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Assay Detail

CHEMBL888229

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

Binding
Displacement of [3H]PGE2 from human EP2 receptor expressed in HEK293 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Prostaglandin E2 receptor EP2 subtype (CHEMBL1881)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.
Xiao Y, Araldi GL, Zhao Z, Brugger N, Karra S, Fischer D, Palmer E.
Bioorg Med Chem Lett (2007) 17 : 4323 -4327
PubMed 17531488 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.89 8.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL548 DINOPROSTONE 4.0 1 8.31
CHEMBL398948 1 7.54
CHEMBL248678 1 7.22
CHEMBL251505 1 7.22
CHEMBL251709 1 7.06
CHEMBL251294 1 6.90
CHEMBL251504 1 6.87
CHEMBL251710 1 6.76
CHEMBL248679 1 6.13
CHEMBL2096894 1 6.10
CHEMBL398947 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL548 DINOPROSTONE Ki = 4.9 nM 8.31
CHEMBL398948 Ki = 29.0 nM 7.54
CHEMBL248678 Ki = 60.0 nM 7.22
CHEMBL251505 Ki = 60.0 nM 7.22
CHEMBL251709 Ki = 88.0 nM 7.06
CHEMBL251294 Ki = 125.5 nM 6.90
CHEMBL251504 Ki = 134.0 nM 6.87
CHEMBL251710 Ki = 173.0 nM 6.76
CHEMBL248679 Ki = 749.0 nM 6.13
CHEMBL2096894 Ki = 802.0 nM 6.10
CHEMBL398947 Ki = 1850.0 nM 5.73