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
BioActive Compounds: 12
Depositor Specified Assays
Show more |
| AID | Name | Type | Probe | Comment |
|---|---|---|---|---|
| 2130 | Fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1). | screening | Primary screen (PME-1 inhibitors) | |
| 2143 | Summary of probe development efforts to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1). | summary | 3 | Summary (PME-1 inhibitors) |
| 2174 | Counterscreen for PME1 inhibitors: fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of lysophospholipase 1 (LYPLA1). | screening | Counterscreen (LYPLA1 inhibitors) | |
| 2171 | Fluorescence polarization-based biochemical high throughput confirmation assay for inhibitors of Protein Phosphatase Methylesterase 1 (PME-1). | screening | Confirmation assay (PME-1 inhibitors) | |
| 2177 | Counterscreen for PME1 inhibitors: fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of lysophospholipase 2 (LYPLA2). | screening | Counterscreen (LYPLA2 inhibitors) | |
| 2232 | Counterscreen for PME1 inhibitors: fluorescence polarization-based biochemical high throughput confirmation assay to identify inhibitors of lysophospholipase 2 (LYPLA2). | screening | Counterscreen confirmation (LYPLA2 inhibitors) | |
| 2233 | Counterscreen for PME1 inhibitors: fluorescence polarization-based biochemical high throughput confirmation assay for inhibitors of lysophospholipase 1 (LYPLA1). | screening | Counterscreen confirmation (LYPLA1 inhibitors) | |
| 2291 | Fluorescence polarization-based Maybridge primary biochemical high throughput screening assay to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1). | screening | Primary screen (PME-1 inhibitors, Maybridge Library) | |
| 2363 | Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Inhibition of PME-1-mediated demethylation of PP2a | screening | MOA assay (Demethylation of PP2a) | |
| 2365 | Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Luminescence-based counterscreen assay to identify cytotoxic compounds | confirmatory | Counterscreen (Cytotoxicity HEC 293T) | |
| 2366 | Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Gel-based Activity-Based Protein Profiling (ABPP) IC50 | confirmatory | ABPP dose response screen (PME-1 inhibitors) | |
| 2368 | Late 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 Assay | screening | MOA assay (PME-1 inhibitors, gel filtration assay) | |
| 2369 | Late stage results from the probe development effort to identify inhibitors of the protein methylesterase PME-1: Gel-based Activity-Based Protein Profiling (ABPP) Inhibition | screening | ABPP screen (PME-1 inhibitors) | |
| 2371 | Late 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 enzyme | confirmatory | ABPP dose response screen (PME-1 inhibitors, purified enzyme) | |
| 463090 | Late 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 site | other | 1 | MOA assay (PME-1 inhibitors, LC-MS assay) |
| 463091 | Late 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 compounds | confirmatory | Counterscreen (Cytotoxicity HeLa) | |
| 463146 | Late stage assay provider results from the probe development effort to identify inhibitors of protein phosphatase methylesterase 1 (PME-1): Fluorescence-based biochemical gel-based ABPP | other | ABPP profiling (PME1 inhibitors in singlicate) | |
| 463149 | Late stage assay provider results from the probe development effort to identify inhibitors of PME-1: Fluorescence-based biochemical gel-based ABPP inhibition and selectivity | other | ABPP profiling (PME1 inhibition and selectivity in singlicate) | |
| 463131 | Late stage assay provider results from the probe development effort to identify inhibitors of protein phosphatase methylesterase 1 (PME-1): fluorescence-based cell-based inhibition | screening | ABPP profiling (PME1 inhibitors in singlicate) | |
| 463130 | Late 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 1 | confirmatory | ABPP profiling dose response (PME1 inhibitors in triplicate) | |
| 463124 | Late 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 2 | confirmatory | ABPP profiling dose response (PME1 inhibitors in triplicate) | |
| 463132 | Late 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 PP2A | screening | MOA assay (PP2a demethylation) | |
| 602468 | 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 among cysteine-reactive proteins | other | ||
| 602485 | Late 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 vivo | other | ||
| 588835 | Late 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 assay | other |
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
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
§ Panel component ID.
