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Assay Detail

CHEMBL4047582

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at OXE receptor in human neutrophils assessed as inhibition of 5-oxo-ETE-induced calcium mobilization incubated for 2 mins followed by 5-oxo-ETE addition measured after 1 min by fluorescence assay
12
Total Activities
12
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

Structure-activity relationship study of β-oxidation resistant indole-based 5-oxo-6,8,11,14-eicosatetraenoic acid (5-oxo-ETE) receptor antagonists.
Ye Q, Chourey S, Wang R, Chintam NR, Gravel S, Powell WS, Rokach J.
Bioorg Med Chem Lett (2017) 27 : 4770 -4776
PubMed 28943042 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.32 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3341972 1 8.22
CHEMBL3115775 1 7.80
CHEMBL4084871 1 7.64
CHEMBL4081391 1 6.24
CHEMBL4091674 1 6.14
CHEMBL4070005 1 5.95
CHEMBL4070795 1 5.88
CHEMBL4090987 1 5.87
CHEMBL4096962 1 5.39
CHEMBL4096265 1 5.26
CHEMBL4069768 1 5.09
CHEMBL3341971 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3341972 IC50 = 6.0 nM 8.22
CHEMBL3115775 IC50 = 16.0 nM 7.80
CHEMBL4084871 IC50 = 23.0 nM 7.64
CHEMBL4081391 IC50 = 580.0 nM 6.24
CHEMBL4091674 IC50 = 720.0 nM 6.14
CHEMBL4070005 IC50 = 1120.0 nM 5.95
CHEMBL4070795 IC50 = 1330.0 nM 5.88
CHEMBL4090987 IC50 = 1360.0 nM 5.87
CHEMBL4096962 IC50 = 4060.0 nM 5.39
CHEMBL4096265 IC50 = 5500.0 nM 5.26
CHEMBL4069768 IC50 = 8150.0 nM 5.09
CHEMBL3341971 IC50 = 2700.0 nM -