Assay Detail
Binding
CHEMBL4401047
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Displacement of [125I]-(Glp1,Nle11,Try14)apelin-13 from recombinant rat EGFP-fused apelin receptor expressed in CHO cell membrane measured after 3 hrs
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Plasma kallikrein cleaves and inactivates apelin-17: Palmitoyl- and PEG-extended apelin-17 analogs as metabolically stable blood pressure-lowering agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 8 | - | - |
| IC50 | 1 | 10.60 | 10.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3234446 | — | — | 1 | 10.60 |
| CHEMBL4439951 | — | — | 1 | - |
| CHEMBL4559795 | — | — | 1 | - |
| CHEMBL4065973 | — | — | 1 | - |
| CHEMBL4098390 | — | — | 1 | - |
| CHEMBL4472749 | — | — | 1 | - |
| CHEMBL4440817 | — | — | 1 | - |
| CHEMBL4464954 | — | — | 1 | - |
| CHEMBL4550078 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3234446 | — | IC50 | = | 0.025 | nM | 10.60 |
| CHEMBL4439951 | — | Inhibition | - | % | - | |
| CHEMBL4559795 | — | Inhibition | - | % | - | |
| CHEMBL4065973 | — | Inhibition | - | % | - | |
| CHEMBL4098390 | — | Inhibition | - | % | - | |
| CHEMBL4472749 | — | Inhibition | - | % | - | |
| CHEMBL4440817 | — | Inhibition | - | % | - | |
| CHEMBL4464954 | — | Inhibition | - | % | - | |
| CHEMBL4550078 | — | Inhibition | - | % | - |