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Assay Detail

CHEMBL1104422

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 counter
10
Total Activities
10
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 N-acylsulfonamide analogs as potent and selective EP3 receptor antagonists.
Asada M, Obitsu T, Kinoshita A, Nakai Y, Nagase T, Sugimoto I, Tanaka M, Takizawa H, Yoshikawa K, Sato K, Narita M, Ohuchida S, Nakai H, Toda M.
Bioorg Med Chem Lett (2010) 20 : 2639 -2643
PubMed 20346663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.66 6.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1092432 1 6.15
CHEMBL1091743 1 5.75
CHEMBL1092431 1 5.64
CHEMBL1091741 1 5.62
CHEMBL1093820 1 5.60
CHEMBL1090937 1 5.46
CHEMBL1091744 1 5.43
CHEMBL1092976 1 -
CHEMBL1090938 1 -
CHEMBL1092097 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1092432 Ki = 710.0 nM 6.15
CHEMBL1091743 Ki = 1800.0 nM 5.75
CHEMBL1092431 Ki = 2300.0 nM 5.64
CHEMBL1091741 Ki = 2400.0 nM 5.62
CHEMBL1093820 Ki = 2500.0 nM 5.60
CHEMBL1090937 Ki = 3500.0 nM 5.46
CHEMBL1091744 Ki = 3700.0 nM 5.43
CHEMBL1092976 Ki > 10000.0 nM -
CHEMBL1090938 Ki > 10000.0 nM -
CHEMBL1092097 Ki > 10000.0 nM -