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Assay Detail

CHEMBL4275246

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

Binding
Inhibition of recombinant human C-terminal His-tagged MAGL expressed in Escherichia coli using 4-NPA as substrate measured after 30 mins
41
Total Activities
41
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

Discovery of long-chain salicylketoxime derivatives as monoacylglycerol lipase (MAGL) inhibitors.
Bononi G, Granchi C, Lapillo M, Giannotti M, Nieri D, Fortunato S, Boustani ME, Caligiuri I, Poli G, Carlson KE, Kim SH, Macchia M, Martinelli A, Rizzolio F, Chicca A, Katzenellenbogen JA, Minutolo F, Tuccinardi T.
Eur J Med Chem (2018) 157 : 817 -836
PubMed 30144699 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 5.25 6.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL570812 1 6.85
CHEMBL4293423 1 6.17
CHEMBL4284088 1 6.15
CHEMBL4282758 1 6.11
CHEMBL4282040 1 6.08
CHEMBL4283120 1 6.04
CHEMBL4293367 1 6.02
CHEMBL4291956 1 6.00
CHEMBL4289986 1 5.96
CHEMBL4285844 1 5.89
CHEMBL4279301 1 5.82
CHEMBL4280805 1 5.77
CHEMBL4279032 1 5.77
CHEMBL4277602 1 5.70
CHEMBL4283165 1 5.62
CHEMBL4286559 1 5.60
CHEMBL4291020 1 5.48
CHEMBL4278225 1 5.32
CHEMBL4284990 1 5.29
CHEMBL4294450 1 5.28
CHEMBL4286138 1 5.14
CHEMBL3409959 1 4.96
CHEMBL4292707 1 4.92
CHEMBL4294185 1 4.80
CHEMBL4287594 1 4.75
CHEMBL4284676 1 4.72
CHEMBL4284214 1 4.70
CHEMBL4279686 1 4.60
CHEMBL4284837 1 4.58
CHEMBL4291427 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL570812 IC50 = 140.0 nM 6.85
CHEMBL4293423 IC50 = 680.0 nM 6.17
CHEMBL4284088 IC50 = 710.0 nM 6.15
CHEMBL4282758 IC50 = 770.0 nM 6.11
CHEMBL4282040 IC50 = 840.0 nM 6.08
CHEMBL4283120 IC50 = 910.0 nM 6.04
CHEMBL4293367 IC50 = 960.0 nM 6.02
CHEMBL4291956 IC50 = 1000.0 nM 6.00
CHEMBL4289986 IC50 = 1100.0 nM 5.96
CHEMBL4285844 IC50 = 1300.0 nM 5.89
CHEMBL4279301 IC50 = 1500.0 nM 5.82
CHEMBL4280805 IC50 = 1700.0 nM 5.77
CHEMBL4279032 IC50 = 1700.0 nM 5.77
CHEMBL4277602 IC50 = 2000.0 nM 5.70
CHEMBL4283165 IC50 = 2400.0 nM 5.62
CHEMBL4286559 IC50 = 2500.0 nM 5.60
CHEMBL4291020 IC50 = 3300.0 nM 5.48
CHEMBL4278225 IC50 = 4800.0 nM 5.32
CHEMBL4284990 IC50 = 5100.0 nM 5.29
CHEMBL4294450 IC50 = 5200.0 nM 5.28
CHEMBL4286138 IC50 = 7200.0 nM 5.14
CHEMBL3409959 IC50 = 11000.0 nM 4.96
CHEMBL4292707 IC50 = 12000.0 nM 4.92
CHEMBL4294185 IC50 = 16000.0 nM 4.80
CHEMBL4287594 IC50 = 18000.0 nM 4.75
CHEMBL4284676 IC50 = 19000.0 nM 4.72
CHEMBL4284214 IC50 = 20000.0 nM 4.70
CHEMBL4279686 IC50 = 25000.0 nM 4.60
CHEMBL4284837 IC50 = 26000.0 nM 4.58
CHEMBL4291427 IC50 = 28000.0 nM 4.55
CHEMBL4281690 IC50 = 30000.0 nM 4.52
CHEMBL3409958 IC50 = 34000.0 nM 4.47
CHEMBL4294836 IC50 = 34000.0 nM 4.47
CHEMBL4286305 IC50 = 36000.0 nM 4.44
CHEMBL4288022 IC50 = 36000.0 nM 4.44
CHEMBL4294988 IC50 = 53000.0 nM 4.28
CHEMBL4277378 IC50 = 69000.0 nM 4.16
CHEMBL4280782 IC50 = 70000.0 nM 4.16
CHEMBL4293107 IC50 > 200000.0 nM -
CHEMBL4293042 IC50 > 200000.0 nM -
CHEMBL4289567 IC50 = 119000.0 nM -