Assay Detail
Binding
CHEMBL1045307
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]PGE2 from human EP2 receptor after 1 hr by liquid scintillation counting
5
Total Activities
5
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
Prostaglandin E2 receptor EP2 subtype (CHEMBL1881) ↗| 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.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.02 | 5.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL565591 | — | — | 1 | 5.38 |
| CHEMBL565992 | — | — | 1 | 5.32 |
| CHEMBL467632 | — | — | 1 | 4.91 |
| CHEMBL565799 | — | — | 1 | 4.48 |
| CHEMBL585581 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL565591 | — | IC50 | = | 4169.0 | nM | 5.38 |
| CHEMBL565992 | — | IC50 | = | 4832.0 | nM | 5.32 |
| CHEMBL467632 | — | IC50 | = | 12261.0 | nM | 4.91 |
| CHEMBL565799 | — | IC50 | = | 32921.0 | nM | 4.48 |
| CHEMBL585581 | — | IC50 | > | 10000.0 | nM | - |