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Assay Detail

CHEMBL5228800

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

Binding
Inhibition of human recombinant MAGL by fluorometric analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Monoglyceride lipase (CHEMBL4191)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold.
Rong J, Mori W, Xia X, Schafroth MA, Zhao C, Van RS, Yamasaki T, Chen J, Xiao Z, Haider A, Ogasawara D, Hiraishi A, Shao T, Zhang Y, Chen Z, Pang F, Hu K, Xie L, Fujinaga M, Kumata K, Gou Y, Fang Y, Gu S, Wei H, Bao L, Xu H, Collier TL, Shao Y, Carson RE, Cravatt BF, Wang L, Zhang MR, Liang SH.
J Med Chem (2021) 64 : 14283 -14298
PubMed 34569803 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.04 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3658400 1 8.38
CHEMBL5274306 1 8.34
CHEMBL5290125 1 7.75
CHEMBL4640364 1 7.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3658400 IC50 = 4.2 nM 8.38
CHEMBL5274306 IC50 = 4.6 nM 8.34
CHEMBL5290125 IC50 = 17.8 nM 7.75
CHEMBL4640364 IC50 = 20.3 nM 7.69