| Data Table(Active) Data Table(All) | Show more |
| PID§ | Name | Substance | Panel Targets | Description | Additional Information | ||
|---|---|---|---|---|---|---|---|
| Active | Inactive | ||||||
| 1 | Abhd10 | 12 | 31 | abhydrolase domain-containing protein 10, mitochondrial precursor [Mus musculus] [gi:269784760] | Taxonomy id: 10090 Gene id: 213012 | ||
| 2 | Anti-Target APEH | 43 | Carboxylesterase 1 (monocyte/macrophage serine esterase 1) [Homo sapiens] [gi:82571745] | Taxonomy id: 10090 Gene id: 235606 | |||
| 3 | Anti-Target PREP | 43 | prolyl endopeptidase [Mus musculus] [gi:6755152] | Taxonomy id: 10090 Gene id: 19072 | |||
| 4 | Anti-Target Kiaa1363 | 43 | neutral cholesterol ester hydrolase 1 [Mus musculus] [gi:30520239] | Taxonomy id: 10090 Gene id: 320024 | |||
| 5 | Anti-Target Magl | 43 | monoglyceride lipase isoform d [Mus musculus] [gi:261878511] | Taxonomy id: 10090 Gene id: 23945 | |||
| 6 | Anti-Target ABHD6 | 43 | monoacylglycerol 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
BAO: version: 1.4b1090
BAO: bioassay specification: assay stage: secondary: selectivity
BAO: bioassay specification: assay biosafety level: bsl1
BAO: assay format: biochemical format: protein format: protein complex 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 detail: binding reporter specification: interaction: protein-small molecule
BAO: detection technology: fluorescence: fluorescence intensity
BAO: bioassay specification: assay stage: secondary: selectivity
BAO: bioassay specification: assay biosafety level: bsl1
BAO: assay format: biochemical format: protein format: protein complex 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 detail: binding reporter specification: interaction: protein-small molecule
BAO: detection technology: fluorescence: fluorescence intensity
Result Definitions
| Show more |
| TID | Name | Description | PID§ | Panel Targets | Histogram | Type | Unit | |
|---|---|---|---|---|---|---|---|---|
| Outcome | The BioAssay activity outcome | Outcome | ||||||
| Score | The BioAssay activity ranking score |  | Integer | |||||
| 1 | Outcome [ABHD10] | One of Active, Inactive, or Not Tested | 1 | abhydrolase domain-containing protein 10, mitochondrial precursor [Mus musculus] | | Outcome | ||
| 2 | Score [ABHD10] | The BioAssay activity ranking score | 1 | | Integer | |||
| 3 | Inhibition at 10 uM [ABHD10] (10μM**) | Inhibition of endogenous mouse ABHD10 upon 10 uM compound treatment as assessed by gel-based competitive ABPP. | 1 | | Integer | % | ||
| 4 | Inhibition at 1 uM [ABHD10] (1μM**) | Inhibition of endogenous mouse ABHD10 upon 1 uM compound treatment as assessed by gel-based competitive ABPP. | 1 | | Integer | % | ||
| 5 | Inhibition 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. | 1 | | Integer | % | ||
| 6 | Outcome [APEH] | One of Active, Inactive, or Not Tested | 2 | Carboxylesterase 1 (monocyte/macrophage serine esterase 1) [Homo sapiens] | | Outcome | ||
| 7 | Score [APEH] | The BioAssay activity ranking score | 2 | | Integer | |||
| 8 | Inhibition at 10 uM [APEH] (10μM**) | Inhibition of endogenous mouse APEH upon 10 uM compound treatment as assessed by gel-based competitive ABPP. | 2 | | Integer | % | ||
| 9 | Inhibition at 1 uM [APEH] (1μM**) | Inhibition of endogenous mouse APEH upon 1 uM compound treatment as assessed by gel-based competitive ABPP. | 2 | | Integer | % | ||
| 10 | Inhibition 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. | 2 | | Integer | % | ||
| 11 | Qualifier [APEH] | Qualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity. | 2 | String | ||||
| 12 | Fold 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. | 2 | | Integer | ratio | ||
| 13 | Outcome [PREP] | One of Active, Inactive, or Not Tested | 3 | prolyl endopeptidase [Mus musculus] | | Outcome | ||
| 14 | Score [PREP] | The BioAssay activity ranking score | 3 | | Integer | |||
| 15 | Inhibition at 10 uM [PREP] (10μM**) | Inhibition of endogenous mouse PREP upon 10 uM compound treatment as assessed by gel-based competitive ABPP. | 3 | | Integer | % | ||
