Compounds > cay 10499
Page last updated: 2024-11-12

cay 10499

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID9924775
CHEMBL ID570812
CHEBI ID189802
SCHEMBL ID7042914
MeSH IDM0529242

Synonyms (18)

Synonym
CHEMBL570812 ,
cay10499
benzyl n-[4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3-yl)-2-methylphenyl]carbamate
CHEBI:189802
bdbm50414921
SCHEMBL7042914
359714-55-9
benzyl (4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3(2h)-yl)-2-methylphenyl)carbamate
(4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3(2h)-yl)-2-methylphenyl)carbamic acid phenylmethyl ester
F82309
MS-25549
[4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3(2h)-yl)-2-methylphenyl]-carbamic acid, phenylmethyl ester
EX-A6711
magl-in-5
HY-119283
CS-0077517
cid 9924775
AKOS040745147
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
carbamate esterAny ester of carbamic acid or its N-substituted derivatives.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (4)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Fatty-acid amide hydrolase 1Homo sapiens (human)IC50 (µMol)0.03100.00020.59827.0000AID1204560; AID1204563; AID1204564; AID1204565; AID441698; AID743616
Coagulation factor XIII A chainHomo sapiens (human)IC50 (µMol)0.00670.00190.01720.0590AID1204560; AID1204565
Fatty-acid amide hydrolase 1Rattus norvegicus (Norway rat)IC50 (µMol)0.49070.00051.33138.0000AID1363928; AID1655065; AID743631
Monoglyceride lipaseHomo sapiens (human)IC50 (µMol)0.17250.00091.126810.0000AID1182968; AID1224111; AID1224112; AID1224113; AID1224114; AID1334999; AID1363879; AID1408145; AID1455122; AID1624776; AID1655069; AID1681844; AID1686606; AID1727417; AID1734184; AID1734187; AID1759076; AID441697; AID743619; AID743632; AID743633
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (16)

Processvia Protein(s)Taxonomy
fatty acid catabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
arachidonic acid metabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
positive regulation of vasoconstrictionFatty-acid amide hydrolase 1Homo sapiens (human)
monoacylglycerol catabolic processFatty-acid amide hydrolase 1Homo sapiens (human)
blood coagulationCoagulation factor XIII A chainHomo sapiens (human)
peptide cross-linkingCoagulation factor XIII A chainHomo sapiens (human)
blood coagulation, fibrin clot formationCoagulation factor XIII A chainHomo sapiens (human)
lipid metabolic processMonoglyceride lipaseHomo sapiens (human)
fatty acid biosynthetic processMonoglyceride lipaseHomo sapiens (human)
inflammatory responseMonoglyceride lipaseHomo sapiens (human)
regulation of signal transductionMonoglyceride lipaseHomo sapiens (human)
arachidonic acid metabolic processMonoglyceride lipaseHomo sapiens (human)
triglyceride catabolic processMonoglyceride lipaseHomo sapiens (human)
acylglycerol catabolic processMonoglyceride lipaseHomo sapiens (human)
regulation of inflammatory responseMonoglyceride lipaseHomo sapiens (human)
regulation of sensory perception of painMonoglyceride lipaseHomo sapiens (human)
monoacylglycerol catabolic processMonoglyceride lipaseHomo sapiens (human)
regulation of endocannabinoid signaling pathwayMonoglyceride lipaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (10)

Processvia Protein(s)Taxonomy
protein bindingFatty-acid amide hydrolase 1Homo sapiens (human)
phospholipid bindingFatty-acid amide hydrolase 1Homo sapiens (human)
fatty acid amide hydrolase activityFatty-acid amide hydrolase 1Homo sapiens (human)
identical protein bindingFatty-acid amide hydrolase 1Homo sapiens (human)
acylglycerol lipase activityFatty-acid amide hydrolase 1Homo sapiens (human)
amidase activityFatty-acid amide hydrolase 1Homo sapiens (human)
protein-glutamine gamma-glutamyltransferase activityCoagulation factor XIII A chainHomo sapiens (human)
protein bindingCoagulation factor XIII A chainHomo sapiens (human)
metal ion bindingCoagulation factor XIII A chainHomo sapiens (human)
lysophospholipase activityMonoglyceride lipaseHomo sapiens (human)
protein bindingMonoglyceride lipaseHomo sapiens (human)
