Assay Detail
Binding
CHEMBL4023905
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at GFP10-tagged human APJ receptor expressed in HEK293 cells assessed as induction of RlucII-tagged beta-arrestin-2 recruitment after 30 mins by BRET assay
17
Total Activities
17
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
A Systematic Exploration of Macrocyclization in Apelin-13: Impact on Binding, Signaling, Stability, and Cardiovascular Effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 17 | 6.82 | 7.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4077162 | — | — | 1 | 7.46 |
| CHEMBL4076652 | — | — | 1 | 7.38 |
| CHEMBL4094033 | — | — | 1 | 7.24 |
| CHEMBL4072606 | — | — | 1 | 7.24 |
| CHEMBL3184840 | — | — | 1 | 7.22 |
| CHEMBL4076049 | — | — | 1 | 7.20 |
| CHEMBL4075302 | — | — | 1 | 7.04 |
| CHEMBL4083079 | — | — | 1 | 6.90 |
| CHEMBL4093319 | — | — | 1 | 6.84 |
| CHEMBL4100822 | — | — | 1 | 6.75 |
| CHEMBL4083756 | — | — | 1 | 6.63 |
| CHEMBL4076755 | — | — | 1 | 6.57 |
| CHEMBL4072080 | — | — | 1 | 6.56 |
| CHEMBL4078407 | — | — | 1 | 6.40 |
| CHEMBL4101053 | — | — | 1 | 6.29 |
| CHEMBL4087671 | — | — | 1 | 6.08 |
| CHEMBL4076140 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4077162 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4076652 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4094033 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4072606 | — | EC50 | = | 58.0 | nM | 7.24 |
| CHEMBL3184840 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4076049 | — | EC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4075302 | — | EC50 | = | 91.0 | nM | 7.04 |
| CHEMBL4083079 | — | EC50 | = | 126.0 | nM | 6.90 |
| CHEMBL4093319 | — | EC50 | = | 145.0 | nM | 6.84 |
| CHEMBL4100822 | — | EC50 | = | 179.0 | nM | 6.75 |
| CHEMBL4083756 | — | EC50 | = | 232.0 | nM | 6.63 |
| CHEMBL4076755 | — | EC50 | = | 272.0 | nM | 6.57 |
| CHEMBL4072080 | — | EC50 | = | 274.0 | nM | 6.56 |
| CHEMBL4078407 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4101053 | — | EC50 | = | 512.0 | nM | 6.29 |
| CHEMBL4087671 | — | EC50 | = | 825.0 | nM | 6.08 |
| CHEMBL4076140 | — | EC50 | = | 857.0 | nM | 6.07 |