| 16 | Inhibition at 1 uM [PREP] (1μM**) | Inhibition of endogenous mouse PREP upon 1 uM compound treatment as assessed by gel-based competitive ABPP. | 3 | | Integer | % | ||
| 17 | Inhibition 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. | 3 | | Integer | % | ||
| 18 | Qualifier [PREP] | Qualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity. | 3 | String | ||||
| 19 | Fold 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. | 3 | | Integer | ratio | ||
| 20 | Outcome [KIAA1363] | One of Active, Inactive, or Not Tested | 4 | neutral cholesterol ester hydrolase 1 [Mus musculus] | | Outcome | ||
| 21 | Score [KIAA1363] | The BioAssay activity ranking score | 4 | | Integer | |||
| 22 | Inhibition at 10 uM [KIAA1363] (10μM**) | Inhibition of endogenous mouse KIAA1363 upon 10 uM compound treatment as assessed by gel-based competitive ABPP. | 4 | | Integer | % | ||
| 23 | Inhibition at 1 uM [KIAA1363] (1μM**) | Inhibition of endogenous mouse KIAA1363 upon 1 uM compound treatment as assessed by gel-based competitive ABPP. | 4 | | Integer | % | ||
| 24 | Inhibition 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. | 4 | | Integer | % | ||
| 25 | Qualifier [KIAA1363] | Qualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity. | 4 | String | ||||
| 26 | Fold 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. | 4 | | Integer | ratio | ||
| 27 | Outcome [MAGL] | One of Active, Inactive, or Not Tested | 5 | monoglyceride lipase isoform d [Mus musculus] | | Outcome | ||
| 28 | Score [MAGL] | The BioAssay activity ranking score | 5 | | Integer | |||
| 29 | Inhibition at 10 uM [MAGL] (10μM**) | Inhibition of endogenous mouse MAGL upon 10 uM compound treatment as assessed by gel-based competitive ABPP. | 5 | | Integer | % | ||
| 30 | Inhibition at 1 uM [MAGL] (1μM**) | Inhibition of endogenous mouse MAGL upon 1 uM compound treatment as assessed by gel-based competitive ABPP. | 5 | | Integer | % | ||
| 31 | Inhibition 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. | 5 | | Integer | % | ||
| 32 | Qualifier [MAGL] | Qualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity. | 5 | String | ||||
| 33 | Fold 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. | 5 | | Integer | ratio | ||
| 34 | Outcome [ABHD6] | One of Active, Inactive, or Not Tested | 6 | monoacylglycerol lipase ABHD6 [Mus musculus] | | Outcome | ||
| 35 | Score [ABHD6] | The BioAssay activity ranking score | 6 | | Integer | |||
| 36 | Inhibition at 10 uM [ABHD6] (10μM**) | Inhibition of endogenous mouse ABHD6 upon 10 uM compound treatment as assessed by gel-based competitive ABPP. | 6 | | Integer | % | ||
| 37 | Inhibition at 1 uM [ABHD6] (1μM**) | Inhibition of endogenous mouse ABHD6 upon 1 uM compound treatment as assessed by gel-based competitive ABPP. | 6 | | Integer | % | ||
| 38 | Inhibition 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. | 6 | | Integer | % | ||
| 39 | Qualifier [ABHD6] | Qualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity. | 6 | String | ||||
| 40 | Fold 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. | 6 | | Integer | ratio | ||
| 41 | Anti-target Count at 10 uM | The 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 ABPP | | Integer | ||||
| 42 | Anti-target Count at 1 uM | The 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 ABPP | | Integer | ||||
| 43 | Anti-target Count at 0.1 uM | The 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 ABPP | | Integer | ||||
| 44 | Qualifier | Qualifier identifies if the resultant fold selectivity was determined manually to be less than or greater than its listed fold selectivity. | String | |||||
| 45 | Overall Fold Selectivity | The 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. | | Integer | ratio |
** Test Concentration. § Panel component ID.
Additional Information
Grant Number: 1 R01 CA132630
Classification
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