protein homodimerization activityMonoglyceride lipaseHomo sapiens (human)
acylglycerol lipase activityMonoglyceride lipaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (12)

Processvia Protein(s)Taxonomy
endoplasmic reticulum membraneFatty-acid amide hydrolase 1Homo sapiens (human)
cytoskeletonFatty-acid amide hydrolase 1Homo sapiens (human)
organelle membraneFatty-acid amide hydrolase 1Homo sapiens (human)
extracellular regionCoagulation factor XIII A chainHomo sapiens (human)
extracellular spaceCoagulation factor XIII A chainHomo sapiens (human)
platelet alpha granule lumenCoagulation factor XIII A chainHomo sapiens (human)
collagen-containing extracellular matrixCoagulation factor XIII A chainHomo sapiens (human)
blood microparticleCoagulation factor XIII A chainHomo sapiens (human)
transferase complexCoagulation factor XIII A chainHomo sapiens (human)
endoplasmic reticulum membraneMonoglyceride lipaseHomo sapiens (human)
cytosolMonoglyceride lipaseHomo sapiens (human)
plasma membraneMonoglyceride lipaseHomo sapiens (human)
membraneMonoglyceride lipaseHomo sapiens (human)
membraneMonoglyceride lipaseHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (72)

Assay IDTitleYearJournalArticle
AID1655069Inhibition of human recombinant MAGL2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors.
AID1182975Inhibition of human MAGL assessed as residual enzyme activity at 100 uM using 4-Nitrophenylacetate substrate incubated for 15 mins2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Docking based virtual screening and molecular dynamics study to identify potential monoacylglycerol lipase inhibitors.
AID1224112Inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Identification and characterization of a new reversible MAGL inhibitor.
AID1681844Inhibition of human recombinant MAGL using 1,3-dihydroxypropan-2-yl 4-pyren-1-ylbutanoate as substrate measured after 45 mins by reverse-phase HPLC-based fluorescence assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Acylated 1
AID1224121Irreversible inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Identification and characterization of a new reversible MAGL inhibitor.
AID441697Inhibition of human MGL activity using [3H]2-oleoylglycerol substrate by liquid scintillation counting2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Bis(dialkylaminethiocarbonyl)disulfides as potent and selective monoglyceride lipase inhibitors.
AID743616Inhibition of FAAH (unknown origin)2013European journal of medicinal chemistry, May, Volume: 63(4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
AID1204565Inhibition of human recombinant FAAH using AMC arachidonoyl amide as substrate preincubated with protein for 60 mins followed by substrate addition by fluorescence assay2015European journal of medicinal chemistry, Jun-05, Volume: 97Pyrazole phenylcyclohexylcarbamates as inhibitors of human fatty acid amide hydrolases (FAAH).
AID1408168Antiproliferative activity against human SKOV3 cells measured after 96 hrs2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors.
AID1759076Inhibition of MAGL (unknown origin)2021Bioorganic & medicinal chemistry letters, 06-01, Volume: 41Discovery of novel reversible monoacylglycerol lipase inhibitors via docking-based virtual screening.
AID1727432Cytotoxicity against cancer-derived human organoids in HGSOC patient assessed as reduction in cell viability up to 100 uM measured after 96 hrs by Celltiter-glo luminescent assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
AID1727430Antiproliferative activity against human OVCAR3 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
AID1408145Inhibition of recombinant human C-terminal His-tagged MAGL expressed in Escherichia coli using 4-NPA as substrate measured after 30 mins2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors.
AID743619Inhibition of MAGL (unknown origin)2013European journal of medicinal chemistry, May, Volume: 63(4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
AID1363928Inhibition of rat FAAH2017Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors.
