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2-arachidonoylglycerol + H2O
arachidonic acid + glycerol
2-monooleoylglycerol + H2O
oleic acid + glycerol
-
-
r
monoacylglycerol + H2O
acylic acid + glycerol
-
-
-
?
1(3)-arachidonoylglycerol + H2O
? + glycerol
-
-
-
?
1(3)-monooleoylglycerol + H2O
oleic acid + glycerol
-
-
-
-
?
1,3-dihydroxypropan-2-yl 4-pyren-1-ylbutanoate
pyrenylbutanoic acid + glycerol
-
-
-
-
?
1-monomyristoylglycerol + H2O
myristic acid + glycerol
-
-
-
-
?
1-monopalmitoylglycerol + H2O
palmitic acid + glycerol
-
-
-
-
?
2-arachidonoylglycerol + H2O
arachidonic acid + glycerol
2-arachidonoylglycerol + H2O
glycerol + arachidonic acid
2-monomyristoylglycerol + H2O
myristic acid + glycerol
-
-
-
-
?
2-monoolein + H2O
?
-
-
-
-
?
2-monooleoylglycerol + H2O
oleic acid + glycerol
2-monopalmitoylglycerol + H2O
palmitic acid + glycerol
-
-
-
-
?
2-oleoylglycerol + H2O
oleic acid + glycerol
bis(monoacylclycerol) phosphate + H2O
?
-
at pH 5.5
-
?
lysobisphosphatidic acid + H2O
?
-
at pH 5.5
-
?
methyl butyrate + H2O
methanol + butanoate
-
-
-
-
?
monoarachidonoylglycerol + H2O
arachidonic acid + glycerol
-
-
-
?
monolinoleoylglycerol + H2O
linoic acid + glycerol
-
-
-
?
monooleoylglycerol + H2O
oleic acid + glycerol
monostearoylglycerol + H2O
stearic acid + glycerol
-
-
-
?
palmitoyl-CoA + H2O
palmitic acid + CoA
-
-
-
-
?
prostaglandin D2-G + H2O
?
-
-
-
-
?
prostaglandin E2-G + H2O
?
-
-
-
-
?
prostaglandin F3alpha-G + H2O
?
-
-
-
-
?
sn-2-arachidonoylglycerol + H2O
arachidonic acid + glycerol
-
-
-
?
tributyrylglycerol + H2O
?
-
-
-
-
?
additional information
?
-
2-arachidonoylglycerol + H2O
arachidonic acid + glycerol
-
-
?
2-arachidonoylglycerol + H2O
arachidonic acid + glycerol
-
-
-
?
2-arachidonoylglycerol + H2O
arachidonic acid + glycerol
-
-
-
?
2-arachidonoylglycerol + H2O
arachidonic acid + glycerol
-
-
-
?
2-arachidonoylglycerol + H2O
arachidonic acid + glycerol
-
-
-
-
?
2-arachidonoylglycerol + H2O
arachidonic acid + glycerol
-
the enzyme is responsible for degradation of 2-arachidonoylglycerol in the brain
-
-
?
2-arachidonoylglycerol + H2O
glycerol + arachidonic acid
-
-
-
-
?
2-arachidonoylglycerol + H2O
glycerol + arachidonic acid
-
presynaptic MGL not only hydrolyzes 2-arachidonoylglycerol released from activated postsynaptic neurons but also contributes to degradation of constitutively produced 2-arachidonoylglycerol and prevention of its accumulation around presynaptic terminals. Thus, the MGL activity determines basal endocannabinoid tone and terminates retrograde endocannabinoid signaling in the hippocampus
-
-
?
2-monooleoylglycerol + H2O
oleic acid + glycerol
-
-
-
-
?
2-monooleoylglycerol + H2O
oleic acid + glycerol
-
-
-
r
2-oleoylglycerol + H2O
oleic acid + glycerol
-
-
-
-
?
2-oleoylglycerol + H2O
oleic acid + glycerol
-
Cys208 plays an important role in MGL function
-
-
?
monooleoylglycerol + H2O
oleic acid + glycerol
-
-
-
-
?
monooleoylglycerol + H2O
oleic acid + glycerol
-
-
-
?
additional information
?
-
enzyme does not hydrolyze palmitoylethanolamine, enzyme preferentially hydrolyzes 2-monoglycerides
-
?
additional information
?
-
-
-
-
-
?
additional information
?
-
-
no activity against long-chain diacylglycerols and triacylglycerols, cholesterol ester, or lysophosphatidylcholine
-
-
?
additional information
?
-
-
substrate specificity, overview
-
-
?
additional information
?
-
-
enzyme exhibits both phosphatidic acid-preferring phospholipase A2 and monoacylglycerol lipase activities with a modest specificity towards unsaturated acyl chains, veryl low di- and triaclyglycerol lipase activity
-
?
additional information
?
