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BioAssay: AID 602355

Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of serine hydrolases in vitro

Name: Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of serine hydrolases in vitro. ..more
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 Tested Compounds
 Tested Compounds
All(3)
 
 
Active(3)
 
 
 Tested Substances
 Tested Substances
All(3)
 
 
Active(3)
 
 
AID: 602355
Data Source: The Scripps Research Institute Molecular Screening Center (DAGLB_INH_FLUO_1X%INH_SH_SEL)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
Deposit Date: 2012-03-09
Hold-until Date: 2013-03-07
Modify Date: 2013-03-07

Data Table ( Complete ):           Active    All
BioActive Compounds: 3
Depositor Specified Assays
Show more
AIDNameTypeProbeComment
504411Fluorescence-based primary biochemical high throughput screening assay to identify inhibitors of human diacylglycerol lipase, beta (DAGLB)screening Primary screen (DAGLB inhibitors in singlicate)
504420Summary of the probe development efforts to identify inhibitors of human diacylglycerol lipase, beta (DAGLB)summary3 Summary (DAGLB inhibitors)
504445Fluorescence-based biochemical high throughput confirmation assay for inhibitors of human diacylglycerol lipase, beta (DAGLB)screening ABPP screen (DAGLB inhibitors in triplicate)
602403Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of recombinant antitarget DAGLa in vitroother
602415Assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): LC/MS-based biochemical inhibition of overexpressed DAGLb substrate turnover in vitroother
624039Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based dose-response biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of antitarget ABHD6 in vitro, set 2confirmatory
624041Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of mouse liver ABHD6 in vivoother
624077Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of mouse liver ABHD6 in vivo upon oral compound administrationother
624468Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): LCMS-based biochemical dose response assayconfirmatory
624472Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of DAGLb by enantiomers of KT116other
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC)
Affiliation: The Scripps Research Institute, TSRI
Assay Provider: Benjamin Cravatt, The Scripps Research Institute (TSRI)
Network: Molecular Library Probe Production Centers Network (MLPCN)
Grant Proposal Number: 1 R01 DA025285
Grant Proposal PI: Benjamin Cravatt, The Scripps Research Institute (TSRI)
External Assay ID: DAGLB_INH_FLUO_1X%INH_SH_SEL

Name: Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of serine hydrolases in vitro.

Description:

Endocannabinoids (ECs) represent a unique group of lipids that function as chemical messengers in the nervous system. To date, the two principle ECs identified in mammals are N-arachidonoyl-ethanolamine (anandamide) and 2-arachidonoyl-glycerol (2-AG). They have been implicated in various physiological and pathological functions including appetite, pain, sensation, memory, and addiction (1). Unlike traditional neurotransmitters, which are stored in vesicles, ECs are synthesized and released on demand, and then rapidly degraded to terminate signaling. Thus, the metabolic pathways that govern EC turnover are critical in determining the magnitude and duration of neuronal signaling events (2). Endocannabinoid biosynthesis, in contrast to degradation, is poorly understood. Recently, two serine hydrolases, DAGL-a and DAGL-B, were cloned and found to selectively cleave sn-1 acyl chains from diacylglycerols (DAG) to generate 2-AG in vitro (3). Their function in the nervous system was validated in vivo by the generation of DAGL-a and DAGL-B knock-out mice (4, 5). However, it is still unclear to what extent DAGL-a/B catalytic activity contributes to 2-AG-mediated signaling. The development of potent and selective inhibitors would offer a means to perturb DAGL-a/B activity in a selective, reversible, and temporally-controlled manner. Given the non-selective nature of current DAGL-a/B inhibitors (6), specific chemical probes would serve as invaluable tools to delineate DAGL-a/B function in 2-AG signaling networks of the brain.

References:

1. Di Marzo, V. (2008) Targeting the endocannabinoid system: to enhance or reduce?, Nat Rev Drug Discov 7, 438-455.
2. Ahn, K., McKinney, M. K., and Cravatt, B. F. (2008) Enzymatic pathways that regulate endocannabinoid signaling in the nervous system, Chem Rev 108, 1687-1707.
3. Bisogno, T., Howell, F., Williams, G., Minassi, A., Cascio, M. G., Ligresti, A., Matias, I., Schiano-Moriello, A., Paul, P., Williams, E. J., Gangadharan, U., Hobbs, C., Di Marzo, V., and Doherty, P. (2003) Cloning of the first sn1-DAG lipases points to the spatial and temporal regulation of endocannabinoid signaling in the brain, J Cell Biol 163, 463-468.
4. Gao, Y., Vasilyev, D. V., Goncalves, M. B., Howell, F. V., Hobbs, C., Reisenberg, M., Shen, R., Zhang, M. Y., Strassle, B. W., Lu, P., Mark, L., Piesla, M. J., Deng, K., Kouranova, E. V., Ring, R. H., Whiteside, G. T., Bates, B., Walsh, F. S., Williams, G., Pangalos, M. N., Samad, T. A., and Doherty, P. (2010) Loss of Retrograde Endocannabinoid Signaling and Reduced Adult Neurogenesis in Diacylglycerol Lipase Knock-out Mice, J Neurosci 30, 2017-2024.
5. Tanimura, A., Yamazaki, M., Hashimotodani, Y., Uchigashima, M., Kawata, S., Abe, M., Kita, Y., Hashimoto, K., Shimizu, T., Watanabe, M., Sakimura, K., and Kano, M. (2010) The Endocannabinoid 2-Arachidonoylglycerol Produced by Diacylglycerol Lipase +/- Mediates Retrograde Suppression of Synaptic Transmission, Neuron 65, 320-327.
6. Hoover, H. S., Blankman, J. L., Niessen, S., and Cravatt, B. F. (2008) Selectivity of inhibitors of endocannabinoid biosynthesis evaluated by activity-based protein profiling, Bioorganic & Medicinal Chemistry Letters 18, 5838-5841.

Keywords:

late stage, late stage AID, assay provider, powders, counterscreen, diacylglycerol lipase, diacylglycerol lipase-beta, DAGL, DAGL-beta, DAGLB, hydrolase, serine hydrolase, appetite, pain, sensation, memory, addiction, activity-based protein profiling, ABPP, gel-based, activity-based probe, fluorophosphonate-rhodamine, FP-Rh, inhibitor, inhibition, serine hydrolases, mouse brain membrane, abhydrolase domain containing protein 11, ABHD11, platelet-activating factor acetylhydrolase 2, PAFAH2, Fatty acid amide hydrolase, FAAH, monoglyceride lipase, MAGL, abhydrolase domain containing protein 6, ABHD6, abhydrolase domain containing protein 12, ABHD12, lysophospholipase 1, LYPLA1, lysophospholipase 2, LYPLA2, phospholipase A2 group VII, PLA2G7, patatin-like phospholipase domain containing 6, PNPLA6, 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
1DAGLb11sn1-specific diacylglycerol lipase beta [Mus musculus] [gi:31559956]
Taxonomy id: 10090
Gene id: 231871
2ABHD113Abhydrolase domain containing 11 [Mus musculus] [gi:47682716]
Taxonomy id: 10090
Gene id: 68758
3PLA2G711platelet-activating factor acetylhydrolase precursor [Mus musculus] [gi:31980752]
Taxonomy id: 10090
Gene id: 27226
4PAFAH22platelet-activating factor acetylhydrolase 2, cytoplasmic [Mus musculus] [gi:225579137]
Taxonomy id: 10090
Gene id: 100163
5FAAH3fatty acid amide hydrolase [Mus musculus] [gi:123253900]
Taxonomy id: 10090
Gene id: 14073
6MAGL3monoacylglycerol lipase ABHD12 [Mus musculus] [gi:159110817]
Taxonomy id: 10090
Gene id: 23945
7ABHD123monoacylglycerol lipase ABHD12 [Mus musculus] [gi:159110817]
Taxonomy id: 10090
Gene id: 76192
8ABHD63monoacylglycerol lipase ABHD6 [Mus musculus] [gi:31560264]
Taxonomy id: 10090
Gene id: 66082
9LYPLA23acyl-protein thioesterase 2 [Mus musculus] [gi:7242156]
Taxonomy id: 10090
Gene id: 26394
10LYPLA13acyl-protein thioesterase 1 [Mus musculus] [gi:6678760]
Taxonomy id: 10090
Gene id: 18777
11PNPLA61neuropathy target esterase [Mus musculus] [gi:170763472]
Taxonomy id: 10090
Gene id: 50767

§ Panel component ID.
Protocol
Assay Overview:

The purpose of this assay is to assay test compound inhibition of serine hydroases (SHs) in a complex proteome using a gel-based competitive activity-based proteomic profiling (ABPP) assay. In this assay, a complex proteome is incubated with test compound followed by reaction with a fluorescently-labeled serine hydrolase-specific activity-based probe, fluorophosphonate-rhodamine (FP-Rh) or the fluorescently-labeled activity-based probe HT-01, which labels a handful of SHs. 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 SH inhibitors will prevent enzyme-probe interactions, thereby decreasing the proportion of bound fluorescent probe, giving lower fluorescence intensity in the band in the gel.

