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Assay Detail

CHEMBL936658

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Binding
Binding affinity to CB1 receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Identification of novel cannabinoid CB1 receptor antagonists by using virtual screening with a pharmacophore model.
Wang H, Duffy RA, Boykow GC, Chackalamannil S, Madison VS.
J Med Chem (2008) 51 : 2439 -2446
PubMed 18363352 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.81 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111 RIMONABANT 4.0 1 8.70
CHEMBL412071 1 8.24
CHEMBL412262 IBIPINABANT 2.0 1 8.11
CHEMBL50925 1 7.15
CHEMBL411481 1 6.85
CHEMBL410267 1 -
CHEMBL376700 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111 RIMONABANT Ki = 1.98 nM 8.70
CHEMBL412071 Ki = 5.8 nM 8.24
CHEMBL412262 IBIPINABANT Ki = 7.8 nM 8.11
CHEMBL50925 Ki = 70.3 nM 7.15
CHEMBL411481 Ki = 141.0 nM 6.85
CHEMBL410267 Ki < 100.0 nM -
CHEMBL376700 Ki = 0.00035 nM -