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Assay Detail

CHEMBL830430

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Binding
Ability to inhibit the binding of [3H]PGD-2 radioligand to membranes of CHO cells stably expressing mouse Prostaglandin E receptor EP3
14
Total Activities
14
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 Expert

Target

Prostaglandin E2 receptor EP3 subtype (CHEMBL4336)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of orally active prostaglandin D2 receptor antagonists.
Torisu K, Kobayashi K, Iwahashi M, Nakai Y, Onoda T, Nagase T, Sugimoto I, Okada Y, Matsumoto R, Nanbu F, Ohuchida S, Nakai H, Toda M.
Bioorg Med Chem Lett (2004) 14 : 4891 -4895
PubMed 15341946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.78 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184684 1 6.12
CHEMBL363984 1 6.01
CHEMBL365243 1 5.92
CHEMBL364841 1 5.77
CHEMBL185251 1 5.77
CHEMBL361457 1 5.66
CHEMBL182555 1 5.48
CHEMBL186925 1 5.48
CHEMBL365908 1 -
CHEMBL365696 1 -
CHEMBL186735 1 -
CHEMBL365829 1 -
CHEMBL359564 1 -
CHEMBL364593 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL184684 Ki = 750.0 nM 6.12
CHEMBL363984 Ki = 980.0 nM 6.01
CHEMBL365243 Ki = 1200.0 nM 5.92
CHEMBL364841 Ki = 1700.0 nM 5.77
CHEMBL185251 Ki = 1700.0 nM 5.77
CHEMBL361457 Ki = 2200.0 nM 5.66
CHEMBL182555 Ki = 3300.0 nM 5.48
CHEMBL186925 Ki = 3300.0 nM 5.48
CHEMBL365908 Ki > 10000.0 nM -
CHEMBL365696 Ki > 10000.0 nM -
CHEMBL186735 Ki > 10000.0 nM -
CHEMBL365829 Ki > 10000.0 nM -
CHEMBL359564 Ki > 10000.0 nM -
CHEMBL364593 Ki > 10000.0 nM -