Protocol Summary:

The following proteome sources, prepared in Dulbecco's PBS (DPBS), were used:

1. Diacylglycerol lipase, beta (DAGLb): Membrane proteome of transiently transfected 293T Hek cells overexpressing mouse DAGLb (25 uL of 0.3 mg/mL).
2. Abhydrolase domain containing protein 11 (ABHD11): recombinant mouse ABHD11 (0.050 uM) doped into membrane proteome of 293T Hek cells (0.3 mg/mL).
3. Platelet-activating factor acetylhydrolase 2 (PAFAH2): Soluble proteome (1 mg/mL) of BW5147-derived murine T-cells.
4. Fatty acid amide hydrolase (FAAH), monoglyceride lipase (MAGL), abhydrolase domain containing protein 6 (ABHD6), abhydrolase domain containing protein 12 (ABHD12), lysophospholipase 1 (LYPLA1), lysophospholipase 2 (LYPLA2), phospholipase A2, group VII (PLA2G7), patatin-like phospholipase domain containing 6 (PNPLA6): Mouse brain membrane proteome (1 mg/mL).

Proteome (25 uL) was treated with test compound (0.5 uL of a 50x stock in DMSO, 10, 2, 0.4, 0.08, 0.016, or 0.003 uM final concentration) or DMSO (0.5 uL) for 30 minutes at 37 C. The activity-based probe FP-Rh (0.5 uL of a 50x stock in DMSO; 1 uM final concentration) or HT-01 (0.5 uL of a 50x stock in DMSO; 1 uM final concentration) was added. HT-01 was utilized to detect DAGLb and PLA2G7, for all other proteins, FP-Rh was used. The reaction was incubated for 30 minutes at 37 C, quenched with an equal volume of 2x SDS-PAGE loading buffer (reducing), separated by SDS-PAGE, and visualized by in-gel fluorescent scanning. The percentage activity remaining for each SH was determined by measuring the integrated optical density of the individual protein bands relative to the DMSO-only (no compound) control.

The percent inhibition for each compound was 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 SH treated with test compound.
High_Control is defined as SH treated with DMSO only (no compound).
Low_Control is defined as background in a blank region of the gel.

PubChem Activity Outcome and Score:

The following applies to each panel in this assay:

Compounds with greater than or equal to 50% inhibition for a given SH at 2 uM test compound concentration were considered active. Compounds with less than 50% inhibition for a given SH at 2 uM test compound concentration were considered inactive.

The reported PubChem Activity Score has been normalized to 100% of the observed value at 2 nM.

DAGLb Score: The PubChem Activity Score range for active compounds is 100-100, and for inactive compounds 0-0.

ABHD11 Score: The PubChem Activity Score range for inactive compounds is 0-0. There are no active compounds.

PLA2G7 Score: The PubChem Activity Score range for active compounds is 100-100, and for inactive compounds 0-0.

PAFAH2 Score: The PubChem Activity Score range for inactive compounds 0-0. There are no active compounds.

FAAH Score: The PubChem Activity Score range for inactive compounds 100-0. There are no active compounds.

MAGL Score: The PubChem Activity Score range for inactive compounds 100-0. There are no active compounds.

ABHD12 Score: The PubChem Activity Score range for inactive compounds 0-0. There are no active compounds.

ABHD6 Score: The PubChem Activity Score range for active compounds 100-100. There are no inactive compounds.

LYPLA2 Score: The PubChem Activity Score range for inactive compounds 0-0. There are no active compounds.

LYPLA1 Score: The PubChem Activity Score range for inactive compounds 0-0. There are no active compounds.

PNPLA6 Score: The PubChem Activity Score range for inactive compounds 100-100. There are no active compounds.

