Assay Detail
Binding
CHEMBL888232
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Displacement of [3H]PGE2 from human EP4 receptor expressed in HEK293 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Prostaglandin E2 receptor EP4 subtype (CHEMBL1836) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel prostaglandin analogs of PGE2 as potent and selective EP2 and EP4 receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.55 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL548 | DINOPROSTONE | 4.0 | 1 | 9.10 |
| CHEMBL251294 | — | — | 1 | 8.60 |
| CHEMBL251505 | — | — | 1 | 8.40 |
| CHEMBL251710 | — | — | 1 | 7.62 |
| CHEMBL251709 | — | — | 1 | 7.60 |
| CHEMBL248679 | — | — | 1 | 7.54 |
| CHEMBL398947 | — | — | 1 | 7.35 |
| CHEMBL248678 | — | — | 1 | 6.93 |
| CHEMBL398948 | — | — | 1 | 6.84 |
| CHEMBL251504 | — | — | 1 | 6.74 |
| CHEMBL2096894 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL548 | DINOPROSTONE | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL251294 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL251505 | — | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL251710 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL251709 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL248679 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL398947 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL248678 | — | Ki | = | 117.0 | nM | 6.93 |
| CHEMBL398948 | — | Ki | = | 145.0 | nM | 6.84 |
| CHEMBL251504 | — | Ki | = | 181.0 | nM | 6.74 |
| CHEMBL2096894 | — | Ki | = | 443.0 | nM | 6.35 |