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Assay Detail

CHEMBL888167

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Functional
Agonist activity at human CB2 in CHO cells assessed as inhibition of cAMP production
3
Total Activities
3
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 Intermediate

Target

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

Publication

2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: discovery of CB2 receptor selective compounds.
Kai H, Morioka Y, Murashi T, Morita K, Shinonome S, Nakazato H, Kawamoto K, Hanasaki K, Takahashi F, Mihara S, Arai T, Abe K, Okabe H, Baba T, Yoshikawa T, Takenaka H.
Bioorg Med Chem Lett (2007) 17 : 4030 -4034
PubMed 17521907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.89 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188 WIN-552122 1 8.96
CHEMBL232730 1 8.21
CHEMBL248135 1 6.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188 WIN-552122 IC50 = 1.1 nM 8.96
CHEMBL232730 IC50 = 6.1 nM 8.21
CHEMBL248135 IC50 = 322.0 nM 6.49