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Assay Detail

CHEMBL2395561

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Functional
Antagonist activity at human GPR55 expressed in CHO cells assessed as inhibition of lysophosphotidylinositol-induced beta-arrestin recruitment preincubated for 30 mins followed by lysophosphotidylinositol induction by beta-galactosidase reporter gene assay
5
Total Activities
5
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

G-protein coupled receptor 55 (CHEMBL1075322)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

8-Benzamidochromen-4-one-2-carboxylic acids: potent and selective agonists for the orphan G protein-coupled receptor GPR35.
Funke M, Thimm D, Schiedel AC, Müller CE.
J Med Chem (2013) 56 : 5182 -5197
PubMed 23713606 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.82 5.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2392183 1 5.21
CHEMBL2392182 1 5.05
CHEMBL2392179 1 4.66
CHEMBL2392174 1 4.66
CHEMBL2392151 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2392183 IC50 = 6200.0 nM 5.21
CHEMBL2392182 IC50 = 8920.0 nM 5.05
CHEMBL2392179 IC50 = 21700.0 nM 4.66
CHEMBL2392174 IC50 = 21700.0 nM 4.66
CHEMBL2392151 IC50 = 29100.0 nM 4.54