-
-
monoacylglycerol lipase is required in the final hydrolysis of 2-monoacylglycerols produced by hormone-sensitive lipase
-
-
?
additional information
?
-
-
the enzyme is involved in prostaglandin metabolism in brain particulate fractions
-
-
?
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4-chlormercurybenzoate
IC50 value is 0.072 mM
arachidonoyl trifluoromethylketone
50% inhibition at 0.0025 mM
hexadecylsufonyl fluoride
50% inhibition at 0.0062 mM
HgCl2
IC50 value is 0.042 mM
JZL184
significantly decreases lipolysis and increases both mono- and diacyglycerol species in INS-1 cells. Analysis of the kinetics of glucose-stimulated insulin secretion (GSIS) shows that inhibition is greater during the sustained phase of secretion. JZL184 does not significantly affect basal insulin secretion at any concentration tested. Kinetics, overview
Maleimide
IC50 value is 0.070 mM
methyl arachidonyl fluorophosphonate
50% inhibition at 0.0008 mM
MJN110
inhibits glucose-stimulated insulin secretion and depolarization-induced insulin secretion in INS-1 (832/13) cells
N-(1-pyrenyl)-maleimide
IC50 value is 0.068 mM
N-arachidonoylmaleimide
IC50 value is 0.00014 mM
N-cyclohexylmaleimide
IC50 value is 0.051 mM
N-hydroxymaleimide
IC50 value is 0.413 mM
N-Phenylmaleimide
IC50 value is 0.044 mM
N-propylmaleimide
IC50 value is 0.053 mM
NEM
IC50 value is 0.053 mM
URB602
inhibits glucose-stimulated insulin secretion and depolarization-induced insulin secretion in INS-1 (832/13) cells
(2R,9Z)-octadec-9-ene-1,2-diamine dihydrochloride
-
inhibits by 42.2%
(2S)-6-[4-(hexyloxy)phenyl]hexane-1,2-diamine
-
exhibits weak inhibitory activity (25.9%)
(2S,9Z)-octadec-9-ene-1,2-diamine
-
selectively inhibits MGL by 49.9%. The presence of a long monounsaturated chain corresponding to oleic acid is a key requirement for the selective inhibition of MGL
(4-amidinophenyl) methanesulfonyl fluoride
-
i.e. APMSF, inhibits at 0.5 mM
(5E)-5-(3-methylbutylidene)-2-thioxo-1,3-thiazolidin-4-one
-
weak inhibitory effect
(5Z,8Z,11Z,14Z)-eicosantetraenoic acid 3-thienyl methyl ester
-
i.e. CAY-10402, 14% inhibition at 0.1 mM
(R)-2-aminohexadecanol
-
inhibits by 30%
(S)-2-aminohexadecanol
-
inhibits by 31.5%
1,2-diaminohexadecane
-
inhibits by 30.3%
1-(20-cyano-16,16-dimethyl-eicosa-5,8,11,14-tetraenoyl)glycerol
-
i.e. O-223
1-(20-hydroxy-16,16-dimethyl-eicosa-5,8,11,14-tetraenoyl)glycerol
-
i.e. O-224
1-arachidin
-
11% inhibition of the membraneous enzyme at 0.1 mM, 19% inhibition of the cytosolic enzyme at 0.1 mM
1-myristin
-
IC50 value for the membraneous and the cytosolic enzyme is 0.032 mM, complete inhibition is possible
1-nor-arachidonoyl-3-(2'3-dihydroxypropyl) urea
-
i.e. O-1502, 39% inhibition at 0.1 mM
1-palmitin
-
44% inhibition of the membraneous enzyme at 0.1 mM, 38% inhibition of the cytosolic enzyme at 0.1 mM
15-deoxy-DELTA12,14-prostaglandin J2
-
-
2,3-dihydroxypropyl (11Z)-icos-11-enoate
-
i.e. O-4066, IC50 value for the membraneous enzyme is 0.026 mM, for the cytosolic enzyme 0.019 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 79%
2,3-dihydroxypropyl (11Z,14Z)-icosa-11,14-dienoate
-
i.e. O-3907, IC50 value for the membraneous enzyme is 0.016 mM, for the cytosolic enzyme 0.0051 mM, complete inhibition is possible
2,3-dihydroxypropyl (4Z,7Z,10Z,13Z)-17-ethylcycloheptadeca-4,7,10,13-tetraene-1-carboxylate
-
i.e. O-1428, IC50 value for the membraneous enzyme is 0.071 mM, for the cytosolic enzyme 0.015 mM, complete inhibition is possible
2,3-dihydroxypropyl (5Z)-icos-5-enoate
-
i.e. 3908, IC50 value for the membraneous enzyme is 0.056 mM, for the cytosolic enzyme 0.021 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 65%
2,3-dihydroxypropyl (5Z,8Z,11Z)-2-ethylcycloheptadeca-5,8,11-triene-1-carboxylate
-
i.e. O-3973, IC50 value for the membraneous enzyme is 0.0083 mM, for the cytosolic enzyme 0.0042 mM, complete inhibition is possible
