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Assay Detail

CHEMBL1287587

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

Functional
Agonist activity at human CB2 receptor expressed in CHO cells assessed as stimulation of [35S]GTPgammaS binding after 1.5 hrs by liquid scintillation spectrophotometry
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cannabinoid receptor 2 (CHEMBL253)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-Bromo-3-(1',1'-dimethylalkyl)-1-deoxy-Δ(8)-tetrahydrocannabinols: New selective ligands for the cannabinoid CB(2) receptor.
Huffman JW, Hepburn SA, Lyutenko N, Thompson AL, Wiley JL, Selley DE, Martin BR.
Bioorg Med Chem (2010) 18 : 7809 -7815
PubMed 20943404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.03 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371214 1 8.40
CHEMBL498346 1 8.34
CHEMBL1277593 1 7.82
CHEMBL1277592 1 7.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371214 EC50 = 4.0 nM 8.40
CHEMBL498346 EC50 = 4.6 nM 8.34
CHEMBL1277593 EC50 = 15.0 nM 7.82
CHEMBL1277592 EC50 = 28.6 nM 7.54