Assay Detail
Binding
CHEMBL5233309
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Displacement of [125I]-pyr-1-apelin-13 from EGFP tagged rat apelin receptor expressed in CHO cell membrane incubated for 3 hrs by gamma counter analysis
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Metabolically stable apelin-analogues, incorporating cyclohexylalanine and homoarginine, as potent apelin receptor activators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 9.17 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4059998 | — | — | 1 | 10.00 |
| CHEMBL4098390 | — | — | 1 | 9.72 |
| CHEMBL5282440 | — | — | 1 | 9.43 |
| CHEMBL4065973 | — | — | 1 | 9.35 |
| CHEMBL5283358 | — | — | 1 | 9.24 |
| CHEMBL5278343 | — | — | 1 | 9.19 |
| CHEMBL5265964 | — | — | 1 | 9.17 |
| CHEMBL5273372 | — | — | 1 | 9.08 |
| CHEMBL5276383 | — | — | 1 | 8.96 |
| CHEMBL5278191 | — | — | 1 | 8.85 |
| CHEMBL5269447 | — | — | 1 | 8.80 |
| CHEMBL4077505 | — | — | 1 | 8.70 |
| CHEMBL5286901 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4059998 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4098390 | — | Ki | = | 0.1905 | nM | 9.72 |
| CHEMBL5282440 | — | Ki | = | 0.3715 | nM | 9.43 |
| CHEMBL4065973 | — | Ki | = | 0.4467 | nM | 9.35 |
| CHEMBL5283358 | — | Ki | = | 0.5754 | nM | 9.24 |
| CHEMBL5278343 | — | Ki | = | 0.6457 | nM | 9.19 |
| CHEMBL5265964 | — | Ki | = | 0.6761 | nM | 9.17 |
| CHEMBL5273372 | — | Ki | = | 0.8318 | nM | 9.08 |
| CHEMBL5276383 | — | Ki | = | 1.096 | nM | 8.96 |
| CHEMBL5278191 | — | Ki | = | 1.413 | nM | 8.85 |
| CHEMBL5269447 | — | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL4077505 | — | Ki | = | 1.995 | nM | 8.70 |
| CHEMBL5286901 | — | Ki | = | 1.995 | nM | 8.70 |