2,3-dihydroxypropyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate
-
i.e. O-3832, IC50 value for the membraneous enzyme is 0.017 mM, for the cytosolic enzyme 0.0082 mM, complete inhibition is possible
2,3-dihydroxypropyl (6Z,9Z,12Z,15Z)-cyclohenicosa-6,9,12,15-tetraene-1-carboxylate
-
IC50 value for the membraneous enzyme is 0.0051 mM, for the cytosolic enzyme 0.0058 mM, complete inhibition is possible
2,3-dihydroxypropyl (7Z,10Z,13Z,16Z)-docosa-7,10,13,16-tetraenoate
-
IC50 value for the membraneous enzyme is 0.011 mM, for the cytosolic enzyme 0.0045 mM, complete inhibition is possible
2,3-dihydroxypropyl (8Z,11Z,14Z)-icosa-8,11,14-trienoate
-
i.e. 3846, IC50 value for the membraneous enzyme is 0.073 mM, for the cytosolic enzyme 0.0075 mM, complete inhibition is possible
2-arachidonoylglycerol
-
inhibits the hydrolysis of cytosolic 2-oleoylglycerol, IC50 value is 0.013 mM, the affinity for the enzyme is highest with an arachidonyl side chain and decreases to fatty acids of shorter chain length
2-methyl-4-isothiazolin-3-one
-
-
2-octyl-4-isothiazolin-3-one
2-octyl-benzo[d]isothiazol-3-one
-
-
2-oleoyl-4-isothiazolin-3-one
-
-
3-methoxy-N-phenyl-1,2,4-thiadiazol-5-amine
-
weak inhibitory effect
4-nitrophenyl 4-[bis(1,3-benzodioxol-5-yl)hydroxymethyl]piperidine-1-carboxylate
-
JZL184
6-methyl-2-p-tolylamino-benzo[d] [1,3]oxazin-4-one
-
i.e. URB754
6-methyl-2-[(4-methylphenyl)amino]-4H-3,1-benzoxazin-4-one
-
URB754, inhibition of brain MAGL expressed in HeLa cells, no inhibition of membrane-bound MAGL. Is not selective for MAGL
alpha-methyl-1-arachidonoyl glycerol
-
compound O-1428, inhibits both cytosolic and membrane-bound MAGL
alpha-methyl-1-arachidonoylglycerol
-
IC50 value is 0.011 mM
arachidonic acid
-
IC50 value is 0.078 mM
arachidonoyl glycine
-
42% inhibition at 0.1 mM
arachidonoyl serinol
-
IC50 value is 0.073 mM
arachidonoyl trifluoromethylketone
arachidonoyltrifluoromethyl ketone
-
i.e. ATFMK, inhibition is reversible by AM281
celastrol
-
inhibits MGL activity, albeit less potently than pristimerin
chlorpyrifos oxon
-
is not selective for MAGL
dihydrocelastrol
-
inhibits MGL activity, albeit less potently than pristimerin
dihydrocelastryl diacetate
-
inhibits MGL activity, albeit less potently than pristimerin
diisopropyl fluorophosphate
-
-
ethyl octylphosphonofluoridate
-
is not selective for MAGL
euphol
-
inhibits MGL activity with high potency. Blocks MGL activity through a reversible and noncompetitive mechanism, which is apparently identical to that of pristimerin
hexadecylsufonyl fluoride
isopropyl dodecylfluorophosphonate
-
is not selective for MAGL
methyl arachidonyl fluorophosphonate
methyl octylphosphonofluoridate
-
is not selective for MAGL
N-(2-hydroxyethyl)-2-oxopentadecanamide
-
exhibits weak inhibitory activity (27.5%) and no selectivity towards MGL
N-(4-hydroxy-2-methylphenyl)arachidonylamide
-
i.e. VDM11, an anandamide uptake inhibitor, substrate of fatty acid amide hydrolase, EC 3.5.1.4, IC50 is 0.021 mM
N-(4-hydroxyphenyl)arachidonylamide
-
i.e. AM404, an anandamide uptake inhibitor, substrate of fatty acid amide hydrolase, EC 3.5.1.4, IC50 is 0.020 mM
N-arachidonoyl dopamine
-
-
noladin ether
-
IC50 value is 0.036 mM
phenylmethylsulfonyl fluoride
-
50% inhibition at 0.155 mM
pristimerin
-
inhibits MGL activity with high potency. Addition to purified MGL produces an almost immediate blockade of MGL activity. Inhibits MGL through a mechanism that is rapid, reversible, and noncompetitive
pristimerol
-
inhibits MGL activity, albeit less potently than pristimerin
S-nonylbenzodioxaphosphorin oxide
-
is not selective for MAGL
URB-602
-
a specific MGL inhibitor
[1,1'-biphenyl]-3-yl-carbamic acid, cyclohexyl ester
-
URB602, noncompetetive selective inhibitor
[4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3-yl)-2-methylphenyl]carbamic acid benzyl ester
