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Assay Detail

CHEMBL1046620

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Binding
Inhibition of human MGL activity using [3H]2-oleoylglycerol substrate by liquid scintillation counting
ChEMBL ↗
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Monoglyceride lipase (CHEMBL4191) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Bis(dialkylaminethiocarbonyl)disulfides as potent and selective monoglyceride lipase inhibitors.
Kapanda CN, Muccioli GG, Labar G, Poupaert JH, Lambert DM.
J Med Chem (2009) 52 : 7310 -7314
PubMed 19883085 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 5.85 7.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL570812 — — 1 7.69
CHEMBL113262 METHOXYARACHIDONOYL FLUOROPHOSPHONATE — 1 7.58
CHEMBL509860 — — 1 7.26
CHEMBL571699 — — 1 6.96
CHEMBL576697 — — 1 6.85
CHEMBL570565 — — 1 6.78
CHEMBL121556 — — 1 6.66
CHEMBL576671 — — 1 6.57
CHEMBL573920 — — 1 6.50
CHEMBL121516 BIS(PIPERIDINYLTHIOCARBONYL)DISULFIDE — 1 6.50
CHEMBL583524 — — 1 6.46
CHEMBL571274 — — 1 6.36
CHEMBL571273 — — 1 6.32
CHEMBL569626 — — 1 6.31
CHEMBL570804 — — 1 6.13
CHEMBL570340 — — 1 6.13
CHEMBL585179 — — 1 6.09
CHEMBL583959 BIS(PYRROLIDINYLTHIOCARBONYL)DISULFIDE — 1 6.04
CHEMBL120563 THIRAM 2.0 1 6.01
CHEMBL571495 — — 1 5.95
CHEMBL964 DISULFIRAM 4.0 1 5.90
CHEMBL578805 — — 1 5.39
CHEMBL570572 — — 1 5.30
CHEMBL571701 — — 1 5.19
CHEMBL281211 ARACHIDONYL TRIFLUOROMETHYLKETONE — 1 5.19
CHEMBL583000 — — 1 5.16
CHEMBL570577 — — 1 5.10
CHEMBL120082 BIS(DIBENZYLAMINETHIOCARBONYL)DISULFIDE — 1 5.02
CHEMBL573921 — — 1 5.02
CHEMBL77767 — — 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL570812 — IC50 = 20.42 nM 7.69
CHEMBL113262 METHOXYARACHIDONOYL FLUOROPHOSPHONATE IC50 = 26.3 nM 7.58
CHEMBL509860 — IC50 = 54.95 nM 7.26
CHEMBL571699 — IC50 = 109.65 nM 6.96
CHEMBL576697 — IC50 = 141.25 nM 6.85
CHEMBL570565 — IC50 = 165.96 nM 6.78
CHEMBL121556 — IC50 = 218.78 nM 6.66
CHEMBL576671 — IC50 = 269.15 nM 6.57
CHEMBL573920 — IC50 = 316.23 nM 6.50
CHEMBL121516 BIS(PIPERIDINYLTHIOCARBONYL)DISULFIDE IC50 = 316.23 nM 6.50
CHEMBL583524 — IC50 = 346.74 nM 6.46
CHEMBL571274 — IC50 = 436.52 nM 6.36
CHEMBL571273 — IC50 = 478.63 nM 6.32
CHEMBL569626 — IC50 = 489.78 nM 6.31
CHEMBL570340 — IC50 = 741.31 nM 6.13
CHEMBL570804 — IC50 = 741.31 nM 6.13
CHEMBL585179 — IC50 = 812.83 nM 6.09
CHEMBL583959 BIS(PYRROLIDINYLTHIOCARBONYL)DISULFIDE IC50 = 912.01 nM 6.04
CHEMBL120563 THIRAM IC50 = 977.24 nM 6.01
CHEMBL571495 — IC50 = 1122.02 nM 5.95
CHEMBL964 DISULFIRAM IC50 = 1258.93 nM 5.90
CHEMBL578805 — IC50 = 4073.8 nM 5.39
CHEMBL570572 — IC50 = 5011.87 nM 5.30
CHEMBL571701 — IC50 = 6456.54 nM 5.19
CHEMBL281211 ARACHIDONYL TRIFLUOROMETHYLKETONE IC50 = 6456.54 nM 5.19
CHEMBL583000 — IC50 = 6918.31 nM 5.16
CHEMBL570577 — IC50 = 7943.28 nM 5.10
CHEMBL120082 BIS(DIBENZYLAMINETHIOCARBONYL)DISULFIDE IC50 = 9549.93 nM 5.02
CHEMBL573921 — IC50 = 9549.93 nM 5.02
CHEMBL77767 — IC50 = 10000.0 nM 5.00
CHEMBL567397 — IC50 = 10471.29 nM 4.98
CHEMBL582932 DITHIODIMORPHOLINE IC50 = 11220.18 nM 4.95
CHEMBL571700 BIS(DIMETHYLAMINETHIOCARBONYL)MONOSULFIDE IC50 = 12302.69 nM 4.91
CHEMBL583322 — IC50 = 15488.17 nM 4.81
CHEMBL582931 (DIETHYLTHIOCARBAMOYL)METHYLENE DIETHYLCARBAMODITHIOATE IC50 = 19054.61 nM 4.72
CHEMBL570813 — IC50 = 20892.96 nM 4.68
CHEMBL570228 — IC50 = 95499.26 nM 4.02
CHEMBL570341 — IC50 = 102329.3 nM -
CHEMBL584158 — IC50 > 1000000.0 nM -
CHEMBL1745 METHYLDIETHYL CARBAMODITHIOATE IC50 > 1000000.0 nM -
CHEMBL569414 (DIETHYLCARBAMOYL)METHYLENE DIETHYLCARBAMODITHIOATE IC50 = 630957.34 nM -
CHEMBL565454 — IC50 = 218776.16 nM -