AID1204563Inhibition of human recombinant FAAH using AMC arachidonoyl amide as substrate preincubated with protein for 0 min followed by substrate addition by fluorescence assay2015European journal of medicinal chemistry, Jun-05, Volume: 97Pyrazole phenylcyclohexylcarbamates as inhibitors of human fatty acid amide hydrolases (FAAH).
AID1408165Antiproliferative activity against human HCT116 cells measured after 96 hrs2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors.
AID1727417Inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate incubated for 30 mins by microplate reader assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
AID1686610Irreversible inhibition of human recombinant MAGL pre-incubated for 60 mins before 4-NPA substrate addition2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Structural Optimization of 4-Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1224111Inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate after 30 mins2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Identification and characterization of a new reversible MAGL inhibitor.
AID1727431Antiproliferative activity against human SKOV3 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
AID1408166Antiproliferative activity against human Caov3 cells measured after 96 hrs2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors.
AID1182968Inhibition of human MAGL using 4-Nitrophenylacetate substrate incubated for 15 mins2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Docking based virtual screening and molecular dynamics study to identify potential monoacylglycerol lipase inhibitors.
AID1686615Antiproliferative activity against human OVCAR-3 cells assessed as reduction in cell viability incubated for 96 hrs by Cell-titer-Glo luminescent cell viability assay2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Structural Optimization of 4-Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1363879Inhibition of recombinant human MAGL2017Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors.
AID1455142Antiproliferative activity against human MRC5 cells after 96 hrs2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID743633Inhibition of MAGL (unknown origin) using 4-nitrophenylacetate as substrate2013European journal of medicinal chemistry, May, Volume: 63(4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
AID1686618Antiproliferative activity against human MRC5 cells assessed as reduction in cell viability incubated for 96 hrs by Cell-titer-Glo luminescent cell viability assay2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Structural Optimization of 4-Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1455139Antiproliferative activity against human OVCAR3 cells after 96 hrs2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1334999Inhibition of recombinant human MAGL using 1,3-dihydroxypropan-2-yl 4-pyren-1-yl-butanoate as substrate after 45 mins by fluorescence-based reversed phase HPLC analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
1-Heteroarylpropan-2-ones as inhibitors of fatty acid amide hydrolase: Studies on structure-activity relationships and metabolic stability.
AID1408167Antiproliferative activity against human OVCAR3 cells measured after 96 hrs2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors.
AID1686608Irreversible inhibition of human recombinant MAGL using 4-NPA substrate measured after 40 fold dilution2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Structural Optimization of 4-Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1455141Antiproliferative activity against human Caov3 cells after 96 hrs2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1455122Inhibition of recombinant human MAGL using 4-NPA as substrate after 30 mins by colorimetric analysis2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1624818Growth inhibition of human SKOV3 cells after 96 hrs by celltiter-glo assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
AID1624817Growth inhibition of human OVCAR3 cells after 96 hrs by celltiter-glo assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
AID1224118Cytotoxicity against human COV318 cells assessed as growth inhibition after 96 hrs2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Identification and characterization of a new reversible MAGL inhibitor.
AID1686606Inhibition of human recombinant MAGL using 4-NPA substrate incubated for 30 mins2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Structural Optimization of 4-Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1686617Antiproliferative activity against human Caov-3 cells assessed as reduction in cell viability incubated for 96 hrs by Cell-titer-Glo luminescent cell viability assay2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Structural Optimization of 4-Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1727429Antiproliferative activity against human CAOV3 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
AID441698Inhibition of human recombinant FAAH-maltose binding protein2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Bis(dialkylaminethiocarbonyl)disulfides as potent and selective monoglyceride lipase inhibitors.
AID743631Inhibition of FAAH in Sprague-Dawley rat brain microsomes assessed as N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide conversion to 4-pyren-1-ylbutanoic acid preincubated for 10 mins measured after 45 mins by HPLC analysis2013European journal of medicinal chemistry, May, Volume: 63(4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
AID1224114Inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate preincubated for 60 mins followed by substrate addition2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Identification and characterization of a new reversible MAGL inhibitor.
