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Assay Detail

CHEMBL3379277

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Binding
Agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Galpha i2 assessed as Galpha GTPase activity using [gamma-33P]GTP by scintillation counting
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of bivalent cannabinoid receptor ligands based on hCB₂R selective benzimidazoles reveal unexpected intrinsic properties.
Nimczick M, Pemp D, Darras FH, Chen X, Heilmann J, Decker M.
Bioorg Med Chem (2014) 22 : 3938 -3946
PubMed 24984935 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.42 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 7.89
CHEMBL3310157 1 5.87
CHEMBL471980 1 5.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 EC50 = 12.88 nM 7.89
CHEMBL3310157 EC50 = 1348.96 nM 5.87
CHEMBL471980 EC50 = 3235.94 nM 5.49