-
CAY10499
1-arachidonoylglycerol
-
IC50 value for the membraneous enzyme is 0.0095 mM, for the cytosolic enzyme 0.0071 mM, complete inhibition is possible
1-arachidonoylglycerol
-
inhibits the hydrolysis of cytosolic 2-oleoylglycerol, IC50 value is 0.017 mM, the affinity for the enzyme is highest with an arachidonyl side chain and decreases to fatty acids of shorter chain length
2-octyl-4-isothiazolin-3-one
-
-
2-octyl-4-isothiazolin-3-one
-
octhilinone, inhibits purified recombinant MGL through a partially reversible mechanism that involves a specific interaction with cysteine 208
arachidonoyl trifluoromethylketone
-
50% inhibition at 0.0025 mM
arachidonoyl trifluoromethylketone
-
50% inhibition at 0.066 mM
arachidonoyl trifluoromethylketone
-
the affinity for the enzyme is highest with an arachidonyl side chain and decreases to fatty acids of shorter chain length
arachidonoyl trifluoromethylketone
-
causes a gradual suppression of cannabinoid-sensitive IPSCs in cultured hippocampal neurons, the suppression is reversed by blocking CB1 receptors and is attenuated by inhibiting 2-AG synthesis, overview
hexadecylsufonyl fluoride
-
50% inhibition at 0.000241 mM
hexadecylsufonyl fluoride
-
50% inhibition at 0.0062 mM
JZL184
-
irreversible inhibitor
JZL184
-
time-dependent inhibitor
methyl arachidonyl fluorophosphonate
-
50% inhibition at 0.0000022 mM
methyl arachidonyl fluorophosphonate
-
50% inhibition at 0.0008 mM
methyl arachidonyl fluorophosphonate
-
i.e. MAFP, inhibits at 0.05 mM
methyl arachidonyl fluorophosphonate
-
i.e. MAFP
methyl arachidonyl fluorophosphonate
-
causes a gradual suppression of cannabinoid-sensitive IPSCs in cultured hippocampal neurons, the suppression is reversed by blocking CB1 receptors and is attenuated by inhibiting 2-AG synthesis, overview
methyl arachidonyl fluorophosphonate
-
MAFP
N-arachidonylmaleimide
-
-
N-arachidonylmaleimide
-
inhibitory effect is attributed to the ability of this compound to react with C242 and form a Michael addition product
N-arachidonylmaleimide
-
inhibits membrane-bound MAGL selectively
URB602
-
-
URB602
-
reversible inhibitor
additional information
inhibition by bulky maleimides derivatives is due to steric hindrance of substrate binding after alkylation of cysteines 242 and/or 208, no inhibition by succimide and N-arachidonylsuccimide
-
additional information
-
immunodepletion of the recombinant enzyme leads to 50% reduced activity
-
additional information
-
inhibitory potency of different 1-arachidonic acid analogues, the chain length of the fatty acid is important for affinity and inhibition, while methylations of the fatty acids do not influence the inhibitory potency, overview
-
additional information
-
no inhibition by URB597, bovine serum albumin decreases the inhibitory effect of arachidonoyl-based compounds, e.g. VDM11
-
additional information
-
inhibitor screening, overview
-
additional information
-
inhibitors of other endocannabinoid hydrolyzing enzymes, fatty acid amide hydrolase and cyclooxygenase-2, have no effect on the 2-AG-induced IPSC suppression
-
additional information
-
3-methoxy-N-phenyl-1,2,4-thiadiazol-5-amine and 3-propoxy-2-benzofuran-1(3H)-one do not inhibit
-
additional information
-
(2S)-6-phenylhexane-1,2-diamine and (2S,9Z)-2-aminooctadec-9-enamide show no inhibition
-
additional information
-
is not inhibited by 1 mM N-arachidonylsuccinimide
-
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0.072
4-chlormercurybenzoate
Rattus norvegicus
IC50 value is 0.072 mM
0.042
HgCl2
Rattus norvegicus
IC50 value is 0.042 mM
0.07
Maleimide
Rattus norvegicus
IC50 value is 0.070 mM
0.068
N-(1-pyrenyl)-maleimide
Rattus norvegicus
IC50 value is 0.068 mM
0.00014
N-arachidonoylmaleimide
Rattus norvegicus
IC50 value is 0.00014 mM
0.051
N-cyclohexylmaleimide
Rattus norvegicus
