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3.1.1.23: acylglycerol lipase

This is an abbreviated version!
For detailed information about acylglycerol lipase, go to the full flat file.

Word Map on EC 3.1.1.23

Reaction

CnHmCO-C3O3H7
+
H2O
=
CnHmCO2H
 +
glycerol

Synonyms

AtMAGL, AtMAGL1, AtMAGL10, AtMAGL11, AtMAGL14, AtMAGL15, AtMAGL16, AtMAGL2, AtMAGL3, AtMAGL4, AtMAGL5, AtMAGL6, AtMAGL7, AtMAGL8, AtMAGL9, fatty acyl monoester lipase, glycerol-monoester acylhydrolase, HMGL, LH57_01015, lipase, lipase G, LipB, lipozyme IM, MAG hydrolase, MAG lipase, MAGL, MAGL-cy, MAGL-m, MAGL16, MAGL6, MAGL8, MGH, MGL, MGL Rv0183, MGL-like activity, MGLL, MGLP, monoacylglycerol hydrolase, monoacylglycerol lipase, monoglycerid lipase, monoglyceridase, monoglyceride hydrolase, monoglyceride lipase, monoglyceride lipase-like activity, monoglyceridyllipase, MSMEG_0220, mtbMGL, patatin-like protein 1, patatin-like protein 16, patatin-like protein 2, patatin-like protein 3, patatin-like protein 4, patatin-like protein 5, patatin-like protein 6, patatin-like protein 7, patatin-like protein 8, patatin-like protein 9, PLP1, PLP16, PLP2, PLP3, PLP4, PLP5, PLP6, PLP7, PLP8, PLP9, Rv0183, Rv0183 protein, Yju3p

ECTree

     3 Hydrolases
         3.1 Acting on ester bonds
             3.1.1 Carboxylic-ester hydrolases
                3.1.1.23 acylglycerol lipase

