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Assay Detail

CHEMBL4426862

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Functional
Agonist activity at rat CB1 receptor expressed in HEK293 cells assessed as decrease in forskolin-stimulated cAMP levels after 30 mins
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 1 (CHEMBL3571)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel C-Ring-Hydroxy-Substituted Controlled Deactivation Cannabinergic Analogues.
Kulkarni S, Nikas SP, Sharma R, Jiang S, Paronis CA, Leonard MZ, Zhang B, Honrao C, Mallipeddi S, Raghav JG, Benchama O, Järbe TU, Bergman J, Makriyannis A.
J Med Chem (2016) 59 : 6903 -6919
PubMed 27367336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.34 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4470925 1 8.60
CHEMBL4475022 1 8.34
CHEMBL4465566 1 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4470925 EC50 = 2.5 nM 8.60
CHEMBL4475022 EC50 = 4.6 nM 8.34
CHEMBL4465566 EC50 = 8.6 nM 8.07