AID743632Inhibition of human recombinant MAGL-mediated 1,3-dihydroxypropan-1-yl 4-pyren-1-ylbutanoate conversion to 4-pyren-1-ylbutanoic acid preincubated for 15 mins measured after 45 mins by HPLC analysis2013European journal of medicinal chemistry, May, Volume: 63(4-Phenoxyphenyl)tetrazolecarboxamides and related compounds as dual inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
AID1182973Inhibition of human MAGL assessed as residual enzyme activity at 1 uM using 4-Nitrophenylacetate substrate incubated for 15 mins2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Docking based virtual screening and molecular dynamics study to identify potential monoacylglycerol lipase inhibitors.
AID1624814Growth inhibition of human HCT116 cells after 96 hrs by celltiter-glo assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
AID1624816Growth inhibition of human Caov3 cells after 96 hrs by celltiter-glo assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
AID1734187Inhibition of human MAGL using 4-Nitrophenylacetate as substrate2016European journal of medicinal chemistry, Oct-04, Volume: 121Hit to lead optimization of a series of N-[4-(1,3-benzothiazol-2-yl)phenyl]acetamides as monoacylglycerol lipase inhibitors with potential anticancer activity.
AID1408164Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs2018European journal of medicinal chemistry, Sep-05, Volume: 157Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors.
AID1455138Antiproliferative activity against human OVSAHO cells after 96 hrs2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1455140Antiproliferative activity against human COV318 cells after 96 hrs2018Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3
Discovery of 1,5-Diphenylpyrazole-3-Carboxamide Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1224116Cytotoxicity against human MCF7 cells assessed as growth inhibition after 96 hrs2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Identification and characterization of a new reversible MAGL inhibitor.
AID1182974Inhibition of human MAGL assessed as residual enzyme activity at 10 uM using 4-Nitrophenylacetate substrate incubated for 15 mins2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Docking based virtual screening and molecular dynamics study to identify potential monoacylglycerol lipase inhibitors.
AID1727427Antiproliferative activity against human HCT116 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
AID1224117Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 96 hrs2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Identification and characterization of a new reversible MAGL inhibitor.
AID1727428Antiproliferative activity against human MDA-MB-231 cells as reduction in cell growth measured after 96 hrs by Celltiter-glo luminescent assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
AID441792Selectivity ratio for human MGL activity to human recombinant FAAH2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
Bis(dialkylaminethiocarbonyl)disulfides as potent and selective monoglyceride lipase inhibitors.
AID1182972Inhibition of human MAGL assessed as residual enzyme activity at 100 nM using 4-Nitrophenylacetate substrate incubated for 15 mins2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Docking based virtual screening and molecular dynamics study to identify potential monoacylglycerol lipase inhibitors.
AID1624815Growth inhibition of human MDA-MB-231 cells after 96 hrs by celltiter-glo assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
AID1686614Antiproliferative activity against human OVSAHO cells assessed as reduction in cell viability incubated for 96 hrs by Cell-titer-Glo luminescent cell viability assay2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Structural Optimization of 4-Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1182970Inhibition of human MAGL assessed as residual enzyme activity at 1 nM using 4-Nitrophenylacetate substrate incubated for 15 mins2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Docking based virtual screening and molecular dynamics study to identify potential monoacylglycerol lipase inhibitors.
AID1624819Growth inhibition of human MRC5 cells after 96 hrs by celltiter-glo assay2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
AID1204564Inhibition of human recombinant FAAH using AMC arachidonoyl amide as substrate preincubated with protein for 30 mins followed by substrate addition by fluorescence assay2015European journal of medicinal chemistry, Jun-05, Volume: 97Pyrazole phenylcyclohexylcarbamates as inhibitors of human fatty acid amide hydrolases (FAAH).