IC50 value is 0.051 mM
0.413
N-hydroxymaleimide
Rattus norvegicus
IC50 value is 0.413 mM
0.044
N-Phenylmaleimide
Rattus norvegicus
IC50 value is 0.044 mM
0.053
N-propylmaleimide
Rattus norvegicus
IC50 value is 0.053 mM
0.053
NEM
Rattus norvegicus
IC50 value is 0.053 mM
0.02
(5E)-5-(3-methylbutylidene)-2-thioxo-1,3-thiazolidin-4-one
Rattus norvegicus
-
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free
0.0095 - 0.017
1-arachidonoylglycerol
0.032
1-myristin
Rattus norvegicus
-
IC50 value for the membraneous and the cytosolic enzyme is 0.032 mM, complete inhibition is possible
0.026
2,3-dihydroxypropyl (11Z)-icos-11-enoate
Rattus norvegicus
-
i.e. O-4066, IC50 value for the membraneous enzyme is 0.026 mM, for the cytosolic enzyme 0.019 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 79%
0.016
2,3-dihydroxypropyl (11Z,14Z)-icosa-11,14-dienoate
Rattus norvegicus
-
i.e. O-3907, IC50 value for the membraneous enzyme is 0.016 mM, for the cytosolic enzyme 0.0051 mM, complete inhibition is possible
0.071
2,3-dihydroxypropyl (4Z,7Z,10Z,13Z)-17-ethylcycloheptadeca-4,7,10,13-tetraene-1-carboxylate
Rattus norvegicus
-
i.e. O-1428, IC50 value for the membraneous enzyme is 0.071 mM, for the cytosolic enzyme 0.015 mM, complete inhibition is possible
0.056
2,3-dihydroxypropyl (5Z)-icos-5-enoate
Rattus norvegicus
-
i.e. 3908, IC50 value for the membraneous enzyme is 0.056 mM, for the cytosolic enzyme 0.021 mM, complete inhibition of the membraneous enzyme is possible, maximal inhibition of the cytosolic enzyme of 65%
0.0083
2,3-dihydroxypropyl (5Z,8Z,11Z)-2-ethylcycloheptadeca-5,8,11-triene-1-carboxylate
Rattus norvegicus
-
i.e. O-3973, IC50 value for the membraneous enzyme is 0.0083 mM, for the cytosolic enzyme 0.0042 mM, complete inhibition is possible
0.017
2,3-dihydroxypropyl (5Z,8Z,11Z,14Z,17Z)-icosa-5,8,11,14,17-pentaenoate
Rattus norvegicus
-
i.e. O-3832, IC50 value for the membraneous enzyme is 0.017 mM, for the cytosolic enzyme 0.0082 mM, complete inhibition is possible
0.0051
2,3-dihydroxypropyl (6Z,9Z,12Z,15Z)-cyclohenicosa-6,9,12,15-tetraene-1-carboxylate
Rattus norvegicus
-
IC50 value for the membraneous enzyme is 0.0051 mM, for the cytosolic enzyme 0.0058 mM, complete inhibition is possible
0.011
2,3-dihydroxypropyl (7Z,10Z,13Z,16Z)-docosa-7,10,13,16-tetraenoate
Rattus norvegicus
-
IC50 value for the membraneous enzyme is 0.011 mM, for the cytosolic enzyme 0.0045 mM, complete inhibition is possible
0.073
2,3-dihydroxypropyl (8Z,11Z,14Z)-icosa-8,11,14-trienoate
Rattus norvegicus
-
i.e. 3846, IC50 value for the membraneous enzyme is 0.073 mM, for the cytosolic enzyme 0.0075 mM, complete inhibition is possible
0.013
2-arachidonoylglycerol
Rattus norvegicus
-
inhibits the hydrolysis of cytosolic 2-oleoylglycerol, IC50 value is 0.013 mM, the affinity for the enzyme is highest with an arachidonyl side chain and decreases to fatty acids of shorter chain length
0.000239
2-methyl-4-isothiazolin-3-one
Rattus norvegicus
-
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free
0.000151 - 0.000722
2-octyl-4-isothiazolin-3-one
0.000059
2-octyl-benzo[d]isothiazol-3-one
Rattus norvegicus
-
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free
0.000043
2-oleoyl-4-isothiazolin-3-one
Rattus norvegicus
-
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free
0.028
3-methoxy-N-phenyl-1,2,4-thiadiazol-5-amine
Rattus norvegicus
-
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free
0.0002
6-methyl-2-[(4-methylphenyl)amino]-4H-3,1-benzoxazin-4-one
Rattus norvegicus
-
MAGL expressed in HeLa cells
0.01 - 0.071
alpha-methyl-1-arachidonoyl glycerol
0.011
alpha-methyl-1-arachidonoylglycerol
Rattus norvegicus
-
IC50 value is 0.011 mM
0.078
arachidonic acid
Rattus norvegicus
-
IC50 value is 0.078 mM
0.073
arachidonoyl serinol
Rattus norvegicus
-
IC50 value is 0.073 mM
0.0016
celastrol
