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Assay Detail

CHEMBL3384491

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

Binding
Inhibition of human recombinant MAGL expressed in HEK293 cells using 2-AG as substrate assessed as remaining activity at 10 uM
16
Total Activities
15
Compounds Tested
2
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

Piperazine and piperidine carboxamides and carbamates as inhibitors of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL).
Korhonen J, Kuusisto A, van Bruchem J, Patel JZ, Laitinen T, Navia-Paldanius D, Laitinen JT, Savinainen JR, Parkkari T, Nevalainen TJ.
Bioorg Med Chem (2014) 22 : 6694 -6705
PubMed 25282655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Activity 15 - -
IC50 1 9.15 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356958 2 9.15
CHEMBL3356963 1 -
CHEMBL3356964 1 -
CHEMBL3356965 1 -
CHEMBL3356966 1 -
CHEMBL3356967 1 -
CHEMBL3356968 1 -
CHEMBL3356969 1 -
CHEMBL3356970 1 -
CHEMBL2164594 1 -
CHEMBL3356972 1 -
CHEMBL3356973 1 -
CHEMBL3356982 1 -
CHEMBL3356983 1 -
CHEMBL3356984 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356958 IC50 = 0.7 nM 9.15
CHEMBL3356958 Activity = 51.0 % -
CHEMBL3356963 Activity = 62.0 % -
CHEMBL3356964 Activity = 96.0 % -
CHEMBL3356965 Activity = 58.0 % -
CHEMBL3356966 Activity = 92.0 % -
CHEMBL3356967 Activity = 86.0 % -
CHEMBL3356968 Activity = 93.0 % -
CHEMBL3356969 Activity = 101.0 % -
CHEMBL3356970 Activity = 94.0 % -
CHEMBL2164594 Activity = 98.0 % -
CHEMBL3356972 Activity = 102.0 % -
CHEMBL3356973 Activity = 78.0 % -
CHEMBL3356982 Activity = 85.0 % -
CHEMBL3356983 Activity = 92.0 % -
CHEMBL3356984 Activity = 89.0 % -