Overall Outcome and Score:

Compounds active against at least one SH were considered active. Compounds inactive against all SHs 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:

293T Hek cells overexpressing mouse DAGLb (Open Biosystems Accession BC016105; provided by Assay Provider)
Recombinant mouse ABHD11 (Open Biosystems Accession BC069866; provided by assay provider)
BW5147-derived murine T-cells (provided by assay provider)
Mouse brain membrane proteome (provided by Assay Provider)
HT-01 (provided by Assay Provider)
FP-Rh (provided by Assay Provider)
DPBS (Cellgro 20-031-CV)
Comment
This assay was performed by the assay provider with powder samples of synthetic compounds.
Categorized Comment
BAO: version: 1.4b1090

BAO: bioassay specification: assay stage: secondary: counter screening

BAO: bioassay specification: assay biosafety level: bsl1

BAO: assay format: biochemical format: protein format: single protein format

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: meta target: molecular target: protein target: enzyme: generic hydrolase

BAO: meta target: biological process target: regulation of molecular function

BAO: meta target detail: binding reporter specification: interaction: protein-small molecule

BAO: detection technology: fluorescence: fluorescence intensity

Result Definitions
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TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
ScoreThe BioAssay activity ranking scoreInteger
1Outcome [DAGLb]One of Active, Inactive, or Not Tested1sn1-specific diacylglycerol lipase beta [Mus musculus]Outcome
2Score [DAGLb]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)1Integer
3Inhibition at 10 uM [DAGLb] (10μM**)Percent Inhibition of overexpressed mouse DAGLb upon 10 uM compound treatment as assessed by gel-based competitive ABPP.1Integer%
4Inhibition at 2 uM [DAGLb] (2μM**)Percent Inhibition of overexpressed mouse DAGLb upon 2 uM compound treatment as assessed by gel-based competitive ABPP.1Integer%
5Inhibition at 0.4 uM [DAGLb] (0.4μM**)Percent Inhibition of overexpressed mouse DAGLb upon 0.4 uM compound treatment as assessed by gel-based competitive ABPP.1Integer%
6Inhibition at 0.08 uM [DAGLb] (0.08μM**)Percent Inhibition of overexpressed mouse DAGLb upon 0.08 uM compound treatment as assessed by gel-based competitive ABPP.1Integer%
7Inhibition at 0.016 uM [DAGLb] (0.016μM**)Percent Inhibition of overexpressed mouse DAGLb upon 0.016 uM compound treatment as assessed by gel-based competitive ABPP.1Integer%
8Inhibition at 0.003 uM [DAGLb] (0.003μM**)Percent Inhibition of overexpressed mouse DAGLb upon 0.003 uM compound treatment as assessed by gel-based competitive ABPP.1Integer%
9Outcome [ABHD11]One of Active, Inactive, or Not Tested2Abhydrolase domain containing 11 [Mus musculus]Outcome
10Score [ABHD11]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)2Integer
11Inhibition at 10 uM [ABHD11] (10μM**)Percent Inhibition of overexpressed mouse ABHD11 upon 10 uM compound treatment as assessed by gel-based competitive ABPP.2Integer%
12Inhibition at 2 uM [ABHD11] (2μM**)Percent Inhibition of overexpressed mouse ABHD11 upon 2 uM compound treatment as assessed by gel-based competitive ABPP.2Integer%
13Inhibition at 0.4 uM [ABHD11] (0.4μM**)Percent Inhibition of overexpressed mouse ABHD11 upon 0.4 uM compound treatment as assessed by gel-based competitive ABPP.2Integer%
14Inhibition at 0.08 uM [ABHD11] (0.08μM**)Percent Inhibition of overexpressed mouse ABHD11 upon 0.08 uM compound treatment as assessed by gel-based competitive ABPP.2Integer%
15Inhibition at 0.016 uM [ABHD11] (0.016μM**)Percent Inhibition of overexpressed mouse ABHD11 upon 0.016 uM compound treatment as assessed by gel-based competitive ABPP.2Integer%
