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Assay Detail

CHEMBL1961333

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

Binding
Displacement of [3H]-PGE2 from mouse EP4 receptor expressed in CHO cells after 60 mins by scintillation counting
22
Total Activities
22
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 EP4 subtype (CHEMBL2489)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of novel prostaglandin analogs as potent and selective EP2/EP4 dual agonists.
Kambe T, Maruyama T, Nakai Y, Yoshida H, Oida H, Maruyama T, Abe N, Nishiura A, Nakai H, Toda M.
Bioorg Med Chem (2012) 20 : 2235 -2251
PubMed 22386979 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 8.52 10.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1957437 1 10.92
CHEMBL1933722 1 9.39
CHEMBL1933724 1 9.30
CHEMBL1933719 1 9.22
CHEMBL1957430 1 9.10
CHEMBL1957434 1 9.10
CHEMBL1957436 1 9.09
CHEMBL1933718 1 9.05
CHEMBL1957435 1 9.03
CHEMBL1933725 1 8.82
CHEMBL222715 1 8.77
CHEMBL1933717 1 8.74
CHEMBL223151 1 8.70
CHEMBL548 DINOPROSTONE 4.0 1 8.51
CHEMBL1933723 1 8.26
CHEMBL1957308 1 8.05
CHEMBL42027 1 8.04
CHEMBL1933721 1 7.92
CHEMBL1933720 1 7.46
CHEMBL1957433 1 7.28
CHEMBL1957432 1 7.11
CHEMBL1957431 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1957437 Ki = 0.012 nM 10.92
CHEMBL1933722 Ki = 0.41 nM 9.39
CHEMBL1933724 Ki = 0.5 nM 9.30
CHEMBL1933719 Ki = 0.6 nM 9.22
CHEMBL1957430 Ki = 0.8 nM 9.10
CHEMBL1957434 Ki = 0.8 nM 9.10
CHEMBL1957436 Ki = 0.81 nM 9.09
CHEMBL1933718 Ki = 0.9 nM 9.05
CHEMBL1957435 Ki = 0.94 nM 9.03
CHEMBL1933725 Ki = 1.5 nM 8.82
CHEMBL222715 Ki = 1.7 nM 8.77
CHEMBL1933717 Ki = 1.8 nM 8.74
CHEMBL223151 Ki = 2.0 nM 8.70
CHEMBL548 DINOPROSTONE Ki = 3.1 nM 8.51
CHEMBL1933723 Ki = 5.5 nM 8.26
CHEMBL1957308 Ki = 9.0 nM 8.05
CHEMBL42027 Ki = 9.2 nM 8.04
CHEMBL1933721 Ki = 12.0 nM 7.92
CHEMBL1933720 Ki = 35.0 nM 7.46
CHEMBL1957433 Ki = 53.0 nM 7.28
CHEMBL1957432 Ki = 78.0 nM 7.11
CHEMBL1957431 Ki = 3000.0 nM 5.52