AID1224113Inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate preincubated for 30 mins followed by substrate addition2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Identification and characterization of a new reversible MAGL inhibitor.
AID1204560Inhibition of human recombinant FAAH using AMC arachidonoyl amide as substrate after 30 mins by fluorescence assay2015European journal of medicinal chemistry, Jun-05, Volume: 97Pyrazole phenylcyclohexylcarbamates as inhibitors of human fatty acid amide hydrolases (FAAH).
AID1182971Inhibition of human MAGL assessed as residual enzyme activity at 10 nM using 4-Nitrophenylacetate substrate incubated for 15 mins2014Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16
Docking based virtual screening and molecular dynamics study to identify potential monoacylglycerol lipase inhibitors.
AID1655065Inhibition of rat FAAH2020Journal of medicinal chemistry, 06-11, Volume: 63, Issue:11
Discovery of Aryl Formyl Piperidine Derivatives as Potent, Reversible, and Selective Monoacylglycerol Lipase Inhibitors.
AID1686616Antiproliferative activity against human COV318 cells assessed as reduction in cell viability incubated for 96 hrs by Cell-titer-Glo luminescent cell viability assay2016Journal of medicinal chemistry, 11-23, Volume: 59, Issue:22
Structural Optimization of 4-Chlorobenzoylpiperidine Derivatives for the Development of Potent, Reversible, and Selective Monoacylglycerol Lipase (MAGL) Inhibitors.
AID1224119Cytotoxicity against human OVCAR3 cells assessed as growth inhibition after 96 hrs2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Identification and characterization of a new reversible MAGL inhibitor.
AID1224120Cytotoxicity against human MSC assessed as growth inhibition after 96 hrs2014Bioorganic & medicinal chemistry, Jul-01, Volume: 22, Issue:13
Identification and characterization of a new reversible MAGL inhibitor.
AID1624776Inhibition of human recombinant MAGL using 4-NPA as substrate after 30 mins2019Journal of medicinal chemistry, 02-28, Volume: 62, Issue:4
Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
AID1734184Inhibition of MAGL (unknown origin)2016European journal of medicinal chemistry, Oct-04, Volume: 121Hit to lead optimization of a series of N-[4-(1,3-benzothiazol-2-yl)phenyl]acetamides as monoacylglycerol lipase inhibitors with potential anticancer activity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (16)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (6.25)29.6817
2010's11 (68.75)24.3611
2020's4 (25.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 13.09

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index13.09 (24.57)
Research Supply Index2.83 (2.92)
Research Growth Index5.92 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (13.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (6.25%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other15 (93.75%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
SubstanceRelationship StrengthStudiesTrialsClassesRoles
phenytoin
[no description available]		2.1510imidazolidine-2,4-dioneanticonvulsant;
drug allergen;
sodium channel blocker;
teratogenic agent
disulfiram
[no description available]		3.5920organic disulfide;
organosulfur acaricide		angiogenesis inhibitor;
antineoplastic agent;
apoptosis inducer;
EC 1.2.1.3 [aldehyde dehydrogenase (NAD(+))] inhibitor;
EC 3.1.1.1 (carboxylesterase) inhibitor;
EC 3.1.1.8 (cholinesterase) inhibitor;
EC 5.99.1.2 (DNA topoisomerase) inhibitor;
ferroptosis inducer;
fungicide;
NF-kappaB inhibitor
hexadecanesulfonyl fluoride
AM 374: a palmitylsulfonyl fluoride; inhibits anandamide amidase; structure given in first source		3.2510acyl fluoride
ethylmaleimide
Ethylmaleimide: A sulfhydryl reagent that is widely used in experimental biochemical studies.		3.2510maleimidesanticoronaviral agent;
