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Assay Detail

CHEMBL657302

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

Functional
Effective concentration for inhibition of human Cannabinoid receptor 2-mediated adenylyl cyclase using African green monkey (COS-7) cells transfected with the cDNA of human CB2 receptor
9
Total Activities
9
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 2 (CHEMBL253)
Type SINGLE PROTEIN
Organism Homo sapiens

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 9 8.38 10.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432107 1 10.11
CHEMBL111724 1 9.68
CHEMBL109393 1 9.10
CHEMBL111148 1 9.00
CHEMBL113230 1 8.34
CHEMBL111340 1 8.27
CHEMBL111702 1 7.41
CHEMBL320408 1 6.93
CHEMBL74415 CANNABINOL 3.0 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432107 EC50 = 0.078 nM 10.11
CHEMBL111724 EC50 = 0.208 nM 9.68
CHEMBL109393 EC50 = 0.79 nM 9.10
CHEMBL111148 EC50 = 1.01 nM 9.00
CHEMBL113230 EC50 = 4.6 nM 8.34
CHEMBL111340 EC50 = 5.4 nM 8.27
CHEMBL111702 EC50 = 39.3 nM 7.41
CHEMBL320408 EC50 = 116.2 nM 6.93
CHEMBL74415 CANNABINOL EC50 = 261.2 nM 6.58