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Assay Detail

CHEMBL840047

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

Binding
Binding affinity against Prostaglandin E receptor in presence of 2% human serum albumin
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Prostaglandin E2 receptor EP1 subtype (CHEMBL1811)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,3-Diarylthiophenes as selective EP1 receptor antagonists.
Ducharme Y, Blouin M, Carrière MC, Chateauneuf A, Côté B, Denis D, Frenette R, Greig G, Kargman S, Lamontagne S, Martins E, Nantel F, O'Neill G, Sawyer N, Metters KM, Friesen RW.
Bioorg Med Chem Lett (2005) 15 : 1155 -1160
PubMed 15686932 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.43 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL185346 1 8.30
CHEMBL180046 1 8.30
CHEMBL182368 1 8.22
CHEMBL360592 1 7.77
CHEMBL2113029 1 7.75
CHEMBL362543 1 7.16
CHEMBL182662 1 7.14
CHEMBL184947 1 7.05
CHEMBL182623 1 6.80
CHEMBL184779 1 6.66
CHEMBL362851 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL185346 Ki = 5.0 nM 8.30
CHEMBL180046 Ki = 5.0 nM 8.30
CHEMBL182368 Ki = 6.0 nM 8.22
CHEMBL360592 Ki = 17.0 nM 7.77
CHEMBL2113029 Ki = 18.0 nM 7.75
CHEMBL362543 Ki = 70.0 nM 7.16
CHEMBL182662 Ki = 72.0 nM 7.14
CHEMBL184947 Ki = 90.0 nM 7.05
CHEMBL182623 Ki = 160.0 nM 6.80
CHEMBL184779 Ki = 220.0 nM 6.66
CHEMBL362851 Ki = 280.0 nM 6.55