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Assay Detail

CHEMBL1936148

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

Binding
Displacement of [3H]-PGE2 from mouse EP2 receptor expressed in CHO cells after 60 mins by liquid scintillation counting
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Prostaglandin E2 receptor EP2 subtype (CHEMBL2488)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of a novel EP2/EP4 dual agonist with high subtype-selectivity.
Kambe T, Maruyama T, Nakano M, Nakai Y, Yoshida T, Matsunaga N, Oida H, Konaka A, Maruyama T, Nakai H, Toda M.
Bioorg Med Chem Lett (2012) 22 : 396 -401
PubMed 22119471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.18 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1933724 1 8.52
CHEMBL1933722 1 8.03
CHEMBL1933728 1 7.89
CHEMBL1933726 1 7.82
CHEMBL1933725 1 7.72
CHEMBL548 DINOPROSTONE 4.0 1 7.66
CHEMBL1933727 1 7.38
CHEMBL1933721 1 7.08
CHEMBL1933719 1 6.90
CHEMBL1933720 1 6.62
CHEMBL1933723 1 6.50
CHEMBL222715 1 6.47
CHEMBL1933718 1 6.39
CHEMBL223151 1 5.60
CHEMBL42027 1 -
CHEMBL1933717 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1933724 Ki = 3.0 nM 8.52
CHEMBL1933722 Ki = 9.3 nM 8.03
CHEMBL1933728 Ki = 13.0 nM 7.89
CHEMBL1933726 Ki = 15.0 nM 7.82
CHEMBL1933725 Ki = 19.0 nM 7.72
CHEMBL548 DINOPROSTONE Ki = 22.0 nM 7.66
CHEMBL1933727 Ki = 42.0 nM 7.38
CHEMBL1933721 Ki = 84.0 nM 7.08
CHEMBL1933719 Ki = 127.0 nM 6.90
CHEMBL1933720 Ki = 240.0 nM 6.62
CHEMBL1933723 Ki = 320.0 nM 6.50
CHEMBL222715 Ki = 340.0 nM 6.47
CHEMBL1933718 Ki = 410.0 nM 6.39
CHEMBL223151 Ki = 2500.0 nM 5.60
CHEMBL42027 Ki > 10000.0 nM -
CHEMBL1933717 Ki > 10000.0 nM -