16Inhibition at 0.003 uM [ABHD11] (0.003μM**)Percent Inhibition of overexpressed mouse ABHD11 upon 0.003 uM compound treatment as assessed by gel-based competitive ABPP.2Integer%
17Outcome [PLA2G7]One of Active, Inactive, or Not Tested3platelet-activating factor acetylhydrolase precursor [Mus musculus]Outcome
18Score [PLA2G7]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)3Integer
19Inhibition at 10 uM [PLA2G7] (10μM**)Percent Inhibition of endogenous mouse PLA2G7 upon 10 uM compound treatment as assessed by gel-based competitive ABPP.3Integer%
20Inhibition at 2 uM [PLA2G7] (2μM**)Percent Inhibition of endogenous mouse PLA2G7 upon 2 uM compound treatment as assessed by gel-based competitive ABPP.3Integer%
21Inhibition at 0.4 uM [PLA2G7] (0.4μM**)Percent Inhibition of endogenous mouse PLA2G7 upon 0.4 uM compound treatment as assessed by gel-based competitive ABPP.3Integer%
22Inhibition at 0.08 uM [PLA2G7] (0.08μM**)Percent Inhibition of endogenous mouse PLA2G7 upon 0.08 uM compound treatment as assessed by gel-based competitive ABPP.3Integer%
23Inhibition at 0.016 uM [PLA2G7] (0.016μM**)Percent Inhibition of endogenous mouse PLA2G7 upon 0.016 uM compound treatment as assessed by gel-based competitive ABPP.3Integer%
24Inhibition at 0.003 uM [PLA2G7] (0.003μM**)Percent Inhibition of endogenous mouse PLA2G7 upon 0.003 uM compound treatment as assessed by gel-based competitive ABPP.3Integer%
25Outcome [PAFAH2]One of Active, Inactive, or Not Tested4platelet-activating factor acetylhydrolase 2, cytoplasmic [Mus musculus]Outcome
26Score [PAFAH2]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)4Integer
27Inhibition at 10 uM [PAFAH2] (10μM**)Percent Inhibition of endogenous mouse PAFAH2 upon 10 uM compound treatment as assessed by gel-based competitive ABPP.4Integer%
28Inhibition at 2 uM [PAFAH2] (2μM**)Percent Inhibition of endogenous mouse PAFAH2 upon 2 uM compound treatment as assessed by gel-based competitive ABPP.4Integer%
29Inhibition at 0.4 uM [PAFAH2] (0.4μM**)Percent Inhibition of endogenous mouse PAFAH2 upon 0.4 uM compound treatment as assessed by gel-based competitive ABPP.4Integer%
30Inhibition at 0.08 uM [PAFAH2] (0.08μM**)Percent Inhibition of endogenous mouse PAFAH2 upon 0.08 uM compound treatment as assessed by gel-based competitive ABPP.4Integer%
31Inhibition at 0.016 uM [PAFAH2] (0.016μM**)Percent Inhibition of endogenous mouse PAFAH2 upon 0.016 uM compound treatment as assessed by gel-based competitive ABPP.4Integer%
32Inhibition at 0.003 uM [PAFAH2] (0.003μM**)Percent Inhibition of endogenous mouse PAFAH2 upon 0.003 uM compound treatment as assessed by gel-based competitive ABPP.4Integer%
33Outcome [FAAH]One of Active, Inactive, or Not Tested5fatty acid amide hydrolase [Mus musculus]Outcome
34Score [FAAH]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)5Integer
35Inhibition at 10 uM [FAAH] (10μM**)Percent Inhibition of endogenous mouse FAAH upon 10 uM compound treatment as assessed by gel-based competitive ABPP.5Integer%
36Inhibition at 2 uM [FAAH] (2μM**)Inhibiti Percent on of endogenous mouse FAAH upon 2 uM compound treatment as assessed by gel-based competitive ABPP.5Integer%
37Inhibition at 0.4 uM [FAAH] (0.4μM**)Percent Inhibition of endogenous mouse FAAH upon 0.4 uM compound treatment as assessed by gel-based competitive ABPP.5Integer%
38Inhibition at 0.08 uM [FAAH] (0.08μM**)Percent Inhibition of endogenous mouse FAAH upon 0.08 uM compound treatment as assessed by gel-based competitive ABPP.5Integer%
39Inhibition at 0.016 uM [FAAH] (0.016μM**)Percent Inhibition of endogenous mouse FAAH upon 0.016 uM compound treatment as assessed by gel-based competitive ABPP.5Integer%
