Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1045309

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

Binding
Displacement of [3H]iloprost from human IP receptor after 1 hr by liquid scintillation counting
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Prostacyclin receptor (CHEMBL1995)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4,5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that does not prolong bleeding.
Singh J, Zeller W, Zhou N, Hategan G, Mishra RK, Polozov A, Yu P, Onua E, Zhang J, Ramírez JL, Sigthorsson G, Thorsteinnsdottir M, Kiselyov AS, Zembower DE, Andrésson T, Gurney ME.
J Med Chem (2010) 53 : 18 -36
PubMed 19957930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.04 5.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL565992 1 5.23
CHEMBL565799 1 5.05
CHEMBL565591 1 4.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL565992 IC50 = 5875.0 nM 5.23
CHEMBL565799 IC50 = 8823.0 nM 5.05
CHEMBL565591 IC50 = 14414.0 nM 4.84