Rattus norvegicus
-
purified MGL, at pH 7.5, 37°C
0.000034
chlorpyrifos oxon
Rattus norvegicus
-
cytosolic MAGL
0.015
dihydrocelastrol
Rattus norvegicus
-
purified MGL, at pH 7.5, 37°C
0.015
dihydrocelastryl diacetate
Rattus norvegicus
-
purified MGL, at pH 7.5, 37°C
0.000003
ethyl octylphosphonofluoridate
Rattus norvegicus
-
cytosolic MAGL
0.000315 - 0.000882
euphol
0.00000076
isopropyl dodecylfluorophosphonate
Rattus norvegicus
-
cytosolic MAGL
0.000003
methyl octylphosphonofluoridate
Rattus norvegicus
-
cytosolic MAGL
0.021
N-(4-hydroxy-2-methylphenyl)arachidonylamide
Rattus norvegicus
-
i.e. VDM11, an anandamide uptake inhibitor, substrate of fatty acid amide hydrolase, EC 3.5.1.4, IC50 is 0.021 mM
0.02
N-(4-hydroxyphenyl)arachidonylamide
Rattus norvegicus
-
i.e. AM404, an anandamide uptake inhibitor, substrate of fatty acid amide hydrolase, EC 3.5.1.4, IC50 is 0.020 mM
0.00003 - 0.000442
N-arachidonylmaleimide
0.0027
N-ethylmaleimide
Rattus norvegicus
-
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free
0.036
noladin ether
Rattus norvegicus
-
IC50 value is 0.036 mM
0.000093 - 0.000398
pristimerin
0.004
pristimerol
Rattus norvegicus
-
purified MGL, at pH 7.5, 37°C
0.00000031
S-nonylbenzodioxaphosphorin oxide
Rattus norvegicus
-
cytosolic MAGL
0.031
SPB 01403
Rattus norvegicus
-
-
0.00041
troglitazone
Rattus norvegicus
-
pH and temperature not specified in the publication
0.028 - 0.075
[1,1'-biphenyl]-3-yl-carbamic acid, cyclohexyl ester
0.0095
1-arachidonoylglycerol
Rattus norvegicus
-
IC50 value for the membraneous enzyme is 0.0095 mM, for the cytosolic enzyme 0.0071 mM, complete inhibition is possible
0.017
1-arachidonoylglycerol
Rattus norvegicus
-
inhibits the hydrolysis of cytosolic 2-oleoylglycerol, IC50 value is 0.017 mM, the affinity for the enzyme is highest with an arachidonyl side chain and decreases to fatty acids of shorter chain length
0.000151
2-octyl-4-isothiazolin-3-one
Rattus norvegicus
-
wild-type, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free
0.000722
2-octyl-4-isothiazolin-3-one
Rattus norvegicus
-
mutant C208G, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free
0.01
alpha-methyl-1-arachidonoyl glycerol
Rattus norvegicus
-
cytosolic MAGL
0.015
alpha-methyl-1-arachidonoyl glycerol
Rattus norvegicus
-
cytosolic MAGL
0.071
alpha-methyl-1-arachidonoyl glycerol
Rattus norvegicus
-
membrane-bound MAGL
0.000315
euphol
Rattus norvegicus
-
purified MG, at pH 7.5, 37°CL
0.000882
euphol
Rattus norvegicus
-
nonpurified MGL, at pH 7.5, 37°C
0.00003
N-arachidonylmaleimide
Rattus norvegicus
-
wild-type, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free
0.000046
N-arachidonylmaleimide
Rattus norvegicus
-
recombinant purified enzyme, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/mlL bovine serum albumin, fatty acid-free
0.000107
N-arachidonylmaleimide
Rattus norvegicus
-
mutant C242G, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free
0.00014
N-arachidonylmaleimide
Rattus norvegicus
-
membrane-bound MAGL
0.000442
N-arachidonylmaleimide
Rattus norvegicus
-
mutant C201G, for 10 min at 37°C, in 50 mM Tris-HCl, pH 8.0, 0.5 mg/ml bovine serum albumin, fatty acid-free
0.000093
pristimerin
Rattus norvegicus
-
purified MGL, at pH 7.5, 37°C
0.000398
pristimerin
Rattus norvegicus
-
nonpurified MGL, at pH 7.5, 37°C
0.028
[1,1'-biphenyl]-3-yl-carbamic acid, cyclohexyl ester
Rattus norvegicus
-
cytosolic MAGL
0.075
[1,1'-biphenyl]-3-yl-carbamic acid, cyclohexyl ester
Rattus norvegicus
-
MAGL expressed in HeLa cells
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Karlsson, M.; Contreras, J.A.; Hellman, U.; Tornqvist, H.; Holm, C.
cDNA cloning, tissue distribution, and identification of the catalytic triad of monoglyceride lipase
J. Biol. Chem.
272
27218-27223
1997
Mus musculus, Rattus norvegicus
brenda
Fredrikson, G.; Tornqvist, H.; Belfrage, P.
