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Assay Detail

CHEMBL4416370

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Functional
Allosteric antagonist activity at human CB1 receptor by Ca2+ assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and Pharmacological Evaluation of 1-Phenyl-3-Thiophenylurea Derivatives as Cannabinoid Type-1 Receptor Allosteric Modulators.
Nguyen T, Gamage TF, Decker AM, Barrus D, Langston TL, Li JX, Thomas BF, Zhang Y.
J Med Chem (2019) 62 : 9806 -9823
PubMed 31596583 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.09 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4078901 1 7.64
CHEMBL3341861 1 7.48
CHEMBL3341880 1 7.48
CHEMBL4450500 1 6.77
CHEMBL1553629 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4078901 IC50 = 23.0 nM 7.64
CHEMBL3341861 IC50 = 33.0 nM 7.48
CHEMBL3341880 IC50 = 33.0 nM 7.48
CHEMBL4450500 IC50 = 169.0 nM 6.77
CHEMBL1553629 IC50 = 853.0 nM 6.07