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Assay Detail

CHEMBL4424599

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Binding
Inhibition of human recombinant MAGL using 4-NPA as substrate after 30 mins
34
Total Activities
34
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

Optimization of a Benzoylpiperidine Class Identifies a Highly Potent and Selective Reversible Monoacylglycerol Lipase (MAGL) Inhibitor.
Granchi C, Lapillo M, Glasmacher S, Bononi G, Licari C, Poli G, El Boustani M, Caligiuri I, Rizzolio F, Gertsch J, Macchia M, Minutolo F, Tuccinardi T, Chicca A.
J Med Chem (2019) 62 : 1932 -1958
PubMed 30715876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 6.19 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3901007 1 8.52
CHEMBL576786 1 7.31
CHEMBL4575018 1 7.13
CHEMBL4536045 1 7.10
CHEMBL4534867 1 6.96
CHEMBL4436371 1 6.87
CHEMBL570812 1 6.87
CHEMBL4435479 1 6.86
CHEMBL4449639 1 6.79
CHEMBL4474818 1 6.71
CHEMBL4472877 1 6.62
CHEMBL4466342 1 6.58
CHEMBL4559346 1 6.43
CHEMBL4549211 1 6.41
CHEMBL4471924 1 6.37
CHEMBL4463252 1 6.34
CHEMBL4282040 1 6.08
CHEMBL4468362 1 6.02
CHEMBL4542020 1 6.00
CHEMBL4442280 1 5.96
CHEMBL4468596 1 5.89
CHEMBL4592963 1 5.89
CHEMBL4530498 1 5.89
CHEMBL4568297 1 5.85
CHEMBL4475604 1 5.66
CHEMBL4468106 1 5.62
CHEMBL4527656 1 5.60
CHEMBL4553078 1 5.58
CHEMBL4577085 1 5.30
CHEMBL4552228 1 5.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3901007 IC50 = 3.0 nM 8.52
CHEMBL576786 IC50 = 49.3 nM 7.31
CHEMBL4575018 IC50 = 74.0 nM 7.13
CHEMBL4536045 IC50 = 80.0 nM 7.10
CHEMBL4534867 IC50 = 110.0 nM 6.96
CHEMBL4436371 IC50 = 136.0 nM 6.87
CHEMBL570812 IC50 = 134.0 nM 6.87
CHEMBL4435479 IC50 = 138.0 nM 6.86
CHEMBL4449639 IC50 = 162.0 nM 6.79
CHEMBL4474818 IC50 = 194.0 nM 6.71
CHEMBL4472877 IC50 = 240.0 nM 6.62
CHEMBL4466342 IC50 = 262.0 nM 6.58
CHEMBL4559346 IC50 = 368.0 nM 6.43
CHEMBL4549211 IC50 = 389.0 nM 6.41
CHEMBL4471924 IC50 = 424.0 nM 6.37
CHEMBL4463252 IC50 = 457.0 nM 6.34
CHEMBL4282040 IC50 = 840.0 nM 6.08
CHEMBL4468362 IC50 = 960.0 nM 6.02
CHEMBL4542020 IC50 = 1000.0 nM 6.00
CHEMBL4442280 IC50 = 1100.0 nM 5.96
CHEMBL4468596 IC50 = 1300.0 nM 5.89
CHEMBL4592963 IC50 = 1300.0 nM 5.89
CHEMBL4530498 IC50 = 1300.0 nM 5.89
CHEMBL4568297 IC50 = 1400.0 nM 5.85
CHEMBL4475604 IC50 = 2200.0 nM 5.66
CHEMBL4468106 IC50 = 2400.0 nM 5.62
CHEMBL4527656 IC50 = 2500.0 nM 5.60
CHEMBL4553078 IC50 = 2600.0 nM 5.58
CHEMBL4577085 IC50 = 5000.0 nM 5.30
CHEMBL4552228 IC50 = 5300.0 nM 5.28
CHEMBL4587797 IC50 = 8200.0 nM 5.09
CHEMBL4451621 IC50 = 8700.0 nM 5.06
CHEMBL4465086 IC50 = 10200.0 nM 4.99
CHEMBL4587625 IC50 = 12300.0 nM 4.91