40Inhibition at 0.003 uM [FAAH] (0.003μM**)Percent Inhibition of endogenous mouse FAAH upon 0.003 uM compound treatment as assessed by gel-based competitive ABPP.5Integer%
41Outcome [MAGL]One of Active, Inactive, or Not Tested6monoacylglycerol lipase ABHD12 [Mus musculus]Outcome
42Score [MAGL]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)6Integer
43Inhibition at 10 uM [MAGL] (10μM**)Percent Inhibition of endogenous mouse MAGL upon 10 uM compound treatment as assessed by gel-based competitive ABPP.6Integer%
44Inhibition at 2 uM [MAGL] (2μM**)Percent Inhibition of endogenous mouse MAGL upon 2 uM compound treatment as assessed by gel-based competitive ABPP.6Integer%
45Inhibition at 0.4 uM [MAGL] (0.4μM**)Percent Inhibition of endogenous mouse MAGL upon 0.4 uM compound treatment as assessed by gel-based competitive ABPP.6Integer%
46Inhibition at 0.08 uM [MAGL] (0.08μM**)Percent Inhibition of endogenous mouse MAGL upon 0.08 uM compound treatment as assessed by gel-based competitive ABPP.6Integer%
47Inhibition at 0.016 uM [MAGL] (0.016μM**)Percent Inhibition of endogenous mouse MAGL upon 0.016 uM compound treatment as assessed by gel-based competitive ABPP.6Integer%
48Inhibition at 0.003 uM [MAGL] (0.003μM**)Percent Inhibition of endogenous mouse MAGL upon 0.003 uM compound treatment as assessed by gel-based competitive ABPP.6Integer%
49Outcome [ABHD12]One of Active, Inactive, or Not Tested7monoacylglycerol lipase ABHD12 [Mus musculus]Outcome
50Score [ABHD12]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)7Integer
51Inhibition at 10 uM [ABHD12] (10μM**)Percent Inhibition of endogenous mouse ABHD12 upon 10 uM compound treatment as assessed by gel-based competitive ABPP.7Integer%
52Inhibition at 2 uM [ABHD12] (2μM**)Percent Inhibition of endogenous mouse ABHD12 upon 2 uM compound treatment as assessed by gel-based competitive ABPP.7Integer%
53Inhibition at 0.4 uM [ABHD12] (0.4μM**)Percent Inhibition of endogenous mouse ABHD12 upon 0.4 uM compound treatment as assessed by gel-based competitive ABPP.7Integer%
54Inhibition at 0.08 uM [ABHD12] (0.08μM**)Percent Inhibition of endogenous mouse ABHD12 upon 0.08 uM compound treatment as assessed by gel-based competitive ABPP.7Integer%
55Inhibition at 0.016 uM [ABHD12] (0.016μM**)Percent Inhibition of endogenous mouse ABHD12 upon 0.016 uM compound treatment as assessed by gel-based competitive ABPP.7Integer%
56Inhibition at 0.003 uM [ABHD12] (0.003μM**)Percent Inhibition of endogenous mouse ABHD12 upon 0.003 uM compound treatment as assessed by gel-based competitive ABPP.7Integer%
57Outcome [ABHD6]One of Active, Inactive, or Not Tested8monoacylglycerol lipase ABHD6 [Mus musculus]Outcome
58Score [ABHD6]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)8Integer
59Inhibition at 10 uM [ABHD6] (10μM**)Percent Inhibition of endogenous mouse ABHD6 upon 10 uM compound treatment as assessed by gel-based competitive ABPP.8Integer%
60Inhibition at 2 uM [ABHD6] (2μM**)Percent Inhibition of endogenous mouse ABHD6 upon 2 uM compound treatment as assessed by gel-based competitive ABPP.8Integer%
61Inhibition at 0.4 uM [ABHD6] (0.4μM**)Percent Inhibition of endogenous mouse ABHD6 upon 0.4 uM compound treatment as assessed by gel-based competitive ABPP.8Integer%
62Inhibition at 0.08 uM [ABHD6] (0.08μM**)Percent Inhibition of endogenous mouse ABHD6 upon 0.08 uM compound treatment as assessed by gel-based competitive ABPP.8Integer%
63Inhibition at 0.016 uM [ABHD6] (0.016μM**)Percent Inhibition of endogenous mouse ABHD6 upon 0.016 uM compound treatment as assessed by gel-based competitive ABPP.8Integer%
64Inhibition at 0.003 uM [ABHD6] (0.003μM**)Percent Inhibition of endogenous mouse ABHD6 upon 0.003 uM compound treatment as assessed by gel-based competitive ABPP.8Integer%
65Outcome [LYPLA2]One of Active, Inactive, or Not Tested9acyl-protein thioesterase 2 [Mus musculus]Outcome