EC 1.3.1.8 [acyl-CoA dehydrogenase (NADP(+))] inhibitor;
EC 2.1.1.122 [(S)-tetrahydroprotoberberine N-methyltransferase] inhibitor;
EC 2.7.1.1 (hexokinase) inhibitor
thiram
Thiram: A dithiocarbamate chemical, used commercially in the rubber processing industry and as a fungicide. In vivo studies indicate that it inactivates the enzyme GLUTATHIONE REDUCTASE. It has mutagenic activity and may induce chromosomal aberrations.. thiram : An organic disulfide that results from the formal oxidative dimerisation of N,N-dimethyldithiocarbamic acid. It is widely used as a fungicidal seed treatment.		2.0510organic disulfideantibacterial drug;
antifungal agrochemical;
antiseptic drug
bis(1-piperidylthiocarbonyl)disulfide
bis(1-piperidylthiocarbonyl)disulfide: indicator for analysis of copper; structure		2.0510
tetramethylthiuram monosulfide
[no description available]		2.0510
4,4'-dithiodimorpholine
4,4'-dithiodimorpholine: rubber vulcanizing agent causing occupational dermatitis; structure		2.0510
methyl diethyldithiocarbamate
[no description available]		2.0510
diphenyl disulfide
[no description available]		3.2510benzenes
diacerein
diacerein: chelates with bivalent metals; a quinone which possesses redox properties; metabolized to active rhein; proposed mechanisms include inhibiting IL1 and metalloproteinases; called a slow acting symptomatic drug in osteoarthritis; no effect of cyclooxygenase;		3.2510anthraquinone
2-n-octyl-4-isothiazolin-3-one
octhilinone : A member of the class of 1,2-thiazole that is 1,2-thiazol-3-one substituted on the nitrogen (position 2) by an octyl group. A fungicide and antibacterial agent, it is used for treatment of canker and other fungal and bacterial diseases in fruit trees. It is no longer approved for use within the European Union.		3.25101,2-thiazolesantibacterial agent;
antifungal agrochemical;
environmental contaminant;
xenobiotic
gemcitabine
gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.		2.3110organofluorine compound;
pyrimidine 2'-deoxyribonucleoside		antimetabolite;
antineoplastic agent;
antiviral drug;
DNA synthesis inhibitor;
EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor;
environmental contaminant;
immunosuppressive agent;
photosensitizing agent;
prodrug;
radiosensitizing agent;
xenobiotic
fluoxetine hydrochloride
fluoxetine hydrochloride : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine hydrochloride. A selective serotonin reuptake inhibitor (SSRI), it is used for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder.		2.2510hydrochloride;
N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine
celastrol methyl ester
celastrol methyl ester: isolated from Tripterygium wilfordii; potent inhibitory activity on both Kir2.1 and ERG1 potassium channels, leading to LONG QT SYNDROME		2.3110carboxylic ester
dabigatran
Dabigatran: A THROMBIN inhibitor which acts by binding and blocking thrombogenic activity and the prevention of thrombus formation. It is used to reduce the risk of stroke and systemic EMBOLISM in patients with nonvalvular atrial fibrillation.. dabigatran : An aromatic amide obtained by formal condensation of the carboxy group of 2-{[(4-carbamimidoylphenyl)amino]methyl}-1-methyl-1H-benzimidazole-5-carboxylic acid with the secondary amoino group of N-pyridin-2-yl-beta-alanine. The active metabolite of the prodrug dabigatran etexilate, it acts as an anticoagulant which is used for the prevention of stroke and systemic embolism.		2.2510aromatic amide;
benzimidazoles;
beta-alanine derivative;
carboxamidine;
pyridines		anticoagulant;
EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor;
EC 3.4.21.5 (thrombin) inhibitor
euphol
euphol: from Euphorbia acaulis Roxb.; structure given in first source		2.3110triterpenoid
urb 597
cyclohexyl carbamic acid 3'-carbamoylbiphenyl-3-yl ester: a fatty acid amide hydrolase inhibitor; structure in first source		4.560biphenyls