Inhibitors

Inhibitors on EC 3.1.1.23 - acylglycerol lipase

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INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(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
(3R)-1-(3,4-dimethylphenyl)-5-oxo-N-[(4-oxo-3,4-dihydrophthalazin-1-yl)methyl]pyrrolidine-3-carboxamide
51.85% residual activity at 0.1 mM
(3R)-N-(3,5-dimethylphenyl)-1-[2-(5-fluoro-1H-indol-3-yl)ethyl]-5-oxopyrrolidine-3-carboxamide
18.61% residual activity at 0.1 mM
(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one
-
16% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
(3S)-N-(1,3-benzodioxol-4-ylmethyl)-1-[4-[(2-chlorobenzyl)oxy]phenyl]-5-oxopyrrolidine-3-carboxamide
51.09% residual activity at 0.1 mM
(4-(4-chlorobenzoyl)piperidin-1-yl)(4-methoxyphenyl)-methanone
-
(4-amidinophenyl) methanesulfonyl fluoride
-
i.e. APMSF, inhibits at 0.5 mM
(4-[4-chlorobenzoyl]piperidin-1-yl)(4-methoxyphenyl)-methanone
-
(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-(3-phenylpropanoyl)-(3R,4R)-3-[1(R)-(3-phenylpropanoyloxy)-ethyl]-4-(acetoxy)-azetidin-2-one
-
100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(3-phenylpropanoyl)-(3R,4R)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-4-(acetoxy)-azetidin-2-one
-
100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(3-phenylpropanoyl)-(3R,4R)-3-[1(R)-(biphenylacetyloxy)-ethyl]-4-(acetoxy)-azetidin-2-one
-
100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0; 66% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(3-phenylpropanoyl)-(3S)-3-[1(R)-(3-phenylpropanoyloxy)-ethyl]-azetidin-2-one
-
100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(3-phenylpropanoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one
-
100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(3-phenylpropanoyl)-(3S)-3-[1(R)-(5-phenylpentanoyloxy)-ethyl]-azetidin-2-one
-
100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(3-phenylpropanoyl)-(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one
-
31% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(4-phenylbutanoyl)-(3R,4R)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-4-(acetoxy)-azetidin-2-one
-
100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(4-phenylbutanoyl)-(3R,4R)-3-[1(R)-hydroxyethyl]-4-(acetoxy)-azetidin-2-one
-
61% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(4-phenylbutanoyl)-(3S)-3-[1(R)-(3-phenylpropanoyloxy)-ethyl]-azetidin-2-one
-
54% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(4-phenylbutanoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one
-
100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(4-phenylbutanoyl)-(3S)-3-[1(R)-(5-phenylpentanoyloxy)-ethyl]-azetidin-2-one
-
59% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(5-phenylpentanoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one
-
39% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(5-phenylpentanoyl)-(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one
-
25% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(hexa-5-enoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one
-
85% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(hexa-5-enoyl)-(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one
-
67% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(pent-4-enoyl)-(3R,4R)-3-[1(R)-(pent-4-enoyloxy)-ethyl]-4-(acetoxy)-azetidin-2-one
-
99% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(pent-4-enoyl)-(3R,4R)-3-[1(R)-hydroxyethyl]-4-(acetoxy)-azetidin-2-one
-
16% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0; 8% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(pent-4-enoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one
-
89% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(pent-4-enoyl)-(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one
-
91% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(pent-4-enoyl)-(3S)-3-[1(R)-(hexa-5-enoyloxy)-ethyl]-azetidin-2-one
-
8% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(pent-4-enoyl)-(3S)-3-[1(R)-(pent-4-enoyloxy)-ethyl]-azetidin-2-one
