Assay Detail
Functional
CHEMBL5098801
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Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of a Hydroxypyrimidinone Compound (<b>21</b>) as a Potent APJ Receptor Agonist for the Potential Treatment of Heart Failure.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 10.00 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5193130 | — | — | 1 | 10.70 |
| CHEMBL5173464 | — | — | 1 | 10.70 |
| CHEMBL5208127 | — | — | 1 | 10.70 |
| CHEMBL5192130 | — | — | 1 | 10.70 |
| CHEMBL5205562 | — | — | 1 | 10.70 |
| CHEMBL5202635 | — | — | 1 | 10.70 |
| CHEMBL5175424 | — | — | 1 | 10.52 |
| CHEMBL5202233 | — | — | 1 | 10.52 |
| CHEMBL5197398 | — | — | 1 | 10.40 |
| CHEMBL414173 | — | — | 1 | 10.30 |
| CHEMBL5170657 | — | — | 1 | 10.22 |
| CHEMBL5179504 | — | — | 1 | 10.15 |
| CHEMBL5199079 | — | — | 1 | 9.70 |
| CHEMBL5184730 | — | — | 1 | 9.70 |
| CHEMBL5185709 | — | — | 1 | 9.40 |
| CHEMBL4870497 | — | — | 1 | 9.40 |
| CHEMBL5206677 | — | — | 1 | 9.22 |
| CHEMBL5190307 | — | — | 1 | 8.74 |
| CHEMBL5197115 | — | — | 1 | 8.72 |
| CHEMBL5190259 | — | — | 1 | 8.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5193130 | — | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5173464 | — | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5208127 | — | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5192130 | — | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5205562 | — | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5202635 | — | EC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5175424 | — | EC50 | = | 0.03 | nM | 10.52 |
| CHEMBL5202233 | — | EC50 | = | 0.03 | nM | 10.52 |
| CHEMBL5197398 | — | EC50 | = | 0.04 | nM | 10.40 |
| CHEMBL414173 | — | EC50 | = | 0.05 | nM | 10.30 |
| CHEMBL5170657 | — | EC50 | = | 0.06 | nM | 10.22 |
| CHEMBL5179504 | — | EC50 | = | 0.07 | nM | 10.15 |
| CHEMBL5199079 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5184730 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL5185709 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4870497 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5206677 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5190307 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5197115 | — | EC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5190259 | — | EC50 | = | 1.9 | nM | 8.72 |