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BioAssay: AID 602354

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

Name: Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): fluorescence-based biochemical dose-response gel-based competitive Activity-Based Protein Profiling (ABPP) inhibition of DAGLb in situ. ..more
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 Tested Compounds
 Tested Compounds
All(2)
 
 
Active(2)
 
 
 Tested Substances
 Tested Substances
All(2)
 
 
Active(2)
 
 
AID: 602354
Data Source: The Scripps Research Institute Molecular Screening Center (DAGLB_INH_FLUO_3XIC50_INSITU)
BioAssay Type: Panel, Confirmatory, Concentration-Response Relationship Observed
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
BioAssay Version:
Deposit Date: 2012-03-09
Hold-until Date: 2012-10-12
Modify Date: 2012-10-12

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compounds: 2
Related Experiments
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AIDNameTypeProbeComment
504411Fluorescence-based primary biochemical high throughput screening assay to identify inhibitors of human diacylglycerol lipase, beta (DAGLB)Screening depositor-specified cross reference: Primary screen (DAGLB inhibitors in singlicate)
504420Summary of the probe development efforts to identify inhibitors of human diacylglycerol lipase, beta (DAGLB)Summary3 depositor-specified cross reference: Summary (DAGLB inhibitors)
504445Fluorescence-based biochemical high throughput confirmation assay for inhibitors of human diacylglycerol lipase, beta (DAGLB)Screening depositor-specified cross reference: 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 depositor-specified cross reference
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 depositor-specified cross reference
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 depositor-specified cross reference
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 depositor-specified cross reference
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 depositor-specified cross reference
624468Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): LCMS-based biochemical dose response assayConfirmatory depositor-specified cross reference
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 depositor-specified cross reference
602299Late 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 overexpressed DAGLb in vitro set 2Other same project related to Summary assay
602300Late 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 overexpressed DAGLb in vitro set 3Other same project related to Summary assay
602301Late 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 anti-target ABHD11 in vitro set 1Other same project related to Summary assay
602302Late 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 overexpressed DAGLb in vitro set 1Other same project related to Summary assay
602303Late 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 overexpressed DAGLb in vitro; triazole urea libraryOther same project related to Summary assay
602311Late 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 mouse brain membrane in vitro set 1Other same project related to Summary assay
602312Late 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 anti-target ABHD11 in vitro set 2Other same project related to Summary assay
602319Late 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 antitarget ABHD6 in vitroOther same project related to Summary assay
602320Late 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 DAGLb in vitroConfirmatory same project related to Summary assay
602321Late 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 mouse brain membrane in vitro set 3Other same project related to Summary assay
602322Late 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 vitroConfirmatory same project related to Summary assay
602323Late 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 mouse brain membrane in vitro set 2Other same project related to Summary assay
602335Late 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 anti-target ABHD6 in situConfirmatory same project related to Summary assay
602337Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compoundsConfirmatory same project related to Summary assay
602339Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysisOther same project related to Summary assay
602341Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis for ABHD6Other same project related to Summary assay
602343Late 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 brain ABHD6 in vivo, set 2Other same project related to Summary assay
602345Late 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 macrophage DAGLb in vivoOther same project related to Summary assay
602347Late 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 brain ABHD6 in vivoOther same project related to Summary assay
602349Late stage assay provider results from the probe development effort to identify inhibitors of DAGLb: fluorescence-based biochemical gel-based competitive Activity-Based Protein Profiling (ABPP) assay to distinguish systemic and peripheral inhibitorsOther same project related to Summary assay
602351Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): LCMS-based animal-based Activity-Based Protein Profiling (ABPP) MudPIT selectivity analysis for ABHD6Other same project related to Summary assay
602353Late stage assay provider results from the probe development effort to identify inhibitors of diacylglycerol lipase, beta (DAGLb): LCMS-based animal-based Activity-Based Protein Profiling (ABPP) MudPIT selectivity analysisOther same project related to Summary assay
602355Late 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 vitroOther same project related to Summary assay
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_3XIC50_INSITU

