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Assay Detail

CHEMBL1073246

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 by liquid scintillation counting
19
Total Activities
19
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 a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.
Asada M, Obitsu T, Nagase T, Sugimoto I, Yamaura Y, Sato K, Narita M, Ohuchida S, Nakai H, Toda M.
Bioorg Med Chem (2009) 17 : 6567 -6582
PubMed 19700331 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 5.72 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL595632 1 6.17
CHEMBL593260 1 6.04
CHEMBL605833 1 5.96
CHEMBL595157 1 5.85
CHEMBL603653 1 5.68
CHEMBL594423 1 5.66
CHEMBL596515 1 5.66
CHEMBL594365 1 5.66
CHEMBL604897 1 5.64
CHEMBL593764 1 5.58
CHEMBL593041 1 5.58
CHEMBL595159 1 5.54
CHEMBL594210 1 5.37
CHEMBL593526 1 -
CHEMBL596499 1 -
CHEMBL603227 1 -
CHEMBL603625 1 -
CHEMBL603633 1 -
CHEMBL595830 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL595632 Ki = 670.0 nM 6.17
CHEMBL593260 Ki = 920.0 nM 6.04
CHEMBL605833 Ki = 1100.0 nM 5.96
CHEMBL595157 Ki = 1400.0 nM 5.85
CHEMBL603653 Ki = 2100.0 nM 5.68
CHEMBL594423 Ki = 2200.0 nM 5.66
CHEMBL596515 Ki = 2200.0 nM 5.66
CHEMBL594365 Ki = 2200.0 nM 5.66
CHEMBL604897 Ki = 2300.0 nM 5.64
CHEMBL593764 Ki = 2600.0 nM 5.58
CHEMBL593041 Ki = 2600.0 nM 5.58
CHEMBL595159 Ki = 2900.0 nM 5.54
CHEMBL594210 Ki = 4300.0 nM 5.37
CHEMBL593526 Ki > 10000.0 nM -
CHEMBL596499 Ki > 10000.0 nM -
CHEMBL603227 Ki > 10000.0 nM -
CHEMBL603625 Ki > 10000.0 nM -
CHEMBL603633 Ki > 10000.0 nM -
CHEMBL595830 Ki > 10000.0 nM -