arachidonyltrifluoromethane
arachidonyltrifluoromethane: structure given in first source; inhibits 85-kDa phospholipase A2. AACOCF3 : A fatty acid derivative that is arachidonic acid in which the OH part of the carboxy group has been replaced by a trifluoromethyl group		2.0510fatty acid derivative;
ketone;
olefinic compound;
organofluorine compound		EC 3.1.1.4 (phospholipase A2) inhibitor
anandamide
anandamide : An N-acylethanolamine 20:4 resulting from the formal condensation of carboxy group of arachidonic acid with the amino group of ethanolamine.		3.2510endocannabinoid;
N-acylethanolamine 20:4		human blood serum metabolite;
neurotransmitter;
vasodilator agent
glyceryl 2-arachidonate
glyceryl 2-arachidonate: binds to cannabinoid receptors; structure in first source. 2-arachidonoylglycerol : An endocannabinoid and an endogenous agonist of the cannabinoid receptors (CB1 and CB2). It is an ester formed from omega-6-arachidonic acid and glycerol.		3.25102-acylglycerol 20:4;
endocannabinoid		human metabolite
[2-(1-piperidinyl)-1,3-benzothiazol-6-yl]-[4-(2-pyridinyl)-1-piperazinyl]methanone
[no description available]		2.3110piperazines;
pyridines
rivaroxaban
Rivaroxaban: A morpholine and thiophene derivative that functions as a FACTOR XA INHIBITOR and is used in the treatment and prevention of DEEP-VEIN THROMBOSIS and PULMONARY EMBOLISM. It is also used for the prevention of STROKE and systemic embolization in patients with non-valvular ATRIAL FIBRILLATION, and for the prevention of atherothrombotic events in patients after an ACUTE CORONARY SYNDROME.. rivaroxaban : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 5-chlorothiophene-2-carboxylic acid with the amino group of 4-{4-[(5S)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl}morpholin-3-one. An anticoagulant used for prophylaxis of venous thromboembolism in patients with knee or hip replacement surgery.		2.2510aromatic amide;
lactam;
monocarboxylic acid amide;
morpholines;
organochlorine compound;
oxazolidinone;
thiophenes		anticoagulant;
EC 3.4.21.6 (coagulation factor Xa) inhibitor
CAY10435
[no description available]		3.2510oxazolopyridine
urb 524
[no description available]		3.2510
ol-135
[no description available]		3.2510
methyl arachidonylfluorophosphonate
[no description available]		2.0510phosphonic ester
urb602
URB602: inhibitor of 2-arachidonoylglycerol (2-AG)-deactivating enzyme, monoacylglycerol lipase, structure in first source		4.1340
ly2183240
LY2183240: structure in first source		3.8730biphenyls
methylphenidate
N-phenyl-4-(quinolin-2-ylmethyl)piperazine-1-carboxamide: a fatty acid amide hydrolase inhibitor; structure in first source		3.2510
omdm 169
OMDM 169: has antinociceptive activity; structure in first source		2.1710
wwl70
[no description available]		2.2110
am 6701
[no description available]		3.9130
jzl 184
JZL 184: inhibits monoacylglycerol lipase; structure in first source		3.4160benzodioxoles
pf 3845
PF 3845: inhibits fatty acid amide hydrolase		3.2510piperidines
pf 750
N-phenyl-4-(quinolin-3-ylmethyl)piperidine-1-carboxamide: a fatty acid amide hydrolase inhibitor; structure in first source		3.2510quinolines
jzl195
JZL195: inhibits both ​fatty-acid amide hydrolase 1 and ​monoglyceride lipase; structure in first source		2.2510
urb937
URB937: a peripherally restricted inhibitor of fatty acid amide hydrolase		3.2510
sar127303
SAR127303: inhibits monoacylglycerol lipase; structure in first source		3.2510
mjn110
MJN110: structure in first source		4.0130
ConditionIndicatedRelationship StrengthStudiesTrials
Nerve Pain
[description not available]		02.1710
Neuralgia
Intense or aching pain that occurs along the course or distribution of a peripheral or cranial nerve.		02.1710
Benign Neoplasms
[description not available]		02.3110
Neoplasms
New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.		02.3110