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BioAssay: AID 588807

Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition and selectivity in a complex proteome for ABHD10

Name: Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition and selectivity in a complex proteome for ABHD10. ..more
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 Tested Compounds
 Tested Compounds
All(43)
 
 
Active(12)
 
 
Inactive(31)
 
 
 Tested Substances
 Tested Substances
All(43)
 
 
Active(12)
 
 
Inactive(31)
 
 
AID: 588807
Data Source: The Scripps Research Institute Molecular Screening Center (ABHD10_INH_FLUO_GELBASEDABPP_SEL)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
BioAssay Version:
Deposit Date: 2011-11-17
Hold-until Date: 2012-05-31
Modify Date: 2012-05-31

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 12
Related Experiments
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AIDNameTypeProbeComment
2130Fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).Screening depositor-specified cross reference: Primary screen (PME-1 inhibitors)
2143Summary of probe development efforts to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).Summary3 depositor-specified cross reference: Summary (PME-1 inhibitors)
2171Fluorescence polarization-based biochemical high throughput confirmation assay for inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).Screening depositor-specified cross reference: Confirmation assay (PME-1 inhibitors)
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)
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: Counterscreen (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: Counterscreen confirmation (LYPLA2 inhibitors)
2233Counterscreen for PME1 inhibitors: fluorescence polarization-based biochemical high throughput confirmation assay for inhibitors of lysophospholipase 1 (LYPLA1).Screening depositor-specified cross reference: Counterscreen confirmation (LYPLA1 inhibitors)
2291Fluorescence polarization-based Maybridge primary biochemical high throughput screening assay to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).Screening depositor-specified cross reference: Primary screen (PME-1 inhibitors, Maybridge Library)
2363Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Inhibition of PME-1-mediated demethylation of PP2aScreening depositor-specified cross reference: MOA assay (Demethylation of PP2a)
2365Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Luminescence-based counterscreen assay to identify cytotoxic compoundsConfirmatory depositor-specified cross reference: Counterscreen (Cytotoxicity HEC 293T)
2366Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Gel-based Activity-Based Protein Profiling (ABPP) IC50Confirmatory depositor-specified cross reference: ABPP dose response screen (PME-1 inhibitors)
2368Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Gel-based Activity-Based Protein Profiling (ABPP) Gel Filtration AssayScreening depositor-specified cross reference: MOA assay (PME-1 inhibitors, gel filtration assay)
2369Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Gel-based Activity-Based Protein Profiling (ABPP) InhibitionScreening depositor-specified cross reference: ABPP screen (PME-1 inhibitors)
2371Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Gel-based Activity-Based Protein Profiling (ABPP) IC50: Purified enzymeConfirmatory depositor-specified cross reference: ABPP dose response screen (PME-1 inhibitors, purified enzyme)
463090Late stage assay provider results from the probe development effort to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1): LC-MS/MS assay to assess binding of compounds to active siteOther depositor-specified cross reference: MOA assay (PME-1 inhibitors, LC-MS assay)
463091Late stage assay provider results from the probe development effort to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1): luminescence-based biochemical dose response assay to determine cytotoxicity of inhibitor compoundsConfirmatory depositor-specified cross reference: Counterscreen (Cytotoxicity HeLa)
463124Late stage assay provider results from the probe development effort to identify inhibitors of protein phosphatase methylesterase 1 (PME-1): Gel-based Activity-Based Protein Profiling (ABPP) IC50 Set 2Confirmatory depositor-specified cross reference: ABPP profiling dose response (PME1 inhibitors in triplicate)
463130Late stage assay provider results from the probe development effort to identify inhibitors of protein phosphatase methylesterase 1 (PME-1): Gel-based Activity-Based Protein Profiling (ABPP) IC50 Set 1Confirmatory depositor-specified cross reference: ABPP profiling dose response (PME1 inhibitors in triplicate)
463131Late stage assay provider results from the probe development effort to identify inhibitors of protein phosphatase methylesterase 1 (PME-1): fluorescence-based cell-based inhibitionScreening depositor-specified cross reference: ABPP profiling (PME1 inhibitors in singlicate)
463132Late stage assay provider results from the probe development effort to identify inhibitors of protein phosphatase methylesterase 1 (PME-1): Inhibition of PME-1-mediated demethylation of PP2AScreening depositor-specified cross reference: MOA assay (PP2a demethylation)
463146Late stage assay provider results from the probe development effort to identify inhibitors of protein phosphatase methylesterase 1 (PME-1): Fluorescence-based biochemical gel-based ABPPOther depositor-specified cross reference: ABPP profiling (PME1 inhibitors in singlicate)
463149Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: Fluorescence-based biochemical gel-based ABPP inhibition and selectivityOther depositor-specified cross reference: ABPP profiling (PME1 inhibition and selectivity in singlicate)
588835Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: fluorescence-based dose response cell-based gel-based competitive Activity-Based Protein Profiling (ABPP) ABHD10 selectivity assayOther depositor-specified cross reference
602468Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition and selectivity among cysteine-reactive proteinsOther depositor-specified cross reference
602485Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: fluorescence-based cell-based gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of ABHD10 in vivoOther depositor-specified cross reference
2202Summary of probe development efforts to identify inhibitors of lysophospholipase 1 (LYPLA1).Summary2 same project related to Summary assay
2203Summary of probe development efforts to identify inhibitors of lysophospholipase 2 (LYPLA2).Summary1 same project related to Summary assay
588796Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: fluorescence-based dose response biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of ABHD10 Set 2Confirmatory same project related to Summary assay
588801Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: fluorescence-based dose response cell-based gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of ABHD10Confirmatory same project related to Summary assay
588802Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: fluorescence-based dose response biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of ABHD10 Set 1Confirmatory same project related to Summary assay
588803Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: LC-MS/MS-based cell-based ABPP-SILAC assayOther1 same project related to Summary assay
588804Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compoundsConfirmatory same project related to Summary assay
588805Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: ABHD10 inhibitor LC-MS/MS-based cell-based ABPP-SILAC assayOther same project related to Summary assay
588806Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: fluorescence-based cell-based gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of ABHD10Other 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: ABHD10_INH_FLUO_GELBASEDABPP_SEL

