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Assay Detail

CHEMBL3364790

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Functional
Partial agonist activity at human cannabinoid CB2 receptor expressed in CHO-K1 cells assessed as [S35]GTPgammaS binding by scintillation counting
15
Total Activities
15
Compounds Tested
1
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 2 (CHEMBL253)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

One-pot heterogeneous synthesis of Δ(3)-tetrahydrocannabinol analogues and xanthenes showing differential binding to CB(1) and CB(2) receptors.
Rosati O, Messina F, Pelosi A, Curini M, Petrucci V, Gertsch J, Chicca A.
Eur J Med Chem (2014) 85 : 77 -86
PubMed 25072877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 7.30 8.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL559612 CP-55940 1 8.03
CHEMBL3329945 1 7.96
CHEMBL465 DRONABINOL 4.0 1 7.91
CHEMBL3329946 1 7.76
CHEMBL3329480 1 6.09
CHEMBL3329481 1 6.03
CHEMBL3329477 1 -
CHEMBL3329478 1 -
CHEMBL3329479 1 -
CHEMBL3329482 1 -
CHEMBL3329483 1 -
CHEMBL3329943 1 -
CHEMBL3329944 1 -
CHEMBL3329947 1 -
CHEMBL188 WIN-552122 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL559612 CP-55940 EC50 = 9.3 nM 8.03
CHEMBL3329945 EC50 = 10.9 nM 7.96
CHEMBL465 DRONABINOL EC50 = 12.3 nM 7.91
CHEMBL3329946 EC50 = 17.4 nM 7.76
CHEMBL3329480 EC50 = 820.0 nM 6.09
CHEMBL3329481 EC50 = 930.0 nM 6.03
CHEMBL3329477 EC50 - -
CHEMBL3329478 EC50 - -
CHEMBL3329479 EC50 - -
CHEMBL3329482 EC50 - -
CHEMBL3329483 EC50 - -
CHEMBL3329943 EC50 - -
CHEMBL3329944 EC50 - -
CHEMBL3329947 EC50 - -
CHEMBL188 WIN-552122 EC50 - -