-
99% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-(pent-4-enoyl)-(3S)-3-[1(R)-hydroxyethyl]-azetidin-2-one
-
89% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0
1-arachidin
-
11% inhibition of the membraneous enzyme at 0.1 mM, 19% inhibition of the cytosolic enzyme at 0.1 mM
1-arachidonoylglycerol
1-methylethyl dodecylphosphonofluoridoate
-
highly potent inhibitor
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
12-deacetylsplendidin C
poor inhibition
15-deoxy-DELTA12,14-prostaglandin J2
1H-benzotriazol-1-yl(4-benzylpiperazin-1-yl)methanone
-
1H-benzotriazol-1-yl[4-(4-bromobenzyl)piperazin-1-yl]methanone
-
1H-benzotriazol-1-yl[4-(4-nitrobenzyl)piperazin-1-yl]methanone
-
1H-benzotriazol-1-yl[4-(naphthalen-2-ylmethyl)piperazin-1-yl]methanone
-
1H-benzotriazol-1-yl[4-[(2E)-3-phenylprop-2-en-1-yl]piperazin-1-yl]methanone
-
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-(4-hydroxyphenyl)ethyl alpha-L-rhamnopyranosyl-(1->3)-[alpha-L-rhamnopyranosyl-(1->6)]-2-O-acetyl-4-O-(4-coumaroyl)-beta-D-glucopyranoside
-
2-(4-hydroxyphenyl)ethyl alpha-L-rhamnopyranosyl-(1->3)-[alpha-L-rhamnopyranosyl-(1->6)]-2-O-acetyl-4-O-beta-D-glucopyranoside
the inhibitor is selective for hMAGL over hLDH, modeling of the binding mode in the MAGL active site. The sugar moiety lies in the wide lipophilic cavity of the protein forming lipophilic interactions with L148, L213, L241, and V183, whereas the 4-hydroxyphenyl-ethyl ring lies into the small pocket of the binding site and forms lipophilic interactions with residues Y194 and V270. A high number of H-bonds stabilizes the binding disposition of the compound
2-(4-hydroxyphenyl)ethyl alpha-L-rhamnopyranosyl-(1->3)-[alpha-L-rhamnopyranosyl-(1->6)]-beta-D-glucopyranoside
-
2-(7-methoxy-2-oxo-2H-chromen-3-yl)-N-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxamide
-
2-(nonylsulfanyl)-4H-1,3,2-benzodioxaphosphinine 2-oxide
-
-
2-arachidonoylglycerol
2-dehydroxysalvileucanthsin A
poor inhibition
2-mercaptoethanol
-
50% residual activity at 1 mM
2-methyl-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
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
3-[(4S)-1-[2-(5-fluoro-1H-indol-3-yl)ethyl]-2,5-dioxoimidazolidin-4-yl]-N-[(1R,2R)-2-methylcyclohexyl]propanamide
57.6% residual activity at 0.1 mM
4-chlormercurybenzoate
IC50 value is 0.072 mM
4-chloromercuribenzoic acid
-
-
4-cyanophenyl ethyl dodecylphosphonate
-
highly potent inhibitor
4-nitrophenyl 4-[bis(1,3-benzodioxol-5-yl)hydroxymethyl]piperidine-1-carboxylate
4-nitrophenyl dodecyl(1-methylethyl)phosphinate
-
-
5-[(biphenyl-4-yl)methyl]-N,N-dimethyl-2H-tetrazole-2-carboxamide
AM6701, conforms to the L shape of the binding site, contacts with the binding site are similar to those seen with the 2-arachidonoylglycerol docking pose. The close contacts with A164 and K165 are lost as the subpocket is not occupied. Instead the biphenyl moiety, which extends further up the binding pocket, makes additional contacts with A156, T157 and K160, thus AM6701 is a non-selective inhibitor
6-methyl-2-p-tolylamino-benzo[d] [1,3]oxazin-4-one
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
AM404
AM6580
-
irreversible inhibitor, i.e. [4-(9H-fluoren-9-yl)-piperazin-1-yl][1,2,3]triazolo[4,5-b]pyridin-1-ylmethanone
AM6701
AM6702
-
-
apolipoprotein A-1
-
-
-
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
arachidonoyltrifluoromethylketone
-
-
arachidonyl trifluoromethylketone
-
-
ATP
-
slightly inhibiting
benzol
-
IC50 is 0.012 mM
benzyl [4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3(2H)-yl)-2-methylphenyl]carbamate
5.12% residual activity at 0.1 mM
benzylphenylcarbamate
-
-
biphenyl-3-yl-carbamic acid cyclohexyl ester
-
i.e. URB602
brandioside
-
CAY 10415
CAY 10514
CAY10499
-
-
celastrol
-
inhibits MGL activity, albeit less potently than pristimerin
chlorpyrifos oxon
ciglitazone
Co2+
-
47% residual activity at 1 mM
CP55,940
Cu2+
-
35% residual activity at 1 mM
decyl benzodioxaphosphorin oxide
-
IC50 is 0.80 nM
deoxycholate
-
17% inhibition at 5 mM
diazoxon
-
IC50 is 0.014 mM
dichlorvos
