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Assay Detail

CHEMBL4256853

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
18
Total Activities
18
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

Novel Highly Potent and Metabolically Resistant Oxoeicosanoid (OXE) Receptor Antagonists That Block the Actions of the Granulocyte Chemoattractant 5-Oxo-6,8,11,14-Eicosatetraenoic Acid (5-oxo-ETE).
Chourey S, Ye Q, Reddy CN, Wang R, Cossette C, Gravel S, Slobodchikova I, Vuckovic D, Rokach J, Powell WS.
J Med Chem (2018) 61 : 5934 -5948
PubMed 29972644 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.80 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4283608 1 9.92
CHEMBL4287941 1 9.55
CHEMBL4281149 1 9.42
CHEMBL4282356 1 8.68
CHEMBL3341972 1 8.22
CHEMBL4284672 1 7.96
CHEMBL4277299 1 7.92
CHEMBL3115775 1 7.77
CHEMBL3115774 1 7.77
CHEMBL4291346 1 7.75
CHEMBL4291464 1 7.64
CHEMBL4279605 1 7.42
CHEMBL4278772 1 7.42
CHEMBL4277207 1 6.92
CHEMBL4280693 1 6.68
CHEMBL4287509 1 6.65
CHEMBL4285167 1 6.58
CHEMBL4292357 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4283608 IC50 = 0.12 nM 9.92
CHEMBL4287941 IC50 = 0.28 nM 9.55
CHEMBL4281149 IC50 = 0.38 nM 9.42
CHEMBL4282356 IC50 = 2.1 nM 8.68
CHEMBL3341972 IC50 = 6.0 nM 8.22
CHEMBL4284672 IC50 = 11.0 nM 7.96
CHEMBL4277299 IC50 = 12.0 nM 7.92
CHEMBL3115775 IC50 = 17.0 nM 7.77
CHEMBL3115774 IC50 = 17.0 nM 7.77
CHEMBL4291346 IC50 = 18.0 nM 7.75
CHEMBL4291464 IC50 = 23.0 nM 7.64
CHEMBL4279605 IC50 = 38.0 nM 7.42
CHEMBL4278772 IC50 = 38.0 nM 7.42
CHEMBL4277207 IC50 = 120.0 nM 6.92
CHEMBL4280693 IC50 = 210.0 nM 6.68
CHEMBL4287509 IC50 = 223.0 nM 6.65
CHEMBL4285167 IC50 = 260.0 nM 6.58
CHEMBL4292357 IC50 = 750.0 nM 6.12