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Assay Detail

CHEMBL4367885

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Functional
Agonist activity at recombinant human CB2R expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels after 30 mins by chemiluminescent detection based cAMP Hunter assay
3
Total Activities
3
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

Structure-activity relationships of thiazole and benzothiazole derivatives as selective cannabinoid CB2 agonists with in vivo anti-inflammatory properties.
Ghonim AE, Ligresti A, Rabbito A, Mahmoud AM, Di Marzo V, Osman NA, Abadi AH.
Eur J Med Chem (2019) 180 : 154 -170
PubMed 31302448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 6.97 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4437741 1 7.24
CHEMBL4559193 1 7.17
CHEMBL4592199 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4437741 EC50 = 57.0 nM 7.24
CHEMBL4559193 EC50 = 68.0 nM 7.17
CHEMBL4592199 EC50 = 306.0 nM 6.51