Assay Detail
Binding
CHEMBL925649
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Binding affinity at human prostaglandin EP4 receptor
19
Total Activities
19
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 EP4 subtype (CHEMBL1836) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.11 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL548 | DINOPROSTONE | 4.0 | 1 | 9.10 |
| CHEMBL249953 | — | — | 1 | 7.89 |
| CHEMBL249538 | — | — | 1 | 7.89 |
| CHEMBL249744 | — | — | 1 | 7.75 |
| CHEMBL398827 | — | — | 1 | 7.58 |
| CHEMBL404414 | — | — | 1 | 7.57 |
| CHEMBL400446 | — | — | 1 | 7.44 |
| CHEMBL400447 | — | — | 1 | 7.36 |
| CHEMBL249540 | — | — | 1 | 7.24 |
| CHEMBL249539 | — | — | 1 | 7.23 |
| CHEMBL249342 | — | — | 1 | 7.17 |
| CHEMBL249952 | — | — | 1 | 6.87 |
| CHEMBL249136 | — | — | 1 | 6.60 |
| CHEMBL249745 | — | — | 1 | 6.48 |
| CHEMBL249954 | — | — | 1 | 5.70 |
| CHEMBL404413 | — | — | 1 | 5.70 |
| CHEMBL249341 | — | — | 1 | 5.22 |
| CHEMBL271896 | BUTAPROST | 2.0 | 1 | - |
| CHEMBL250153 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL548 | DINOPROSTONE | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL249953 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL249538 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL249744 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL398827 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL404414 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL400446 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL400447 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL249540 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL249539 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL249342 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL249952 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL249136 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL249745 | — | Ki | = | 330.0 | nM | 6.48 |
| CHEMBL249954 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL404413 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL249341 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL271896 | BUTAPROST | Ki | > | 10000.0 | nM | - |
| CHEMBL250153 | — | Ki | > | 50000.0 | nM | - |