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Assay Detail

CHEMBL917774

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

Functional
Activity at human CB1 receptor by [35S]GTP-gamma-S binding stimulation assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: new templates among the CB1 cannabinoid receptor inverse agonists.
Muccioli GG, Wouters J, Scriba GK, Poppitz W, Poupaert JH, Lambert DM.
J Med Chem (2005) 48 : 7486 -7490
PubMed 16279809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 6.84 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL334533 DEXANABINOL 3.0 1 9.22
CHEMBL111 RIMONABANT 4.0 1 8.00
CHEMBL224627 1 6.35
CHEMBL427241 1 6.30
CHEMBL436309 1 6.16
CHEMBL224113 1 5.98
CHEMBL224697 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL334533 DEXANABINOL EC50 = 0.6 nM 9.22
CHEMBL111 RIMONABANT EC50 = 10.1 nM 8.00
CHEMBL224627 EC50 = 450.0 nM 6.35
CHEMBL427241 EC50 = 500.0 nM 6.30
CHEMBL436309 EC50 = 700.0 nM 6.16
CHEMBL224113 EC50 = 1050.0 nM 5.98
CHEMBL224697 EC50 = 1250.0 nM 5.90