Assay Detail
Functional
CHEMBL4386419
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human EP4 receptor expressed in HEK293T/17 cells assessed as increase in GalphaS-mediated CREB activation measured after 6 to 24 hrs by SEAP reporter gene-based chemiluminescence assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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
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 |
|---|---|---|---|
| EC50 | 6 | 10.33 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL292964 | — | — | 1 | 11.00 |
| CHEMBL548 | DINOPROSTONE | 4.0 | 1 | 10.70 |
| CHEMBL3955128 | — | — | 1 | 10.68 |
| CHEMBL42027 | — | — | 1 | 10.19 |
| CHEMBL3918816 | — | — | 1 | 10.06 |
| CHEMBL4558749 | — | — | 1 | 9.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL292964 | — | EC50 | = | 0.01 | nM | 11.00 |
| CHEMBL548 | DINOPROSTONE | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL3955128 | — | EC50 | = | 0.021 | nM | 10.68 |
| CHEMBL42027 | — | EC50 | = | 0.065 | nM | 10.19 |
| CHEMBL3918816 | — | EC50 | = | 0.088 | nM | 10.06 |
| CHEMBL4558749 | — | EC50 | = | 0.476 | nM | 9.32 |