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Assay Detail

CHEMBL3588433

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

Binding
Displacement of [3H]-PGE2 from human EP4 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type ECV-304
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin E2 receptor EP4 subtype (CHEMBL1836)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A selective prostaglandin E2 receptor subtype 2 (EP2) antagonist increases the macrophage-mediated clearance of amyloid-beta plaques.
Fox BM, Beck HP, Roveto PM, Kayser F, Cheng Q, Dou H, Williamson T, Treanor J, Liu H, Jin L, Xu G, Ma J, Wang S, Olson SH.
J Med Chem (2015) 58 : 5256 -5273
PubMed 26061158 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 4.91 5.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3586353 1 5.50
CHEMBL3586309 1 5.46
CHEMBL3586359 1 4.75
CHEMBL3586362 1 4.70
CHEMBL3586361 1 4.52
CHEMBL3586360 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3586353 IC50 = 3200.0 nM 5.50
CHEMBL3586309 IC50 = 3500.0 nM 5.46
CHEMBL3586359 IC50 = 18000.0 nM 4.75
CHEMBL3586362 IC50 = 20000.0 nM 4.70
CHEMBL3586361 IC50 = 30000.0 nM 4.52
CHEMBL3586360 IC50 = 30000.0 nM 4.52