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Assay Detail

CHEMBL1053085

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human recombinant MGL by liquid scintillation counting
16
Total Activities
16
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

The synthesis and biological evaluation of para-substituted phenolic N-alkyl carbamates as endocannabinoid hydrolyzing enzyme inhibitors.
Minkkilä A, Myllymäki MJ, Saario SM, Castillo-Melendez JA, Koskinen AM, Fowler CJ, Leppänen J, Nevalainen T.
Eur J Med Chem (2009) 44 : 2994 -3008
PubMed 19232787 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.06 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL561924 1 6.85
CHEMBL569368 1 6.00
CHEMBL557234 1 5.68
CHEMBL565019 1 5.38
CHEMBL559034 1 5.10
CHEMBL560119 1 5.08
CHEMBL541001 1 4.92
CHEMBL553472 1 4.85
CHEMBL549493 1 4.77
CHEMBL560460 1 4.75
CHEMBL557916 1 4.72
CHEMBL558834 1 4.66
CHEMBL557506 1 4.62
CHEMBL558048 1 4.62
CHEMBL559985 1 4.52
CHEMBL551567 1 4.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL561924 IC50 = 140.0 nM 6.85
CHEMBL569368 IC50 = 1000.0 nM 6.00
CHEMBL557234 IC50 = 2100.0 nM 5.68
CHEMBL565019 IC50 = 4200.0 nM 5.38
CHEMBL559034 IC50 = 8000.0 nM 5.10
CHEMBL560119 IC50 = 8400.0 nM 5.08
CHEMBL541001 IC50 = 12000.0 nM 4.92
CHEMBL553472 IC50 = 14000.0 nM 4.85
CHEMBL549493 IC50 = 17000.0 nM 4.77
CHEMBL560460 IC50 = 18000.0 nM 4.75
CHEMBL557916 IC50 = 19000.0 nM 4.72
CHEMBL558834 IC50 = 22000.0 nM 4.66
CHEMBL557506 IC50 = 24000.0 nM 4.62
CHEMBL558048 IC50 = 24000.0 nM 4.62
CHEMBL559985 IC50 = 30000.0 nM 4.52
CHEMBL551567 IC50 = 43000.0 nM 4.37