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Assay Detail

CHEMBL929255

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

Functional
Agonist activity at human cloned CB2 receptor by [35S]GTP-gamma-S binding assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Sulfamoyl benzamides as novel CB2 cannabinoid receptor ligands.
Worm K, Zhou QJ, Saeui CT, Green RC, Cassel JA, Stabley GJ, DeHaven RN, Conway-James N, LaBuda CJ, Koblish M, Little PJ, Dolle RE.
Bioorg Med Chem Lett (2008) 18 : 2830 -2835
PubMed 18430570 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 7.64 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL256753 1 8.37
CHEMBL255474 1 8.34
CHEMBL256752 1 8.18
CHEMBL256962 1 8.06
CHEMBL442447 1 8.03
CHEMBL256110 1 7.92
CHEMBL255096 1 7.85
CHEMBL258242 1 7.68
CHEMBL404650 1 7.60
CHEMBL258243 1 7.60
CHEMBL255681 1 7.36
CHEMBL258244 1 7.32
CHEMBL404457 1 6.90
CHEMBL429851 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL256753 EC50 = 4.3 nM 8.37
CHEMBL255474 EC50 = 4.6 nM 8.34
CHEMBL256752 EC50 = 6.6 nM 8.18
CHEMBL256962 EC50 = 8.8 nM 8.06
CHEMBL442447 EC50 = 9.3 nM 8.03
CHEMBL256110 EC50 = 12.0 nM 7.92
CHEMBL255096 EC50 = 14.0 nM 7.85
CHEMBL258242 EC50 = 21.0 nM 7.68
CHEMBL404650 EC50 = 25.0 nM 7.60
CHEMBL258243 EC50 = 25.0 nM 7.60
CHEMBL255681 EC50 = 44.0 nM 7.36
CHEMBL258244 EC50 = 48.0 nM 7.32
CHEMBL404457 EC50 = 125.0 nM 6.90
CHEMBL429851 EC50 = 1800.0 nM 5.75