Name: Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition and selectivity in a complex proteome for ABHD10.

Description:

Protein phosphatase methylesterase-1 (PME-1)-mediated methylesterification is thought to control the binding of different subunits to protein phosphatase 2A (PP2A) (1), which, along with protein phosphatase 1 (PP1), is responsible for > 90% of all serine/threonine phosphatase activity (2). PME-1 has also been identified as a protector of sustained ERK pathway activity in malignant gliomas (3), suggesting a link between cancer progression and PME-1-regulated methylesterification. A fluorescence-polarization activity-based protein profiling (fluopol-ABPP) HTS assay for PME-1 inhibitor discovery (AIDs 2130 and 2171) unveiled a phenomenal class of potent and selective inhibitors, the aza-beta lactams (ABLs). During medicinal chemistry campaign to refine ABL inhibitors for PME-1 (See Probe Report for ML174 on the NCBI bookshelf http://www.ncbi.nlm.nih.gov/books/NBK47352/), we observed that one of the common anti-targets of several ABL members was the uncharacterized serine hydrolase abhydrolase domain containing protein 10 (ABHD10). We have preliminary evidence that ABHD10 functions as a lipase in situ (unpublished); however is physiological substrates and biological role(s) have not yet been explored. A principle goal of post-genomic research is to elucidate the molecular and cellular roles of uncharacterized enzymes like ABHD10, work that requires selective chemical tools to inactivate enzyme activity in a controlled manner.


References:

1. Wu, J., Tolstykh, T., Lee, J., Boyd, K., Stock, J. B., Broach, J. R. (2000). Carboxyl methylation of the phosphoprotein phosphatase 2A catalytic subunit promotes its functional association with regulatory subunits in vivo. Embo J. 19, 5672-5681.
2. Oliver, C. J., Shenolikar, S. (1998). Physiologic importance of protein phosphatase inhibitors. Front. Biosci. 3, D961-972.
3. Puustinen, P., Junttila, M. R., Vanhatupa, S., Sablina, A. A., Hector, M. E., Teittinen, K., Raheem, O., Ketola, K., Lin, S., Kast, J., Haapasalo, H., Hahn, W. C., Westermarck, J. (2009). PME-1 protects extracellular signal-regulated kinase pathway activity from protein phosphatase 2A-mediated inactivation in human malignant glioma. Cancer Res. 69, 2870-2877.

