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Assay Detail

CHEMBL4180663

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

Functional
Positive allosteric modulation of human CB1 receptor expressed in CHO-K1 cell membranes assessed as induction of [3H]CP55,940 binding after 1.5 hrs by liquid scintillation counting assay
6
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel analogs of PSNCBAM-1 as allosteric modulators of cannabinoid CB1 receptor.
Bertini S, Chicca A, Gado F, Arena C, Nieri D, Digiacomo M, Saccomanni G, Zhao P, Abood ME, Macchia M, Gertsch J, Manera C.
Bioorg Med Chem (2017) 25 : 6427 -6434
PubMed 29079014 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.18 7.37
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4215809 2 7.37
CHEMBL3341861 1 6.57
CHEMBL4206416 1 5.89
CHEMBL4203175 1 4.87
CHEMBL4210152 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4215809 EC50 = 43.0 nM 7.37
CHEMBL3341861 EC50 = 270.0 nM 6.57
CHEMBL4206416 EC50 = 1300.0 nM 5.89
CHEMBL4203175 EC50 = 13500.0 nM 4.87
CHEMBL4215809 Activity - -
CHEMBL4210152 EC50 > 10000.0 nM -