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Assay Detail

CHEMBL3405396

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

Binding
Inhibition of human recombinant MAGL using 2-arachidonoylglycerol substrate assessed as arachidonic acid by HPLC analysis
14
Total Activities
7
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

Loratadine analogues as MAGL inhibitors.
Patel JZ, Ahenkorah S, Vaara M, Staszewski M, Adams Y, Laitinen T, Navia-Paldanius D, Parkkari T, Savinainen JR, Walczyński K, Laitinen JT, Nevalainen TJ.
Bioorg Med Chem Lett (2015) 25 : 1436 -1442
PubMed 25752982 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.08 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3087181 2 9.44
CHEMBL3401455 2 7.34
CHEMBL3402827 2 7.33
CHEMBL3401457 2 7.01
CHEMBL3401456 2 6.68
CHEMBL3402819 2 6.19
CHEMBL3402820 2 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3087181 IC50 = 0.3631 nM 9.44
CHEMBL3087181 IC50 = 0.36 nM 9.44
CHEMBL3401455 IC50 = 45.71 nM 7.34
CHEMBL3401455 IC50 = 46.0 nM 7.34
CHEMBL3402827 IC50 = 46.77 nM 7.33
CHEMBL3402827 IC50 = 47.0 nM 7.33
CHEMBL3401457 IC50 = 97.72 nM 7.01
CHEMBL3401457 IC50 = 98.0 nM 7.01
CHEMBL3401456 IC50 = 208.93 nM 6.68
CHEMBL3401456 IC50 = 208.0 nM 6.68
CHEMBL3402819 IC50 = 645.65 nM 6.19
CHEMBL3402819 IC50 = 645.0 nM 6.19
CHEMBL3402820 IC50 = 2570.4 nM 5.59
CHEMBL3402820 IC50 = 2570.0 nM 5.59