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Assay Detail

CHEMBL658114

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

Binding
Binding affinity towards Cannabinoid receptor 1 was determined using [3H]-CP- cannabinoid as radioligand with mouse brain membrane
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL3037)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Arachidonylsulfonyl derivatives as cannabinoid CB1 receptor and fatty acid amide hydrolase inhibitors.
Segall Y, Quistad GB, Nomura DK, Casida JE.
Bioorg Med Chem Lett (2003) 13 : 3301 -3303
PubMed 12951114 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.92 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333149 ISOPROPYL DODECYLFLUOROPHOSPHONATE 1 8.74
CHEMBL97038 DODECANESULFONYL FLUORIDE 1 8.16
CHEMBL112486 1 6.52
CHEMBL113262 METHOXYARACHIDONOYL FLUOROPHOSPHONATE 1 6.28
CHEMBL15848 ANANDAMIDE 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333149 ISOPROPYL DODECYLFLUOROPHOSPHONATE IC50 = 1.8 nM 8.74
CHEMBL97038 DODECANESULFONYL FLUORIDE IC50 = 6.9 nM 8.16
CHEMBL112486 IC50 = 304.0 nM 6.52
CHEMBL113262 METHOXYARACHIDONOYL FLUOROPHOSPHONATE IC50 = 530.0 nM 6.28
CHEMBL15848 ANANDAMIDE IC50 = 12000.0 nM 4.92