Keywords:

late stage, late stage AID, assay provider, powders, abhdyrolase domain containing protein 10, ABHD10, uncharacterized, PME-1, protein phosphatase methylesterase 1, PPME-1, counterscreen, anti-targets, acylpeptide hydrolase, Apeh, prolyl endopeptidase, Prep, arylacetamide deacetylase-like 1, Kiaa1363, monoacylglycerol lipase, Magl, abhydrolase domain containing protein 6 Abhd6, activity-based protein profiling, ABPP, gel-based, fluorophosphonate rhodamine, FP-Rh, inhibitor, selectivity, Scripps, Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN
Panel Information
Targets
    Data Table(Active)    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1Abhd101231abhydrolase domain-containing protein 10, mitochondrial precursor [Mus musculus] [gi:269784760]
Taxonomy id: 10090
Gene id: 213012
2Anti-Target APEH43Carboxylesterase 1 (monocyte/macrophage serine esterase 1) [Homo sapiens] [gi:82571745]
Taxonomy id: 10090
Gene id: 235606
3Anti-Target PREP43prolyl endopeptidase [Mus musculus] [gi:6755152]
Taxonomy id: 10090
Gene id: 19072
4Anti-Target Kiaa136343neutral cholesterol ester hydrolase 1 [Mus musculus] [gi:30520239]
Taxonomy id: 10090
Gene id: 320024
5Anti-Target Magl43monoglyceride lipase isoform d [Mus musculus] [gi:261878511]
Taxonomy id: 10090
Gene id: 23945
6Anti-Target ABHD643monoacylglycerol lipase ABHD6 [Mus musculus] [gi:31560264]
Taxonomy id: 10090
Gene id: 66082

