Assay Detail
Binding
CHEMBL5041571
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition [125I]-[Nle75,Tyr77][Pyr1]-Ape13 binding to YFP-tagged human APJ E20A mutant expressed in HEK293 cell membranes incubated for 1 hr by scintillation counting method
4
Total Activities
4
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 |
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 |
|---|---|---|---|
| IC50 | 4 | 7.22 | 8.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5087847 | — | — | 1 | 8.27 |
| CHEMBL5079665 | — | — | 1 | 7.75 |
| CHEMBL5076304 | — | — | 1 | 7.01 |
| CHEMBL5091291 | — | — | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5087847 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL5079665 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5076304 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL5091291 | — | IC50 | = | 1382.0 | nM | 5.86 |