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

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 -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 -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, abhydrolase domain containing protein 6, ABHD6, activity-based protein profiling, ABPP, gel-based, activity-based probe, HT-01, inhibitor, inhibition, dose response, IC50, in situ, Neuro-2A, Scripps, Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN
Panel Information
Targets
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1DAGLb2sn1-specific diacylglycerol lipase beta [Mus musculus] [gi:31559956]
Taxonomy id: 10090
Gene id: 231871
2ABHD62monoacylglycerol 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 the IC50 values of powder samples of test compounds for DAGLb and anti-target ABHD6 inhibition in a complex proteome lysate. In this assay, a fluorescently-labeled activity-based probe, HT-01, which selectively labels several serine hydrolases including DAGLb and ABHD6, is used to label DAGLb and ABHD6 in the presence of test compounds. 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 enzyme 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:
Cultured Neuro-2A murine neuroblastoma cells (5 mL DMEM medium with 10% FCS) were treated with test compound (1 uL of 5000x stock in DMSO) or DMSO only (1 uL) and incubated for 4 hours at 37 C. Cells were washed with DPBS (4x), harvested, and homogenized by sonication. The protein concentration was adjusted to 2 mg/mL with Dulbecco's PBS (DPBS), and an aliquot (50 uL) was reacted with HT-01 (1 uL of a 50x stock in DMSO; 1 uM final concentration) for 30 minutes at 37 C. Samples were quenched with an equal volume of 2x 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 DAGLb and anti-target ABHD6 bands relative to the DMSO-only (no compound) control. IC50 values were determined from dose-response curves from three replicates at each inhibitor concentration (9-point 1:3 dilution series from 0.333 uM to 0.000033 uM (333 nM to 0.033 nM)).
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 DAGLb or ABHD6 treated with test compound.
High_Control is defined as DAGLb or ABHD6 treated with DMSO only (no compound).
Low_Control is defined as background in a blank region of the gel.
For each test compound, percent inhibition was plotted 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). The software-generated IC50 values are reported.
PubChem Activity Outcome and Score:
The following applies to each panel in this assay:
Compounds with an IC50 less than or equal to 50 nM were considered active. Compounds with an IC50 greater than 50 nM were considered inactive.
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.
DAGLb Score: The PubChem Activity Score range for active compounds is 100-1. There are no inactive compounds.
ABHD6 Score: The PubChem Activity Score range for active compounds is 100-1. There are no inactive compounds.
Overall Outcome and Score:
Compounds active for DAGLb were considered active regardless of the ABHD6 outcome. Compounds inactive for DAGLb were considered inactive regardless of the ABHD6 outcome.
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. There are no inactive compounds.
List of Reagents:
Neuro-2A cells (provided by Assay Provider)
HT-01 (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 - additional comments and annotations
From BioAssay Depositor:
BAO: assay format: biochemical format: protein format: single protein 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: alternate confirmatory
BAO: detection technology: fluorescence: fluorescence intensity
BAO: meta target detail: binding reporter specification: interaction: protein-small molecule
BAO: meta target: biological process target: regulation of molecular function
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 [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
3Average IC50 [DAGLb]*The average concentration at which 50 percent of the activity in the antagonist assay is observed; (IC50) shown in nanomolar.1FloatμM
4Inhibition at 0.333 uM [1, DAGLb] (0.333μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.333 uM compound concentration; replicate [1]1Float%
5Inhibition at 0.1 uM [1, DAGLb] (0.1μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.1 uM compound concentration; replicate [1]1Float%
6Inhibition at 0.033 uM [1, DAGLb] (0.033μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.033 uM compound concentration; replicate [1]1Float%
7Inhibition at 0.01 uM [1, DAGLb] (0.01μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.01 uM compound concentration; replicate [1]1Float%
8Inhibition at 0.0033 uM [1, DAGLb] (0.0033μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.0033 uM compound concentration; replicate [1]1Float%
9Inhibition at 0.001 uM [1, DAGLb] (0.001μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.001 uM compound concentration; replicate [1]1Float%
10Inhibition at 0.00033 uM [1, DAGLb] (0.00033μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.00033 uM compound concentration; replicate [1]1Float%
11Inhibition at 0.0001 uM [1, DAGLb] (0.0001μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.0001 uM compound concentration; replicate [1]1Float%
12Inhibition at 0.000033 uM [1, DAGLb] (3.3e-05μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.000033 uM compound concentration; replicate [1]1Float%
13Inhibition at 0.333 uM [2, DAGLb] (0.333μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.333 uM compound concentration; replicate [2]1Float%
14Inhibition at 0.1 uM [2, DAGLb] (0.1μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.1 uM compound concentration; replicate [2]1Float%
15Inhibition at 0.033 uM [2, DAGLb] (0.033μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.033 uM compound concentration; replicate [2]1Float%
16Inhibition at 0.01 uM [2, DAGLb] (0.01μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.01 uM compound concentration; replicate [2]1Float%
17Inhibition at 0.0033 uM [2, DAGLb] (0.0033μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.0033 uM compound concentration; replicate [2]1Float%
18Inhibition at 0.001 uM [2, DAGLb] (0.001μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.001 uM compound concentration; replicate [2]1Float%
