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Assay Detail

CHEMBL4124581

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Functional
Agonist activity at human PK-tagged OXER1 expressed in CHOK1 cells assessed as EA-tagged beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation assay
6
Total Activities
6
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

Oxoeicosanoid receptor 1 (CHEMBL1628461)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, molecular modelling studies and biological evaluation of new oxoeicosanoid receptor 1 agonists.
Stepniewski TM, Torrens-Fontanals M, Rodríguez-Espigares I, Giorgino T, Primdahl KG, Vik A, Stenstrøm Y, Selent J, Hansen TV.
Bioorg Med Chem (2018) 26 : 3580 -3587
PubMed 29866479 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.14 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18028 5-OXO-ETE 1 6.66
CHEMBL4127146 1 6.42
CHEMBL165682 1 5.81
CHEMBL4130040 1 5.68
CHEMBL4128214 1 -
CHEMBL4128585 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18028 5-OXO-ETE EC50 = 220.0 nM 6.66
CHEMBL4127146 EC50 = 380.0 nM 6.42
CHEMBL165682 EC50 = 1540.0 nM 5.81
CHEMBL4130040 EC50 = 2080.0 nM 5.68
CHEMBL4128214 EC50 > 100000.0 nM -
CHEMBL4128585 EC50 > 100000.0 nM -