§ Panel component ID.
Protocol
Assay Overview:
The purpose of this assay is to determine whether powder samples of test compounds can inhibit ABHD10 in a complex proteomic lysate and to estimate compound selectivity using an activity-based proteomic profiling (ABPP) assay. In this assay, a complex proteome is incubated with test compound followed by reaction with a rhodamine-conjugated fluorophosphonate (FP-Rh) activity-based probe. The reaction products are separated by SDS-PAGE and visualized in-gel using a flatbed fluorescence scanner. The percentage activity remaining is determined by measuring the integrated optical density (IOD) of the bands. As designed, test compounds that act as ABHD10 inhibitors will prevent enzyme-probe interactions, thereby decreasing the proportion of bound fluorescent probe, giving lower fluorescence intensity in the band in the gel. Percent inhibition is calculated relative to a DMSO (no compound) control.
Protocol Summary:
Mouse brain membrane proteome (1 mg/mL in DPBS; 50 uL reaction volume) was treated with 10 uM, 1 uM or 0.1 uM test compound (1 uL of a 50x stock in DMSO). Test compounds were incubated for 30 minutes at 37 C, and FP-Rh (1 uL of 50x stock in DMSO) was added to a final concentration of 1 uM. The reaction was incubated for 30 minutes at 25 C, quenched with 4x SDS-PAGE loading buffer, separated by SDS-PAGE and visualized by in-gel fluorescent scanning. The percentage activity remaining was determined by measuring the integrated optical density of the target (ABHD10) and anti-target (acylpeptide hydrolase [APEH], prolyl endopeptidase [PREP], arylacetamide deacetylase-like 1 [KIAA1363], monoacylglycerol lipase [MAGL], and abhydrolase domain containing protein 6 [ABHD6]) bands relative to a DMSO-only (no compound) control.
The % inhibition was then calculated as follows:
%_Inhibition = ( 1 - ( IOD_Test_Compound - Median_IOD_Low_Control ) / ( Median_IOD_High_Control - Median_IOD_Low_Control ) ) * 100
Where:
Test_Compound is defined as target or anti-target treated with test compound.
High_Control is defined as target or anti-target treated with DMSO only (no compound).
Low_Control is defined as background in a blank region of the gel.
Fold_selectivity > [Conc_<50%_INH_Anti-target] / [Conc_>=50%_INH_target]
Where:
[Conc_<50%_INH_Anti-target] is the test compound concentration at which less than 50% inhibition of the anti-target is observed.
[Conc_>=50%_INH_target] is the test compound concentration at which greater than or equal to 50% inhibition of target is observed.
If [Conc_>=50%_INH_target] is not determined, then Fold Selectivity is not determined.
If [Conc_<50%_INH_Anti-target] < [Conc_>=50%_INH_target], Fold Selectivity is 0.
PubChem Activity Outcome and Score:
The following applies to each panel in this assay:
Compounds with greater than or equal to 50% inhibition at 0.1 uM test compound concentration were considered active. Compounds with less than 50% inhibition at 0.1 uM test compound concentration were considered inactive.
The reported PubChem Activity Score has been normalized to 100% of the observed value at 0.1 uM.
ABHD10 Score: The PubChem Activity Score range for active compounds is 100-57, and for inactive compounds 47-0.
APEH Score: The PubChem Activity Score range for inactive compounds is 100-0. There are no active compounds.
PREP Score: The PubChem Activity Score range for inactive compounds is 100-0. There are no active compounds.
KIAA1363 Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.
MAGL Score: The PubChem Activity Score range for inactive compounds is 100-0. There are no active compounds.
ABHD6 Score: The PubChem Activity Score range for inactive compounds is 100-0. There are no active compounds.
Overall Outcome and Score:
Compounds with greater than or equal to 50% inhibition of ABHD10 at 0.1 uM test compound concentration and 10-fold or greater selectivity against all anti-targets were considered active. Compounds with less than 50% inhibition at 0.1 uM test compound concentration and/or less than 10-fold selectivity against all anti-targets were considered inactive.
The PubChem Activity Score is assigned a value of 100 for active compounds, and 0 for inactive compounds.
The PubChem Activity Score range for active compounds is 100-100, and for inactive compounds 0-0.
List of Reagents:
Mouse brain membrane proteome (provided by Assay Provider)
FP-Rh (provided by the Assay Provider)
DPBS (Cellgro 20-031-CV)
Comment
This assay was performed by the assay provider with powder samples of synthetic compounds.
Categorized Comment - additional comments and annotations
From BioAssay Depositor:
BAO: assay format: biochemical format: protein format: protein complex format
BAO: bioassay specification: assay biosafety level: bsl1
BAO: bioassay specification: assay measurement type: endpoint assay
BAO: bioassay specification: assay readout content: assay readout method: regular screening
BAO: bioassay specification: assay readout content: content readout type: single readout
BAO: bioassay specification: assay stage: secondary: selectivity
BAO: detection technology: fluorescence: fluorescence intensity
BAO: meta target detail: binding reporter specification: interaction: protein-small molecule
BAO: meta target: molecular target: protein target: enzyme: generic hydrolase
BAO: version: 1.4b1090
From PubChem:
Assay Format: Biochemical
Result Definitions
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TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1Outcome [ABHD10]One of Active, Inactive, or Not Tested1abhydrolase domain-containing protein 10, mitochondrial precursor [Mus musculus]Outcome
2Score [ABHD10]The BioAssay activity ranking score1Integer
3Inhibition at 10 uM [ABHD10] (10μM**)Inhibition of endogenous mouse ABHD10 upon 10 uM compound treatment as assessed by gel-based competitive ABPP.1Integer%
4Inhibition at 1 uM [ABHD10] (1μM**)Inhibition of endogenous mouse ABHD10 upon 1 uM compound treatment as assessed by gel-based competitive ABPP.1Integer%
5Inhibition at 0.1 uM [ABHD10] (0.1μM**)Inhibition of endogenous mouse ABHD10 upon 0.1 uM compound treatment as assessed by gel-based competitive ABPP.1Integer%
