Assay Detail
Binding
CHEMBL4040233
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-pyr-1-apelin-13 from rat C-terminal EGFP-tagged APJ receptor expressed in CHO cell membranes after 3 hrs by Wallac gamma counting
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthetic Modification within the "RPRL" Region of Apelin Peptides: Impact on Cardiovascular Activity and Stability to Neprilysin and Plasma Degradation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 9.66 | 10.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3234446 | — | — | 1 | 10.28 |
| CHEMBL4059998 | — | — | 1 | 10.00 |
| CHEMBL4075830 | — | — | 1 | 9.92 |
| CHEMBL4077740 | — | — | 1 | 9.89 |
| CHEMBL4069459 | — | — | 1 | 9.89 |
| CHEMBL4076754 | — | — | 1 | 9.85 |
| CHEMBL4059541 | — | — | 1 | 9.85 |
| CHEMBL4076953 | — | — | 1 | 9.82 |
| CHEMBL4103607 | — | — | 1 | 9.77 |
| CHEMBL4061039 | — | — | 1 | 9.74 |
| CHEMBL4098390 | — | — | 1 | 9.72 |
| CHEMBL3184840 | — | — | 1 | 9.52 |
| CHEMBL4065973 | — | — | 1 | 9.35 |
| CHEMBL4075655 | — | — | 1 | 9.25 |
| CHEMBL4085677 | — | — | 1 | 9.00 |
| CHEMBL4077505 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3234446 | — | Ki | = | 0.053 | nM | 10.28 |
| CHEMBL4059998 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4075830 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL4077740 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL4069459 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL4076754 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL4059541 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL4076953 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL4103607 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL4061039 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL4098390 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL3184840 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL4065973 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL4075655 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL4085677 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4077505 | — | Ki | = | 2.0 | nM | 8.70 |