19Inhibition at 0.00033 uM [2, DAGLb] (0.00033μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.00033 uM compound concentration; replicate [2]1Float%
20Inhibition at 0.0001 uM [2, DAGLb] (0.0001μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.0001 uM compound concentration; replicate [2]1Float%
21Inhibition at 0.000033 uM [2, DAGLb] (3.3e-05μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.000033 uM compound concentration; replicate [2]1Float%
22Inhibition at 0.333 uM [3, DAGLb] (0.333μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.333 uM compound concentration; replicate [3]1Float%
23Inhibition at 0.1 uM [3, DAGLb] (0.1μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.1 uM compound concentration; replicate [3]1Float%
24Inhibition at 0.033 uM [3, DAGLb] (0.033μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.033 uM compound concentration; replicate [3]1Float%
25Inhibition at 0.01 uM [3, DAGLb] (0.01μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.01 uM compound concentration; replicate [3]1Float%
26Inhibition at 0.0033 uM [3, DAGLb] (0.0033μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.0033 uM compound concentration; replicate [3]1Float%
27Inhibition at 0.001 uM [3, DAGLb] (0.001μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.001 uM compound concentration; replicate [3]1Float%
28Inhibition at 0.00033 uM [3, DAGLb] (0.00033μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.00033 uM compound concentration; replicate [3]1Float%
29Inhibition at 0.0001 uM [3, DAGLb] (0.0001μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.0001 uM compound concentration; replicate [3]1Float%
30Inhibition at 0.000033 uM [3, DAGLb] (3.3e-05μM**)The value for percent inhibition of endogenous mouse DAGLb in situ at 0.000033 uM compound concentration; replicate [3]1Float%
31Outcome [ABHD6]One of Active, Inactive, or Not Tested2monoacylglycerol lipase ABHD6 [Mus musculus]Outcome
32Score [ABHD6]The BioAssay activity ranking score. (See PubChem Activity Outcome and Score section in Protocol for details.)2Integer
33Average IC50 [ABHD6]*The average concentration at which 50 percent of the activity in the antagonist assay is observed; (IC50) shown in nanomolar.2FloatμM
34Inhibition at 0.333 uM [1, ABHD6] (0.333μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.333 uM compound concentration; replicate [1]2Float%
35Inhibition at 0.1 uM [1, ABHD6] (0.1μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.1 uM compound concentration; replicate [1]2Float%
36Inhibition at 0.033 uM [1, ABHD6] (0.033μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.033 uM compound concentration; replicate [1]2Float%
37Inhibition at 0.01 uM [1, ABHD6] (0.01μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.01 uM compound concentration; replicate [1]2Float%
38Inhibition at 0.0033 uM [1, ABHD6] (0.0033μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.0033 uM compound concentration; replicate [1]2Float%
39Inhibition at 0.001 uM [1, ABHD6] (0.001μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.001 uM compound concentration; replicate [1]2Float%
40Inhibition at 0.00033 uM [1, ABHD6] (0.00033μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.00033 uM compound concentration; replicate [1]2Float%
41Inhibition at 0.0001 uM [1, ABHD6] (0.0001μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.0001 uM compound concentration; replicate [1]2Float%
42Inhibition at 0.000033 uM [1, ABHD6] (3.3e-05μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.000033 uM compound concentration; replicate [1]2Float%
43Inhibition at 0.333 uM [2, ABHD6] (0.333μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.333 uM compound concentration; replicate [2]2Float%
44Inhibition at 0.1 uM [2, ABHD6] (0.1μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.1 uM compound concentration; replicate [2]2Float%
45Inhibition at 0.033 uM [2, ABHD6] (0.033μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.033 uM compound concentration; replicate [2]2Float%
46Inhibition at 0.01 uM [2, ABHD6] (0.01μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.01 uM compound concentration; replicate [2]2Float%
47Inhibition at 0.0033 uM [2, ABHD6] (0.0033μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.0033 uM compound concentration; replicate [2]2Float%
48Inhibition at 0.001 uM [2, ABHD6] (0.001μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.001 uM compound concentration; replicate [2]2Float%
49Inhibition at 0.00033 uM [2, ABHD6] (0.00033μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.00033 uM compound concentration; replicate [2]2Float%
50Inhibition at 0.0001 uM [2, ABHD6] (0.0001μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.0001 uM compound concentration; replicate [2]2Float%
51Inhibition at 0.000033 uM [2, ABHD6] (3.3e-05μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.000033 uM compound concentration; replicate [2]2Float%
52Inhibition at 0.333 uM [3, ABHD6] (0.333μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.333 uM compound concentration; replicate [3]2Float%
53Inhibition at 0.1 uM [3, ABHD6] (0.1μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.1 uM compound concentration; replicate [3]2Float%
54Inhibition at 0.033 uM [3, ABHD6] (0.033μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.033 uM compound concentration; replicate [3]2Float%
55Inhibition at 0.01 uM [3, ABHD6] (0.01μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.01 uM compound concentration; replicate [3]2Float%
56Inhibition at 0.0033 uM [3, ABHD6] (0.0033μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.0033 uM compound concentration; replicate [3]2Float%
57Inhibition at 0.001 uM [3, ABHD6] (0.001μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.001 uM compound concentration; replicate [3]2Float%
58Inhibition at 0.00033 uM [3, ABHD6] (0.00033μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.00033 uM compound concentration; replicate [3]2Float%
59Inhibition at 0.0001 uM [3, ABHD6] (0.0001μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.0001 uM compound concentration; replicate [3]2Float%
60Inhibition at 0.000033 uM [3, ABHD6] (3.3e-05μM**)The value for percent inhibition of endogenous mouse ABHD6 in situ at 0.000033 uM compound concentration; replicate [3]2Float%

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

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