6Outcome [APEH]One of Active, Inactive, or Not Tested2Carboxylesterase 1 (monocyte/macrophage serine esterase 1) [Homo sapiens]Outcome
7Score [APEH]The BioAssay activity ranking score2Integer
8Inhibition at 10 uM [APEH] (10μM**)Inhibition of endogenous mouse APEH upon 10 uM compound treatment as assessed by gel-based competitive ABPP.2Integer%
9Inhibition at 1 uM [APEH] (1μM**)Inhibition of endogenous mouse APEH upon 1 uM compound treatment as assessed by gel-based competitive ABPP.2Integer%
10Inhibition at 0.1 uM [APEH] (0.1μM**)Inhibition of endogenous mouse APEH upon 0.1 uM compound treatment as assessed by gel-based competitive ABPP.2Integer%
11Qualifier [APEH]Qualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity.2String
12Fold Selectivity [APEH]The ratio of the test compound concentration at which less than 50% inhibition of the anti-target APEH is observed over the test compound concentration at which greater than or equal to 50% inhibition of ABHD10 is observed.2Integerratio
13Outcome [PREP]One of Active, Inactive, or Not Tested3prolyl endopeptidase [Mus musculus]Outcome
14Score [PREP]The BioAssay activity ranking score3Integer
15Inhibition at 10 uM [PREP] (10μM**)Inhibition of endogenous mouse PREP upon 10 uM compound treatment as assessed by gel-based competitive ABPP.3Integer%
16Inhibition at 1 uM [PREP] (1μM**)Inhibition of endogenous mouse PREP upon 1 uM compound treatment as assessed by gel-based competitive ABPP.3Integer%
17Inhibition at 0.1 uM [PREP] (0.1μM**)Inhibition of endogenous mouse PREP upon 0.1 uM compound treatment as assessed by gel-based competitive ABPP.3Integer%
18Qualifier [PREP]Qualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity.3String
19Fold Selectivity [PREP]The ratio of the test compound concentration at which less than 50% inhibition of the anti-target PREP is observed over the test compound concentration at which greater than or equal to 50% inhibition of ABHD10 is observed.3Integerratio
20Outcome [KIAA1363]One of Active, Inactive, or Not Tested4neutral cholesterol ester hydrolase 1 [Mus musculus]Outcome
21Score [KIAA1363]The BioAssay activity ranking score4Integer
22Inhibition at 10 uM [KIAA1363] (10μM**)Inhibition of endogenous mouse KIAA1363 upon 10 uM compound treatment as assessed by gel-based competitive ABPP.4Integer%
23Inhibition at 1 uM [KIAA1363] (1μM**)Inhibition of endogenous mouse KIAA1363 upon 1 uM compound treatment as assessed by gel-based competitive ABPP.4Integer%
24Inhibition at 0.1 uM [KIAA1363] (0.1μM**)Inhibition of endogenous mouse KIAA1363 upon 0.1 uM compound treatment as assessed by gel-based competitive ABPP.4Integer%
25Qualifier [KIAA1363]Qualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity.4String
26Fold Selectivity [KIAA1363]The ratio of the test compound concentration at which less than 50% inhibition of the anti-target KIAA1363 is observed over the test compound concentration at which greater than or equal to 50% inhibition of ABHD10 is observed.4Integerratio
27Outcome [MAGL]One of Active, Inactive, or Not Tested5monoglyceride lipase isoform d [Mus musculus]Outcome
28Score [MAGL]The BioAssay activity ranking score5Integer
29Inhibition at 10 uM [MAGL] (10μM**)Inhibition of endogenous mouse MAGL upon 10 uM compound treatment as assessed by gel-based competitive ABPP.5Integer%
30Inhibition at 1 uM [MAGL] (1μM**)Inhibition of endogenous mouse MAGL upon 1 uM compound treatment as assessed by gel-based competitive ABPP.5Integer%
31Inhibition at 0.1 uM [MAGL] (0.1μM**)Inhibition of endogenous mouse MAGL upon 0.1 uM compound treatment as assessed by gel-based competitive ABPP.5Integer%
32Qualifier [MAGL]Qualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity.5String
33Fold Selectivity [MAGL]The ratio of the test compound concentration at which less than 50% inhibition of the anti-target MAGL is observed over the test compound concentration at which greater than or equal to 50% inhibition of ABHD10 is observed.5Integerratio
34Outcome [ABHD6]One of Active, Inactive, or Not Tested6monoacylglycerol lipase ABHD6 [Mus musculus]Outcome
35Score [ABHD6]The BioAssay activity ranking score6Integer
36Inhibition at 10 uM [ABHD6] (10μM**)Inhibition of endogenous mouse ABHD6 upon 10 uM compound treatment as assessed by gel-based competitive ABPP.6Integer%
37Inhibition at 1 uM [ABHD6] (1μM**)Inhibition of endogenous mouse ABHD6 upon 1 uM compound treatment as assessed by gel-based competitive ABPP.6Integer%
38Inhibition at 0.1 uM [ABHD6] (0.1μM**)Inhibition of endogenous mouse ABHD6 upon 0.1 uM compound treatment as assessed by gel-based competitive ABPP.6Integer%
39Qualifier [ABHD6]Qualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity.6String
40Fold Selectivity [ABHD6]The ratio of the test compound concentration at which less than 50% inhibition of the anti-target ABHD6 is observed over the test compound concentration at which greater than or equal to 50% inhibition of ABHD10 is observed.6Integerratio
41Anti-target Count at 10 uMThe total number of observed anti-targets with greater than or equal to 50% inhibition at 10 uM test compound concentration as assessed by gel-based ABPPInteger
42Anti-target Count at 1 uMThe total number of observed anti-targets with greater than or equal to 50% inhibition at 1 uM test compound concentration as assessed by gel-based ABPPInteger
43Anti-target Count at 0.1 uMThe total number of observed anti-targets with greater than or equal to 50% inhibition at 0.1 uM test compound concentration as assessed by gel-based ABPPInteger
44QualifierQualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity.String
45Overall Fold SelectivityThe smallest ratio of the test compound concentration at which less than 50% inhibition of the anti-target (as calcuated for APEH, PREP, KIAA1363, MAGL, and ABHD6) is observed over the test compound concentration at which greater than or equal to 50% inhibition of ABHD10 is observed.Integerratio

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

Classification
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