66Score [LYPLA2]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)9Integer
67Inhibition at 10 uM [LYPLA2] (10μM**)Percent Inhibition of endogenous mouse LYPLA2 upon 10 uM compound treatment as assessed by gel-based competitive ABPP.9Integer%
68Inhibition at 2 uM [LYPLA2] (2μM**)Percent Inhibition of endogenous mouse LYPLA2 upon 2 uM compound treatment as assessed by gel-based competitive ABPP.9Integer%
69Inhibition at 0.4 uM [LYPLA2] (0.4μM**)Percent Inhibition of endogenous mouse LYPLA2 upon 0.4 uM compound treatment as assessed by gel-based competitive ABPP.9Integer%
70Inhibition at 0.08 uM [LYPLA2] (0.08μM**)Percent Inhibition of endogenous mouse LYPLA2 upon 0.08 uM compound treatment as assessed by gel-based competitive ABPP.9Integer%
71Inhibition at 0.016 uM [LYPLA2] (0.016μM**)Percent Inhibition of endogenous mouse LYPLA2 upon 0.016 uM compound treatment as assessed by gel-based competitive ABPP.9Integer%
72Inhibition at 0.003 uM [LYPLA2] (0.003μM**)Percent Inhibition of endogenous mouse LYPLA2 upon 0.003 uM compound treatment as assessed by gel-based competitive ABPP.9Integer%
73Outcome [LYPLA1]One of Active, Inactive, or Not Tested10acyl-protein thioesterase 1 [Mus musculus]Outcome
74Score [LYPLA1]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)10Integer
75Inhibition at 10 uM [LYPLA1] (10μM**)Percent Inhibition of endogenous mouse LYPLA1 upon 10 uM compound treatment as assessed by gel-based competitive ABPP.10Integer%
76Inhibition at 2 uM [LYPLA1] (2μM**)Percent Inhibition of endogenous mouse LYPLA1 upon 2 uM compound treatment as assessed by gel-based competitive ABPP.10Integer%
77Inhibition at 0.4 uM [LYPLA1] (0.4μM**)Percent Inhibition of endogenous mouse LYPLA1 upon 0.4 uM compound treatment as assessed by gel-based competitive ABPP.10Integer%
78Inhibition at 0.08 uM [LYPLA1] (0.08μM**)Percent Inhibition of endogenous mouse LYPLA1 upon 0.08 uM compound treatment as assessed by gel-based competitive ABPP.10Integer%
79Inhibition at 0.016 uM [LYPLA1] (0.016μM**)Percent Inhibition of endogenous mouse LYPLA1 upon 0.016 uM compound treatment as assessed by gel-based competitive ABPP.10Integer%
80Inhibition at 0.003 uM [LYPLA1] (0.003μM**)Percent Inhibition of endogenous mouse LYPLA1 upon 0.003 uM compound treatment as assessed by gel-based competitive ABPP.10Integer%
81Outcome [PNPLA6]One of Active, Inactive, or Not Tested11neuropathy target esterase [Mus musculus]Outcome
82Score [PNPLA6]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)11Integer
83Inhibition at 10 uM [PNPLA6] (10μM**)Percent Inhibition of endogenous mouse PNPLA6 upon 10 uM compound treatment as assessed by gel-based competitive ABPP.11Integer%
84Inhibition at 2 uM [PNPLA6] (2μM**)Percent Inhibition of endogenous mouse PNPLA6 upon 2 uM compound treatment as assessed by gel-based competitive ABPP.11Integer%
85Inhibition at 0.4 uM [PNPLA6] (0.4μM**)Percent Inhibition of endogenous mouse PNPLA6 upon 0.4 uM compound treatment as assessed by gel-based competitive ABPP.11Integer%
86Inhibition at 0.08 uM [PNPLA6] (0.08μM**)Percent Inhibition of endogenous mouse PNPLA6 upon 0.08 uM compound treatment as assessed by gel-based competitive ABPP.11Integer%
87Inhibition at 0.016 uM [PNPLA6] (0.016μM**)Percent Inhibition of endogenous mouse PNPLA6 upon 0.016 uM compound treatment as assessed by gel-based competitive ABPP.11Integer%
88Inhibition at 0.003 uM [PNPLA6] (0.003μM**)Percent Inhibition of endogenous mouse PNPLA6 upon 0.003 uM compound treatment as assessed by gel-based competitive ABPP.11Integer%

** Test Concentration. § Panel component ID.
Additional Information
Grant Number: 1 R01 DA025285

Classification
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