Assay Detail
Functional
CHEMBL5041573
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Agonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assay
15
Total Activities
15
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
Size-Reduced Macrocyclic Analogues of [Pyr<sup>1</sup>]-apelin-13 Showing Negative Gα<sub>12</sub> Bias Still Produce Prolonged Cardiac Effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 15 | 7.30 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5085866 | — | — | 1 | 8.62 |
| CHEMBL5078149 | — | — | 1 | 8.18 |
| CHEMBL5094438 | — | — | 1 | 7.72 |
| CHEMBL4083079 | — | — | 1 | 7.66 |
| CHEMBL5091081 | — | — | 1 | 7.48 |
| CHEMBL5092962 | — | — | 1 | 7.39 |
| CHEMBL5079665 | — | — | 1 | 7.35 |
| CHEMBL5087847 | — | — | 1 | 7.31 |
| CHEMBL5080649 | — | — | 1 | 7.20 |
| CHEMBL5072626 | — | — | 1 | 6.86 |
| CHEMBL5074959 | — | — | 1 | 6.79 |
| CHEMBL5089609 | — | — | 1 | 6.73 |
| CHEMBL5082518 | — | — | 1 | 6.60 |
| CHEMBL5092604 | — | — | 1 | 6.36 |
| CHEMBL5091501 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5085866 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL5078149 | — | EC50 | = | 6.6 | nM | 8.18 |
| CHEMBL5094438 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4083079 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5091081 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5092962 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5079665 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5087847 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5080649 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5072626 | — | EC50 | = | 137.0 | nM | 6.86 |
| CHEMBL5074959 | — | EC50 | = | 161.0 | nM | 6.79 |
| CHEMBL5089609 | — | EC50 | = | 187.0 | nM | 6.73 |
| CHEMBL5082518 | — | EC50 | = | 249.0 | nM | 6.60 |
| CHEMBL5092604 | — | EC50 | = | 441.0 | nM | 6.36 |
| CHEMBL5091501 | — | EC50 | > | 10000.0 | nM | - |