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Assay Detail

CHEMBL931258

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Functional
Antagonist activity against EP3 receptor by FLIPR assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Prostaglandin E2 receptor EP3 subtype (CHEMBL3710)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.
Hall A, Billinton A, Brown SH, Chowdhury A, Giblin GM, Goldsmith P, Hurst DN, Naylor A, Patel S, Scoccitti T, Theobald PJ.
Bioorg Med Chem Lett (2008) 18 : 2684 -2690
PubMed 18378447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.33 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL257997 1 6.50
CHEMBL257134 1 6.40
CHEMBL255675 1 6.40
CHEMBL403407 1 6.30
CHEMBL402392 1 6.30
CHEMBL254763 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL257997 Ki = 316.23 nM 6.50
CHEMBL257134 Ki = 398.11 nM 6.40
CHEMBL255675 Ki = 398.11 nM 6.40
CHEMBL403407 Ki = 501.19 nM 6.30
CHEMBL402392 Ki = 501.19 nM 6.30
CHEMBL254763 Ki = 794.33 nM 6.10