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Assay Detail

CHEMBL658203

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

Functional
Effective concentration for inhibition of Cannabinoid receptor 1-mediated adenylyl cyclase activity using African green monkey (COS-7) cells transfected with the cDNA of rat CB1 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Cannabinol derivatives: binding to cannabinoid receptors and inhibition of adenylylcyclase.
Rhee MH, Vogel Z, Barg J, Bayewitch M, Levy R, Hanus L, Breuer A, Mechoulam R.
J Med Chem (1997) 40 : 3228 -3233
PubMed 9379442 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 8.31 10.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432107 1 10.46
CHEMBL111724 1 10.25
CHEMBL109393 1 9.74
CHEMBL111148 1 9.24
CHEMBL111340 1 8.62
CHEMBL113230 1 8.02
CHEMBL465 DRONABINOL 4.0 1 7.96
CHEMBL111702 1 7.88
CHEMBL111099 1 7.40
CHEMBL109972 1 7.24
CHEMBL74415 CANNABINOL 3.0 1 6.92
CHEMBL320408 1 6.03

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432107 EC50 = 0.035 nM 10.46
CHEMBL111724 EC50 = 0.056 nM 10.25
CHEMBL109393 EC50 = 0.18 nM 9.74
CHEMBL111148 EC50 = 0.58 nM 9.24
CHEMBL111340 EC50 = 2.4 nM 8.62
CHEMBL113230 EC50 = 9.6 nM 8.02
CHEMBL465 DRONABINOL EC50 = 11.0 nM 7.96
CHEMBL111702 EC50 = 13.3 nM 7.88
CHEMBL111099 EC50 = 39.9 nM 7.40
CHEMBL109972 EC50 = 58.1 nM 7.24
CHEMBL74415 CANNABINOL EC50 = 120.0 nM 6.92
CHEMBL320408 EC50 = 927.0 nM 6.03