Hormone-sensitive lipase and monoacylglycerol lipase are both required for complete degradation of adipocyte triacylglycerol
Biochim. Biophys. Acta
876
288-293
1986
Rattus norvegicus
brenda
Errasfa, M.
Characterization of several phospholipase activities and diacylglycerol/2-monoacylglycerol lipases in rat alveolar macrophages
Biochim. Biophys. Acta
1085
201-208
1991
Rattus norvegicus
brenda
Konrad, R.J.; Major, C.D.; Wolf, B.A.
Diacylglycerol hydrolysis to arachidonic acid is necessary for insulin secretion from isolated pancreatic islets: sequential actions of diacylglycerol and monoacylglycerol lipases
Biochemistry
33
13284-13294
1994
Rattus norvegicus
brenda
Sakurada, T.; Noma, A.
Subcellular localization and some properties of monoacylglycerol lipase in rat adipocytes
J. Biochem.
90
1413-1419
1981
Rattus norvegicus
brenda
Tornqvist, H.; Belfrage, P.
Monoacylglycerol lipase from rat adipose tissue
Methods Enzymol.
71
647-652
1981
Rattus norvegicus
-
brenda
De Jong, B.J.P.; Kalkman, C.; Hulsmann, W.C.
Partial purification and properties of monoacylglycerol lipase and two esterases from isolated rat small intestinal epithelial cells
Biochim. Biophys. Acta
530
56-66
1978
Rattus norvegicus
brenda
Ikeda, Y.; Okamura, K.; Fujii, S.
Purification and characterization of rat liver microsomal monoacylglycerol lipase in comparison to the other esterases
Biochim. Biophys. Acta
488
128-139
1977
Rattus norvegicus
brenda
Saario, S.M.; Savinainen, J.R.; Laitinen, J.T.; Jarvinen, T.; Niemi, R.
Monoglyceride lipase-like enzymatic activity is responsible for hydrolysis of 2-arachidonoylglycerol in rat cerebellar membranes
Biochem. Pharmacol.
67
1381-1387
2004
Rattus norvegicus
brenda
Dinh, T.P.; Freund, T.F.; Piomelli, D.
A role for monoglyceride lipase in 2-arachidonoylglycerol inactivation
Chem. Phys. Lipids
121
149-158
2002
Rattus norvegicus
brenda
Ito, M.; Tchoua, U.; Okamoto, M.; Tojo, H.
Purification and properties of a phospholipase A2/lipase preferring phosphatidic acid, bis(monoacylglycerol) phosphate, and monoacylglycerol from rat testis
J. Biol. Chem.
277
43674-43681
2002
Rattus norvegicus
brenda
Dinh, T.P.; Carpenter, D.; Leslie, F.M.; Freund, T.F.; Katona, I.; Sensi, S.L.; Kathuria, S.; Piomelli, D.
Brain monoglyceride lipase participating in endocannabinoid inactivation
Proc. Natl. Acad. Sci. USA
99
10819-10824
2002
Rattus norvegicus (Q8R431)
brenda
Vandevoorde, S.; Saha, B.; Mahadevan, A.; Razdan, R.K.; Pertwee, R.G.; Martin, B.R.; Fowler, C.J.
Influence of the degree of unsaturation of the acyl side chain upon the interaction of analogues of 1-arachidonoylglycerol with monoacylglycerol lipase and fatty acid amide hydrolase
Biochem. Biophys. Res. Commun.
337
104-109
2005
Rattus norvegicus
brenda
Ghafouri, N.; Tiger, G.; Razdan, R.K.; Mahadevan, A.; Pertwee, R.G.; Martin, B.R.; Fowler, C.J.
Inhibition of monoacylglycerol lipase and fatty acid amide hydrolase by analogues of 2-arachidonoylglycerol
Br. J. Pharmacol.
143
774-784
2004
Rattus norvegicus
brenda
Vandevoorde, S.; Fowler, C.J.
Inhibition of fatty acid amide hydrolase and monoacylglycerol lipase by the anandamide uptake inhibitor VDM11: evidence that VDM11 acts as an FAAH substrate
Br. J. Pharmacol.
145
885-893
2005
Rattus norvegicus
brenda
Saario, S.M.; Salo, O.M.; Nevalainen, T.; Poso, A.; Laitinen, J.T.; Jarvinen, T.; Niemi, R.
Characterization of the sulfhydryl-sensitive site in the enzyme responsible for hydrolysis of 2-arachidonoyl-glycerol in rat cerebellar membranes
Chem. Biol.
12
649-656
2005
Rattus norvegicus (Q8R431)
brenda
Dinh, T.P.; Kathuria, S.; Piomelli, D.
