Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5533636

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

Binding
Inhibition of human recombinant MAGL using 4-nitrophenylacetate as substrate incubated for 30 mins by microplate reader analysis
20
Total Activities
20
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

Design, synthesis, ADME and biological evaluation of benzylpiperidine and benzylpiperazine derivatives as novel reversible monoacylglycerol lipase (MAGL) inhibitors.
Di Stefano M, Masoni S, Bononi G, Poli G, Galati S, Gado F, Manzi S, Vagaggini C, Brai A, Caligiuri I, Asif K, Rizzolio F, Macchia M, Chicca A, Sodi A, Di Bussolo V, Minutolo F, Meier P, Gertsch J, Granchi C, Dreassi E, Tuccinardi T.
Eur J Med Chem (2024) 263 : 115916 -115916
PubMed 37976705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.72 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5567027 1 8.89
CHEMBL5176915 1 8.68
CHEMBL5595401 1 8.60
CHEMBL5567389 1 8.57
CHEMBL5570158 1 8.28
CHEMBL5590627 1 8.15
CHEMBL5571621 1 7.88
CHEMBL5574704 1 7.84
CHEMBL5549926 1 7.68
CHEMBL5573282 1 7.65
CHEMBL5575182 1 7.49
CHEMBL5549920 1 7.39
CHEMBL5563136 1 7.35
CHEMBL576786 1 7.33
CHEMBL5593092 1 7.31
CHEMBL5570616 1 7.21
CHEMBL5565395 1 6.95
CHEMBL5574429 1 6.83
CHEMBL5564512 1 6.62
CHEMBL5570539 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5567027 IC50 = 1.3 nM 8.89
CHEMBL5176915 IC50 = 2.1 nM 8.68
CHEMBL5595401 IC50 = 2.5 nM 8.60
CHEMBL5567389 IC50 = 2.7 nM 8.57
CHEMBL5570158 IC50 = 5.2 nM 8.28
CHEMBL5590627 IC50 = 7.1 nM 8.15
CHEMBL5571621 IC50 = 13.2 nM 7.88
CHEMBL5574704 IC50 = 14.4 nM 7.84
CHEMBL5549926 IC50 = 20.8 nM 7.68
CHEMBL5573282 IC50 = 22.5 nM 7.65
CHEMBL5575182 IC50 = 32.3 nM 7.49
CHEMBL5549920 IC50 = 40.4 nM 7.39
CHEMBL5563136 IC50 = 44.8 nM 7.35
CHEMBL576786 IC50 = 47.0 nM 7.33
CHEMBL5593092 IC50 = 49.1 nM 7.31
CHEMBL5570616 IC50 = 61.2 nM 7.21
CHEMBL5565395 IC50 = 112.0 nM 6.95
CHEMBL5574429 IC50 = 149.0 nM 6.83
CHEMBL5564512 IC50 = 242.0 nM 6.62
CHEMBL5570539 IC50 > 1000.0 nM -