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Assay Detail

CHEMBL3588430

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

Binding
Displacement of [3H]-PGE2 from human EP2 receptor overexpressed in human ECV304 cell membranes by scintillation proximity assay
ChEMBL ↗
54
Total Activities
54
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 EP2 subtype (CHEMBL1881) ↗
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 54 6.21 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3586362 — — 1 8.70
CHEMBL3586361 — — 1 8.10
CHEMBL3586360 — — 1 8.10
CHEMBL3586359 — — 1 7.70
CHEMBL3586312 — — 1 7.70
CHEMBL3586347 — — 1 7.52
CHEMBL3586340 — — 1 7.22
CHEMBL3586309 — — 1 7.16
CHEMBL3586353 — — 1 7.10
CHEMBL3586342 — — 1 7.10
CHEMBL3586346 — — 1 7.05
CHEMBL3586314 — — 1 7.00
CHEMBL3586322 — — 1 7.00
CHEMBL3586324 — — 1 7.00
CHEMBL3586345 — — 1 7.00
CHEMBL3586313 — — 1 6.70
CHEMBL3586352 — — 1 6.70
CHEMBL3586311 — — 1 6.70
CHEMBL3586315 — — 1 6.70
CHEMBL3586328 — — 1 6.52
CHEMBL3586337 — — 1 6.52
CHEMBL3586341 — — 1 6.40
CHEMBL3586335 — — 1 6.40
CHEMBL3586320 — — 1 6.22
CHEMBL3586321 — — 1 6.22
CHEMBL3586310 — — 1 6.16
CHEMBL3586333 — — 1 6.16
CHEMBL3586343 — — 1 6.10
CHEMBL3586348 — — 1 5.96
CHEMBL3586339 — — 1 5.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3586362 — IC50 = 2.0 nM 8.70
CHEMBL3586361 — IC50 = 8.0 nM 8.10
CHEMBL3586360 — IC50 = 8.0 nM 8.10
CHEMBL3586359 — IC50 = 20.0 nM 7.70
CHEMBL3586312 — IC50 = 20.0 nM 7.70
CHEMBL3586347 — IC50 = 30.0 nM 7.52
CHEMBL3586340 — IC50 = 60.0 nM 7.22
CHEMBL3586309 — IC50 = 70.0 nM 7.16
CHEMBL3586353 — IC50 = 80.0 nM 7.10
CHEMBL3586342 — IC50 = 80.0 nM 7.10
CHEMBL3586346 — IC50 = 90.0 nM 7.05
CHEMBL3586345 — IC50 = 100.0 nM 7.00
CHEMBL3586324 — IC50 = 100.0 nM 7.00
CHEMBL3586322 — IC50 = 100.0 nM 7.00
CHEMBL3586314 — IC50 = 100.0 nM 7.00
CHEMBL3586313 — IC50 = 200.0 nM 6.70
CHEMBL3586315 — IC50 = 200.0 nM 6.70
CHEMBL3586311 — IC50 = 200.0 nM 6.70
CHEMBL3586352 — IC50 = 200.0 nM 6.70
CHEMBL3586328 — IC50 = 300.0 nM 6.52
CHEMBL3586337 — IC50 = 300.0 nM 6.52
CHEMBL3586341 — IC50 = 400.0 nM 6.40
CHEMBL3586335 — IC50 = 400.0 nM 6.40
CHEMBL3586320 — IC50 = 600.0 nM 6.22
CHEMBL3586321 — IC50 = 600.0 nM 6.22
CHEMBL3586310 — IC50 = 700.0 nM 6.16
CHEMBL3586333 — IC50 = 700.0 nM 6.16
CHEMBL3586343 — IC50 = 800.0 nM 6.10
CHEMBL3586348 — IC50 = 1100.0 nM 5.96
CHEMBL3586339 — IC50 = 1100.0 nM 5.96
CHEMBL3586349 — IC50 = 1500.0 nM 5.82
CHEMBL3586354 — IC50 = 1600.0 nM 5.80
CHEMBL3586319 — IC50 = 1800.0 nM 5.75
CHEMBL3586338 — IC50 = 2700.0 nM 5.57
CHEMBL3586326 — IC50 = 2800.0 nM 5.55
CHEMBL3586356 — IC50 = 4000.0 nM 5.40
CHEMBL3586344 — IC50 = 5600.0 nM 5.25
CHEMBL3586355 — IC50 = 6000.0 nM 5.22
CHEMBL3586336 — IC50 = 6400.0 nM 5.19
CHEMBL3586316 — IC50 = 10000.0 nM 5.00
CHEMBL3586334 — IC50 = 10000.0 nM 5.00
CHEMBL3586332 — IC50 = 12000.0 nM 4.92
CHEMBL3586357 — IC50 = 13000.0 nM 4.89
CHEMBL3586350 — IC50 = 14000.0 nM 4.85
CHEMBL3586327 — IC50 = 15000.0 nM 4.82
CHEMBL3586330 — IC50 = 15000.0 nM 4.82
CHEMBL3586323 — IC50 = 30000.0 nM 4.52
CHEMBL3586317 — IC50 = 30000.0 nM 4.52
CHEMBL3586318 — IC50 = 30000.0 nM 4.52
CHEMBL3586358 — IC50 > 30000.0 nM -