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Assay Detail

CHEMBL1072745

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

Binding
Inhibition of MAGL in mouse brain membrane
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Monoglyceride lipase (CHEMBL5774)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
Long JZ, Jin X, Adibekian A, Li W, Cravatt BF.
J Med Chem (2010) 53 : 1830 -1842
PubMed 20099888 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 6.70 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL576786 1 8.00
CHEMBL603704 1 8.00
CHEMBL602281 1 7.82
CHEMBL606201 1 7.72
CHEMBL604758 1 7.40
CHEMBL601243 1 7.30
CHEMBL600429 1 7.30
CHEMBL597515 1 7.16
CHEMBL604948 1 7.16
CHEMBL599989 1 7.14
CHEMBL597699 1 7.10
CHEMBL602283 1 7.05
CHEMBL601244 1 7.05
CHEMBL591688 1 7.05
CHEMBL603111 1 6.89
CHEMBL602499 1 6.70
CHEMBL603077 1 6.70
CHEMBL601002 1 6.52
CHEMBL600428 1 6.30
CHEMBL599725 1 6.29
CHEMBL599724 1 6.25
CHEMBL602282 1 6.17
CHEMBL602292 1 6.16
CHEMBL597514 1 6.09
CHEMBL597700 1 6.05
CHEMBL599731 1 5.96
CHEMBL599726 1 5.89
CHEMBL602293 1 5.86
CHEMBL602084 1 5.82
CHEMBL605004 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL576786 IC50 = 10.0 nM 8.00
CHEMBL603704 IC50 = 10.0 nM 8.00
CHEMBL602281 IC50 = 15.0 nM 7.82
CHEMBL606201 IC50 = 19.0 nM 7.72
CHEMBL604758 IC50 = 40.0 nM 7.40
CHEMBL601243 IC50 = 50.0 nM 7.30
CHEMBL600429 IC50 = 50.0 nM 7.30
CHEMBL597515 IC50 = 70.0 nM 7.16
CHEMBL604948 IC50 = 70.0 nM 7.16
CHEMBL599989 IC50 = 73.0 nM 7.14
CHEMBL597699 IC50 = 80.0 nM 7.10
CHEMBL602283 IC50 = 90.0 nM 7.05
CHEMBL601244 IC50 = 90.0 nM 7.05
CHEMBL591688 IC50 = 90.0 nM 7.05
CHEMBL603111 IC50 = 130.0 nM 6.89
CHEMBL602499 IC50 = 200.0 nM 6.70
CHEMBL603077 IC50 = 200.0 nM 6.70
CHEMBL601002 IC50 = 300.0 nM 6.52
CHEMBL600428 IC50 = 500.0 nM 6.30
CHEMBL599725 IC50 = 510.0 nM 6.29
CHEMBL599724 IC50 = 560.0 nM 6.25
CHEMBL602282 IC50 = 670.0 nM 6.17
CHEMBL602292 IC50 = 690.0 nM 6.16
CHEMBL597514 IC50 = 810.0 nM 6.09
CHEMBL597700 IC50 = 900.0 nM 6.05
CHEMBL599731 IC50 = 1100.0 nM 5.96
CHEMBL599726 IC50 = 1300.0 nM 5.89
CHEMBL602293 IC50 = 1390.0 nM 5.86
CHEMBL602084 IC50 = 1530.0 nM 5.82
CHEMBL605004 IC50 = 2120.0 nM 5.67
CHEMBL599990 IC50 = 6120.0 nM 5.21
CHEMBL601003 IC50 > 100000.0 nM -
CHEMBL602936 IC50 > 50000.0 nM -
CHEMBL601892 IC50 > 50000.0 nM -
CHEMBL601893 IC50 > 50000.0 nM -