supplemented] [2] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-supplemented medium; replicate [2]2Float%
59Surviving Cells at 50 uM [Serum-supplemented] [3] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-supplemented medium; replicate [3]2Float%
60Surviving Cells at 50 uM [Serum-supplemented] [4] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-supplemented medium; replicate [4]2Float%
61Surviving Cells at 50 uM [Serum-supplemented] [5] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-supplemented medium; replicate [5]2Float%
62Surviving Cells at 50 uM [Serum-supplemented] [6] (50μM**)Value of % surviving cells at 50 uM compound concentration in serum-supplemented medium; replicate [6]2Float%
63Surviving Cells at 10 uM [Serum-supplemented] [1] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-supplemented medium; replicate [1]2Float%
64Surviving Cells at 10 uM [Serum-supplemented] [2] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-supplemented medium; replicate [2]2Float%
65Surviving Cells at 10 uM [Serum-supplemented] [3] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-supplemented medium; replicate [3]2Float%
66Surviving Cells at 10 uM [Serum-supplemented] [4] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-supplemented medium; replicate [4]2Float%
67Surviving Cells at 10 uM [Serum-supplemented] [5] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-supplemented medium; replicate [5]2Float%
68Surviving Cells at 10 uM [Serum-supplemented] [6] (10μM**)Value of % surviving cells at 10 uM compound concentration in serum-supplemented medium; replicate [6]2Float%
69Surviving Cells at 2 uM [Serum-supplemented] [1] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-supplemented medium; replicate [1]2Float%
70Surviving Cells at 2 uM [Serum-supplemented] [2] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-supplemented medium; replicate [2]2Float%
71Surviving Cells at 2 uM [Serum-supplemented] [3] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-supplemented medium; replicate [3]2Float%
72Surviving Cells at 2 uM [Serum-supplemented] [4] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-supplemented medium; replicate [4]2Float%
73Surviving Cells at 2 uM [Serum-supplemented] [5] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-supplemented medium; replicate [5]2Float%
74Surviving Cells at 2 uM [Serum-supplemented] [6] (2μM**)Value of % surviving cells at 2 uM compound concentration in serum-supplemented medium; replicate [6]2Float%
75Surviving Cells at 0.4 uM [Serum-supplemented] [1] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-supplemented medium; replicate [1]2Float%
76Surviving Cells at 0.4 uM [Serum-supplemented] [2] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-supplemented medium; replicate [2]2Float%
77Surviving Cells at 0.4 uM [Serum-supplemented] [3] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-supplemented medium; replicate [3]2Float%
78Surviving Cells at 0.4 uM [Serum-supplemented] [4] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-supplemented medium; replicate [4]2Float%
79Surviving Cells at 0.4 uM [Serum-supplemented] [5] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-supplemented medium; replicate [5]2Float%
80Surviving Cells at 0.4 uM [Serum-supplemented] [6] (0.4μM**)Value of % surviving cells at 0.4 uM compound concentration in serum-supplemented medium; replicate [6]2Float%
81Surviving Cells at 0.08 uM [Serum-supplemented] [1] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-supplemented medium; replicate [1]2Float%
82Surviving Cells at 0.08 uM [Serum-supplemented] [2] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-supplemented medium; replicate [2]2Float%
83Surviving Cells at 0.08 uM [Serum-supplemented] [3] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-supplemented medium; replicate [3]2Float%
84Surviving Cells at 0.08 uM [Serum-supplemented] [4] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-supplemented medium; replicate [4]2Float%
85Surviving Cells at 0.08 uM [Serum-supplemented] [5] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-supplemented medium; replicate [5]2Float%
86Surviving Cells at 0.08 uM [Serum-supplemented] [6] (0.08μM**)Value of % surviving cells at 0.08 uM compound concentration in serum-supplemented medium; replicate [6]2Float%
87Surviving Cells at 0.016 uM [Serum-supplemented] [1] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-supplemented medium; replicate [1]2Float%
88Surviving Cells at 0.016 uM [Serum-supplemented] [2] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-supplemented medium; replicate [2]2Float%
89Surviving Cells at 0.016 uM [Serum-supplemented] [3] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-supplemented medium; replicate [3]2Float%
90Surviving Cells at 0.016 uM [Serum-supplemented] [4] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-supplemented medium; replicate [4]2Float%
91Surviving Cells at 0.016 uM [Serum-supplemented] [5] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-supplemented medium; replicate [5]2Float%
92Surviving Cells at 0.016 uM [Serum-supplemented] [6] (0.016μM**)Value of % surviving cells at 0.016 uM compound concentration in serum-supplemented medium; replicate [6]2Float%
93Surviving Cells at 0.0032 uM [Serum-supplemented] [1] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-supplemented medium; replicate [1]2Float%
94Surviving Cells at 0.0032 uM [Serum-supplemented] [2] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-supplemented medium; replicate [2]2Float%
95Surviving Cells at 0.0032 uM [Serum-supplemented] [3] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-supplemented medium; replicate [3]2Float%
96Surviving Cells at 0.0032 uM [Serum-supplemented] [4] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-supplemented medium; replicate [4]2Float%
97Surviving Cells at 0.0032 uM [Serum-supplemented] [5] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-supplemented medium; replicate [5]2Float%
98Surviving Cells at 0.0032 uM [Serum-supplemented] [6] (0.0032μM**)Value of % surviving cells at 0.0032 uM compound concentration in serum-supplemented medium; replicate [6]2Float%

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

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