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Assay Detail

CHEMBL4329658

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Functional
Allosteric modulation of CB1 receptor (unknown origin) assessed as inhibition of calcium mobilization by FLIPR assay
12
Total Activities
12
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

Allosteric CB<sub>1</sub> Receptor Modulators for the Treatment of CB<sub>1</sub> Related Diseases and Conditions.
Kargbo RB.
ACS Med Chem Lett (2018) 9 : 1162 -1163
PubMed 30613319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.50 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4096928 1 7.75
CHEMBL4067016 1 7.66
CHEMBL4078901 1 7.64
CHEMBL4077975 1 7.57
CHEMBL4070648 1 7.50
CHEMBL3341861 1 7.48
CHEMBL4462132 1 7.46
CHEMBL4459402 1 7.44
CHEMBL4513876 1 7.40
CHEMBL4584264 1 7.39
CHEMBL4443345 1 7.38
CHEMBL4089126 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4096928 IC50 = 18.0 nM 7.75
CHEMBL4067016 IC50 = 22.0 nM 7.66
CHEMBL4078901 IC50 = 23.0 nM 7.64
CHEMBL4077975 IC50 = 27.0 nM 7.57
CHEMBL4070648 IC50 = 32.0 nM 7.50
CHEMBL3341861 IC50 = 33.0 nM 7.48
CHEMBL4462132 IC50 = 35.0 nM 7.46
CHEMBL4459402 IC50 = 36.0 nM 7.44
CHEMBL4513876 IC50 = 40.0 nM 7.40
CHEMBL4584264 IC50 = 41.0 nM 7.39
CHEMBL4443345 IC50 = 42.0 nM 7.38
CHEMBL4089126 IC50 = 47.0 nM 7.33