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Assay Detail

CHEMBL3384490

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
39
Total Activities
20
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

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
IC50 39 7.37 9.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3087181 2 9.44
CHEMBL3356971 2 9.26
CHEMBL3356985 1 9.16
CHEMBL1232635 2 9.07
CHEMBL3356956 2 8.89
CHEMBL3356957 2 8.77
CHEMBL3356975 2 8.26
CHEMBL3356974 2 8.11
CHEMBL3356981 2 7.38
CHEMBL3356979 2 7.16
CHEMBL3356976 2 7.13
CHEMBL3356960 2 6.88
CHEMBL3352862 2 6.59
CHEMBL3356959 2 6.56
CHEMBL602499 2 6.46
CHEMBL3356980 2 6.18
CHEMBL3356978 2 5.96
CHEMBL3356962 2 5.78
CHEMBL3356961 2 5.72
CHEMBL3356977 2 5.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3087181 IC50 = 0.3631 nM 9.44
CHEMBL3087181 IC50 = 0.4 nM 9.40
CHEMBL3356971 IC50 = 0.5495 nM 9.26
CHEMBL3356971 IC50 = 0.6 nM 9.22
CHEMBL3356985 IC50 = 0.6918 nM 9.16
CHEMBL1232635 IC50 = 0.8511 nM 9.07
CHEMBL1232635 IC50 = 0.9 nM 9.05
CHEMBL3356956 IC50 = 1.3 nM 8.89
CHEMBL3356956 IC50 = 1.318 nM 8.88
CHEMBL3356957 IC50 = 1.7 nM 8.77
CHEMBL3356957 IC50 = 1.698 nM 8.77
CHEMBL3356975 IC50 = 5.5 nM 8.26
CHEMBL3356975 IC50 = 5.495 nM 8.26
CHEMBL3356974 IC50 = 7.8 nM 8.11
CHEMBL3356974 IC50 = 7.762 nM 8.11
CHEMBL3356981 IC50 = 41.69 nM 7.38
CHEMBL3356981 IC50 = 42.0 nM 7.38
CHEMBL3356979 IC50 = 69.18 nM 7.16
CHEMBL3356979 IC50 = 70.0 nM 7.16
CHEMBL3356976 IC50 = 74.0 nM 7.13
CHEMBL3356976 IC50 = 74.13 nM 7.13
CHEMBL3356960 IC50 = 132.0 nM 6.88
CHEMBL3356960 IC50 = 131.83 nM 6.88
CHEMBL3352862 IC50 = 257.04 nM 6.59
CHEMBL3352862 IC50 = 257.0 nM 6.59
CHEMBL3356959 IC50 = 275.42 nM 6.56
CHEMBL3356959 IC50 = 275.0 nM 6.56
CHEMBL602499 IC50 = 346.74 nM 6.46
CHEMBL602499 IC50 = 347.0 nM 6.46
CHEMBL3356980 IC50 = 660.0 nM 6.18
CHEMBL3356980 IC50 = 660.69 nM 6.18
CHEMBL3356978 IC50 = 1100.0 nM 5.96
CHEMBL3356978 IC50 = 1122.02 nM 5.95
CHEMBL3356962 IC50 = 1660.0 nM 5.78
CHEMBL3356962 IC50 = 1659.59 nM 5.78
CHEMBL3356961 IC50 = 1905.46 nM 5.72
CHEMBL3356961 IC50 = 1905.0 nM 5.72
CHEMBL3356977 IC50 = 2844.0 nM 5.55
CHEMBL3356977 IC50 = 2818.38 nM 5.55