Assay Detail
Binding
CHEMBL3421345
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Displacement of [125I]apelin-13[Glp65,Nle75,Tyr77] from YFP epitope-tagged human APJ receptor expressed in HEK293 cell membranes incubated for 1 hr by Cheng-Prusoff equation analysis
24
Total Activities
24
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
C-Terminal modifications of apelin-13 significantly change ligand binding, receptor signaling, and hypotensive action.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 24 | 8.75 | 10.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3417384 | — | — | 1 | 10.80 |
| CHEMBL3417378 | — | — | 1 | 9.70 |
| CHEMBL3417389 | — | — | 1 | 9.47 |
| CHEMBL3417385 | — | — | 1 | 9.42 |
| CHEMBL3417377 | — | — | 1 | 9.32 |
| CHEMBL3417390 | — | — | 1 | 9.16 |
| CHEMBL3417379 | — | — | 1 | 9.00 |
| CHEMBL3184840 | — | — | 1 | 9.00 |
| CHEMBL3417386 | — | — | 1 | 8.92 |
| CHEMBL3417380 | — | — | 1 | 8.89 |
| CHEMBL3414601 | — | — | 1 | 8.85 |
| CHEMBL3417291 | — | — | 1 | 8.68 |
| CHEMBL3417388 | — | — | 1 | 8.66 |
| CHEMBL3417381 | — | — | 1 | 8.31 |
| CHEMBL3417383 | — | — | 1 | 8.27 |
| CHEMBL3417375 | — | — | 1 | 8.20 |
| CHEMBL3414600 | — | — | 1 | 8.04 |
| CHEMBL3417387 | — | — | 1 | 7.96 |
| CHEMBL3417382 | — | — | 1 | 7.94 |
| CHEMBL3417376 | — | — | 1 | 7.84 |
| CHEMBL3417391 | — | — | 1 | 7.34 |
| CHEMBL3417392 | — | — | 1 | - |
| CHEMBL3417393 | — | — | 1 | - |
| CHEMBL3417394 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3417384 | — | Ki | = | 0.016 | nM | 10.80 |
| CHEMBL3417378 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL3417389 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL3417385 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL3417377 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL3417390 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL3417379 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3184840 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL3417386 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL3417380 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL3414601 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL3417291 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3417388 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL3417381 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL3417383 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL3417375 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL3414600 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL3417387 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3417382 | — | Ki | = | 11.4 | nM | 7.94 |
| CHEMBL3417376 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL3417391 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL3417392 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3417393 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL3417394 | — | Ki | > | 10000.0 | nM | - |