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Assay Detail

CHEMBL4177820

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

Binding
Inhibition of recombinant human full length MAGL expressed in HEK293 cells preincubated for 30 mins followed by FP-Rh addition after 30 mins by gel-based ABPP assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Monoglyceride lipase (CHEMBL4191)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Therapeutic Potential of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and N-Acylethanolamine Acid Amidase Inhibitors.
Tuo W, Leleu-Chavain N, Spencer J, Sansook S, Millet R, Chavatte P.
J Med Chem (2017) 60 : 4 -46
PubMed 27766867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.27 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356976 1 8.43
CHEMBL3901007 1 8.23
CHEMBL3959117 1 8.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356976 IC50 = 3.7 nM 8.43
CHEMBL3901007 IC50 = 5.9 nM 8.23
CHEMBL3959117 IC50 = 6.9 nM 8.16