Assay Detail
Binding
CHEMBL4386415
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Displacement of [3H]PGE2 from human recombinant EP3 receptor expressed in HEK293 cell membranes after 120 mins by liquid scintillation counting method
6
Total Activities
6
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 | Autocuration |
Target
Prostaglandin E2 receptor EP3 subtype (CHEMBL3710) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Difluoromethylene at the γ-Lactam α-Position Improves 11-Deoxy-8-aza-PGE<sub>1</sub> Series EP<sub>4</sub> Receptor Binding and Activity: 11-Deoxy-10,10-difluoro-8-aza-PGE<sub>1</sub> Analog (KMN-159) as a Potent EP<sub>4</sub> Agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 6.74 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL548 | DINOPROSTONE | 4.0 | 1 | 8.66 |
| CHEMBL3918816 | — | — | 1 | 6.59 |
| CHEMBL3955128 | — | — | 1 | 6.46 |
| CHEMBL4558749 | — | — | 1 | 6.06 |
| CHEMBL42027 | — | — | 1 | 5.93 |
| CHEMBL292964 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL548 | DINOPROSTONE | Ki | = | 2.17 | nM | 8.66 |
| CHEMBL3918816 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL3955128 | — | Ki | = | 350.0 | nM | 6.46 |
| CHEMBL4558749 | — | Ki | = | 880.0 | nM | 6.06 |
| CHEMBL42027 | — | Ki | = | 1175.0 | nM | 5.93 |
| CHEMBL292964 | — | Ki | - | — | - |