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Assay Detail

CHEMBL2154449

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Functional
Agonist activity at human CB2 receptor expressed in CHO cell membranes after 1 hr by [35S]GTPgammaS binding assay
6
Total Activities
6
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

Scaffold hopping strategy toward original pyrazolines as selective CB₂ receptor ligands.
Gembus V, Furman C, Millet R, Mansouri R, Chavatte P, Levacher V, Brière JF.
Eur J Med Chem (2012) 58 : 396 -404
PubMed 23151320 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.92 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381689 SR-144528 1 8.68
CHEMBL188 WIN-552122 1 7.05
CHEMBL2151380 1 6.72
CHEMBL2151370 1 6.53
CHEMBL2151379 1 6.43
CHEMBL2151377 1 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381689 SR-144528 EC50 = 2.1 nM 8.68
CHEMBL188 WIN-552122 EC50 = 89.6 nM 7.05
CHEMBL2151380 EC50 = 191.0 nM 6.72
CHEMBL2151370 EC50 = 297.0 nM 6.53
CHEMBL2151379 EC50 = 371.0 nM 6.43
CHEMBL2151377 EC50 = 749.0 nM 6.13