Assay Detail
Binding
CHEMBL933109
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Displacement of [3H]PGE4 from human EP4 receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Prostaglandin E2 receptor EP4 subtype (CHEMBL1836) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and evaluation of a gamma-lactam as a highly selective EP2 and EP4 receptor agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.74 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL258332 | — | — | 1 | 10.70 |
| CHEMBL272276 | — | — | 1 | 10.30 |
| CHEMBL548 | DINOPROSTONE | 4.0 | 1 | 9.10 |
| CHEMBL251294 | — | — | 1 | 9.00 |
| CHEMBL257217 | — | — | 1 | 9.00 |
| CHEMBL222715 | — | — | 1 | 8.70 |
| CHEMBL272277 | — | — | 1 | 8.70 |
| CHEMBL257658 | — | — | 1 | 8.05 |
| CHEMBL271488 | — | — | 1 | 7.57 |
| CHEMBL272969 | — | — | 1 | 6.31 |
| CHEMBL271896 | BUTAPROST | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL258332 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL272276 | — | Ki | = | 0.05 | nM | 10.30 |
| CHEMBL548 | DINOPROSTONE | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL251294 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL257217 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL222715 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL272277 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL257658 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL271488 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL272969 | — | Ki | = | 490.0 | nM | 6.31 |
| CHEMBL271896 | BUTAPROST | Ki | > | 10000.0 | nM | - |