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Assay Detail

CHEMBL1211490

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

Binding
Displacement of [3H]CP55490 from human recombinant cannabinoid CB1 receptor expressed in CHO cells
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and cannabinoid-1 receptor binding affinity of conformationally constrained analogs of taranabant.
Kopka IE, Lin LS, Jewell JP, Lanza TJ, Fong TM, Shen CP, Lao ZJ, Ha S, Castonguay LG, Van der Ploeg L, Goulet MT, Hagmann WK.
Bioorg Med Chem Lett (2010) 20 : 4757 -4761
PubMed 20643546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.36 9.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL373626 1 9.27
CHEMBL1209596 1 9.23
CHEMBL220360 TARANABANT 3.0 1 9.13
CHEMBL1209597 1 7.66
CHEMBL1209668 2 7.60
CHEMBL1209598 1 6.47
CHEMBL1209670 1 6.09
CHEMBL1209669 1 5.89
CHEMBL1209749 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL373626 IC50 = 0.54 nM 9.27
CHEMBL1209596 IC50 = 0.59 nM 9.23
CHEMBL220360 TARANABANT IC50 = 0.74 nM 9.13
CHEMBL1209597 IC50 = 22.0 nM 7.66
CHEMBL1209668 IC50 = 25.0 nM 7.60
CHEMBL1209668 IC50 = 260.0 nM 6.58
CHEMBL1209598 IC50 = 340.0 nM 6.47
CHEMBL1209670 IC50 = 810.0 nM 6.09
CHEMBL1209669 IC50 = 1300.0 nM 5.89
CHEMBL1209749 IC50 = 2000.0 nM 5.70