RNA interference suggests a primary role for monoacylglycerol lipase in the degradation of the endocannabinoid 2-arachidonoylglycerol
Mol. Pharmacol.
66
1260-1264
2004
Homo sapiens, Rattus norvegicus
brenda
Vila, A.; Rosengarth, A.; Piomelli, D.; Cravatt, B.; Marnett, L.J.
Hydrolysis of prostaglandin glycerol esters by the endocannabinoid-hydrolyzing enzymes, monoacylglycerol lipase and fatty acid amide hydrolase
Biochemistry
46
9578-9585
2007
Rattus norvegicus
brenda
Saario, S.M.; Poso, A.; Juvonen, R.O.; Jaervinen, T.; Salo-Ahen, O.M.
Fatty acid amide hydrolase inhibitors from virtual screening of the endocannabinoid system
J. Med. Chem.
49
4650-4656
2006
Homo sapiens, Rattus norvegicus
brenda
Hashimotodani, Y.; Ohno-Shosaku, T.; Kano, M.
Presynaptic monoacylglycerol lipase activity determines basal endocannabinoid tone and terminates retrograde endocannabinoid signaling in the hippocampus
J. Neurosci.
27
1211-1219
2007
Mus musculus, Mus musculus C57BL/6, Rattus norvegicus
brenda
Duncan, M.; Thomas, A.D.; Cluny, N.L.; Patel, A.; Patel, K.D.; Lutz, B.; Piomelli, D.; Alexander, S.P.; Sharkey, K.A.
Distribution and function of monoacylglycerol lipase in the gastrointestinal tract
Am. J. Physiol. Gastrointest. Liver Physiol.
295
G1255-G1265
2008
Mus musculus, Rattus norvegicus
brenda
Zvonok, N.; Williams, J.; Johnston, M.; Pandarinathan, L.; Janero, D.R.; Li, J.; Krishnan, S.C.; Makriyannis, A.
Full mass spectrometric characterization of human monoacylglycerol lipase generated by large-scale expression and single-step purification
J. Proteome Res.
7
2158-2164
2008
Rattus norvegicus (Q8R431), Homo sapiens (Q99685), Homo sapiens
brenda
Holtfrerich, A.; Makharadze, T.; Lehr, M.
High-performance liquid chromatography assay with fluorescence detection for the evaluation of inhibitors against human recombinant monoacylglycerol lipase
Anal. Biochem.
399
218-224
2010
Homo sapiens, Mus musculus, Rattus norvegicus
brenda
Magrioti, V.; Naxakis, G.; Hadjipavlou-Litina, D.; Makriyannis, A.; Kokotos, G.
A novel monoacylglycerol lipase inhibitor with analgesic and anti-inflammatory activity
Bioorg. Med. Chem. Lett.
18
5424-5427
2008
Rattus norvegicus
brenda
King, A.R.; Lodola, A.; Carmi, C.; Fu, J.; Mor, M.; Piomelli, D.
A critical cysteine residue in monoacylglycerol lipase is targeted by a new class of isothiazolinone-based enzyme inhibitors
Br. J. Pharmacol.
157
974-983
2009
Rattus norvegicus
brenda
King, A.R.; Dotsey, E.Y.; Lodola, A.; Jung, K.M.; Ghomian, A.; Qiu, Y.; Fu, J.; Mor, M.; Piomelli, D.
Discovery of potent and reversible monoacylglycerol lipase inhibitors
Chem. Biol.
16
1045-1052
2009
Rattus norvegicus
brenda
Vandevoorde, S.
Overview of the chemical families of fatty acid amide hydrolase and monoacylglycerol lipase inhibitors
Curr. Top. Med. Chem.
8
247-267
2008
Homo sapiens, Mus musculus, Rattus norvegicus
brenda
Bjoerklund, E.; Noren, E.; Nilsson, J.; Fowler, C.J.
Inhibition of monoacylglycerol lipase by troglitazone, N-arachidonoyl dopamine and the irreversible inhibitor JZL184: comparison of two different assays
Br. J. Pharmacol.
161
1512-1526
2010
Homo sapiens, Rattus norvegicus
brenda
Guindon, J.; Guijarro, A.; Piomelli, D.; Hohmann, A.G.
Peripheral antinociceptive effects of inhibitors of monoacylglycerol lipase in a rat model of inflammatory pain
Br. J. Pharmacol.
163
1464-1478
2011
Rattus norvegicus
brenda
Berdan, C.A.; Erion, K.A.; Burritt, N.E.; Corkey, B.E.; Deeney, J.T.
Inhibition of monoacylglycerol lipase activity decreases glucose-stimulated insulin secretion in INS-1 (832/13) cells and rat islets
PLoS ONE
11
e0149008
2016
Rattus norvegicus (Q8R431), Rattus norvegicus Sprague-Dawley (Q8R431)
brenda