-
IC50 is 0.013 mM
diethyl 3,5,6-trichloropyridin-2-yl phosphate
-
-
diethyl 4-nitrophenyl phosphate
-
-
Diethyl p-nitrophenyl phosphate
diethyldicarbonate
-
20% residual activity at 1 mM
dihydrocelastrol
-
inhibits MGL activity, albeit less potently than pristimerin
dihydrocelastryl diacetate
-
inhibits MGL activity, albeit less potently than pristimerin
diisopropyl fluorophosphate
diisopropylfluorophosphate
-
75% residual activity at 1 mM
Disulfiram
dithiothreitol
-
-
dodecane-1-sulfonyl fluoride
-
-
dodecyl benzodioxaphosphorin oxide
-
IC50 is 0.83 nM
dodecyl sulfonyl fluoride
-
IC50 is 200 nM
E600
-
inactivation
EDTA
-
50% residual activity at 1 mM
eriodictyol
-
ethyl 3,5,6-trichloropyridin-2-yl dodecylphosphonate
-
-
ethyl octylphosphonofluoridate
euphol
-
inhibits MGL activity with high potency. Blocks MGL activity through a reversible and noncompetitive mechanism, which is apparently identical to that of pristimerin
Fe3+
-
35% residual activity at 1 mM
heptyl benzodioxaphosphorin oxide
-
IC50 is 45 nM
hexadecylsufonyl fluoride
Hg2+
-
30% residual activity at 1 mM
HgCl2
isopropyl dodecylfluorophosphate
-
i.e. IDFP, n-C12H25P(O)(OCH3)F, IC50 is 0.76 nM
isopropyl dodecylfluorophosphonate
-
is not selective for MAGL
isopropyldodecylfluorophosphonate
-
-
jewenol A
reversible inhibitor, catalytic site binding structure, overview
JJKK-048
-
i.e. 4-[bis-(benzo[d][1,3]dioxol-5-yl)methyl]-piperidin-1-yl}(1H-1,2,4-triazol-1-yl)methanone
JZL184
LY2183240
is less potent than JZL184
Maleimide
IC50 value is 0.070 mM
meloxicam
Mercury chloride
-
-
methyl (5Z,8Z,11Z,14Z)-icosa-5,8,11,14- tetraenylphosphonofluoridate
-
completely inhibits 4-nitophenyl acetate hydrolysis by pure human MGL at 0.1 mM
methyl arachidonyl fluorophosphonate
methyl icosylphosphonofluoridoate
-
-
methyl octylphosphonofluoridate
methylarachidonoylfluorophosphonate
-
-
MJN110
inhibits glucose-stimulated insulin secretion and depolarization-induced insulin secretion in INS-1 (832/13) cells
Mn2+
-
58% residual activity at 1 mM
N-(1-pyrenyl)-maleimide
IC50 value is 0.068 mM
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
N-arachidonoylmaleimide
N-arachidonyl maleimide
N-arachidonylmaleimide
N-benzoylthiocarbamic cyclohexylethyl ester
-
-
N-cyclohexylmaleimide
IC50 value is 0.051 mM
N-ethylmaleimide
N-hydroxymaleimide
IC50 value is 0.413 mM
N-n-heptyl benzodioxaphosphorin oxide
-
IC50 is 150 nM
N-Phenylmaleimide
IC50 value is 0.044 mM
N-propylmaleimide
IC50 value is 0.053 mM
N-[3-(4-fluorophenyl)-6-oxopyrazolo[5,1-c]pyrido[4,3-e][1,2,4]triazin-7(6H)-yl]-2-(naphthalen-2-yloxy)acetamide
72.3% residual activity at 0.1 mM
N-[4-(1,3-benzothiazol-2-yl)phenyl]-2-(1H-benzotriazol-1-yl)acetamide
14.28% residual activity at 0.1 mM
noladin ether
-
IC50 value is 0.036 mM
O-n-octyl benzodioxaphosphorin oxide
-
IC50 is 150 nM
octane-1-sulfonyl fluoride
-
-
octyl sulfonyl fluoride
-
IC50 is 140 nM
oleanolic acid
-
p-bromophenacyl bromide
-
partial inhibition
p-chloromercuribenzoic acid
-
45% residual activity at 1 mM
palmitoyl-CoA
-
-
paraoxon
-
IC50 is 0.0023 mM
pedalitin
-
phenylmethylsulfonyl fluoride
pinoresinol 4-O-beta-D-glucopyranoside
-
pristimerin
pristimerol
-
inhibits MGL activity, albeit less potently than pristimerin
Protamine sulfate
-
-
-
Protocatechualdehyde
-
pseudorosmaricin
poor inhibition
rosiglitazone
S-heptyl benzodioxaphosphorin oxide
-
IC50 is 2.9 nM
S-nonyl benzodioxaphosphorin oxide
-
IC50 is 0.31 nM
S-nonylbenzodioxaphosphorin oxide
-
is not selective for MAGL
S-pentyl benzodioxaphosphorin oxide
-
IC50 is 3.1 nM
SAR629
-
substrate mimic
sodium cholate
-
-
SPB 01403
-
-
stearyl benzodioxaphosphorin oxide
-
IC50 is 51 nM
tetrahydrolipstatin
Triton X-100
-
10% inhibition at 0.25%
troglitazone
URB-602
-
a specific MGL inhibitor
URB602
Zn2+
-
27% residual activity at 1 mM
[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
[4-[bis(1,3-benzodioxol-5-yl)methyl]-1-piperidinyl](1H-1,2,4-triazol-1-yl)methanone
a highly potent selective inhibitor
additional information
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