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Assay Detail

CHEMBL4733345

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 assay
27
Total Activities
27
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 and biological evaluation of second-generation benzoylpiperidine derivatives as reversible monoacylglycerol lipase (MAGL) inhibitors.
Granchi C,Bononi G,Ferrisi R,Gori E,Mantini G,Glasmacher S,Poli G,Palazzolo S,Caligiuri I,Rizzolio F,Canzonieri V,Perin T,Gertsch J,Sodi A,Giovannetti E,Macchia M,Minutolo F,Tuccinardi T,Chicca A
Eur J Med Chem (2021) 209 : 112857 -112857
PubMed 33045662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.44 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4757403 1 7.75
CHEMBL4747585 1 7.52
CHEMBL4758717 1 7.51
CHEMBL4755606 1 7.44
CHEMBL4798508 1 7.31
CHEMBL4789288 1 7.13
CHEMBL4758976 1 7.11
CHEMBL4536045 1 7.09
CHEMBL4798272 1 6.89
CHEMBL570812 1 6.89
CHEMBL4435479 1 6.85
CHEMBL4746545 1 6.56
CHEMBL4794653 1 6.43
CHEMBL4753531 1 6.12
CHEMBL4784401 1 6.00
CHEMBL4753368 1 5.70
CHEMBL4754790 1 5.64
CHEMBL4784941 1 5.48
CHEMBL4755379 1 5.47
CHEMBL4763206 1 5.37
CHEMBL4758281 1 5.36
CHEMBL4752739 1 5.35
CHEMBL4755839 1 5.09
CHEMBL4778126 1 -
CHEMBL4757544 1 -
CHEMBL4763651 1 -
CHEMBL4755309 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4757403 IC50 = 18.0 nM 7.75
CHEMBL4747585 IC50 = 30.0 nM 7.52
CHEMBL4758717 IC50 = 31.0 nM 7.51
CHEMBL4755606 IC50 = 36.0 nM 7.44
CHEMBL4798508 IC50 = 49.0 nM 7.31
CHEMBL4789288 IC50 = 74.0 nM 7.13
CHEMBL4758976 IC50 = 78.0 nM 7.11
CHEMBL4536045 IC50 = 81.0 nM 7.09
CHEMBL4798272 IC50 = 129.0 nM 6.89
CHEMBL570812 IC50 = 130.0 nM 6.89
CHEMBL4435479 IC50 = 142.0 nM 6.85
CHEMBL4746545 IC50 = 278.0 nM 6.56
CHEMBL4794653 IC50 = 368.0 nM 6.43
CHEMBL4753531 IC50 = 758.0 nM 6.12
CHEMBL4784401 IC50 = 1000.0 nM 6.00
CHEMBL4753368 IC50 = 2000.0 nM 5.70
CHEMBL4754790 IC50 = 2300.0 nM 5.64
CHEMBL4784941 IC50 = 3300.0 nM 5.48
CHEMBL4755379 IC50 = 3400.0 nM 5.47
CHEMBL4763206 IC50 = 4300.0 nM 5.37
CHEMBL4758281 IC50 = 4400.0 nM 5.36
CHEMBL4752739 IC50 = 4500.0 nM 5.35
CHEMBL4755839 IC50 = 8200.0 nM 5.09
CHEMBL4778126 IC50 > 10000.0 nM -
CHEMBL4757544 IC50 > 10000.0 nM -
CHEMBL4763651 IC50 > 10000.0 nM -
CHEMBL4755309 IC50 > 10000.0 nM -