Assay Detail
Binding
CHEMBL4023904
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Activity at human APJ receptor expressed in HEK293 cells assessed as dissociation of Galphai1 from Gbetagamma subunit after 5 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 | 8.40 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4077162 | — | — | 1 | 9.40 |
| CHEMBL4072606 | — | — | 1 | 9.10 |
| CHEMBL4076652 | — | — | 1 | 9.00 |
| CHEMBL3184840 | — | — | 1 | 8.96 |
| CHEMBL4094033 | — | — | 1 | 8.89 |
| CHEMBL4076049 | — | — | 1 | 8.77 |
| CHEMBL4093319 | — | — | 1 | 8.70 |
| CHEMBL4075302 | — | — | 1 | 8.68 |
| CHEMBL4083079 | — | — | 1 | 8.43 |
| CHEMBL4083756 | — | — | 1 | 8.24 |
| CHEMBL4100822 | — | — | 1 | 8.22 |
| CHEMBL4072080 | — | — | 1 | 8.04 |
| CHEMBL4101053 | — | — | 1 | 7.72 |
| CHEMBL4076755 | — | — | 1 | 7.72 |
| CHEMBL4078407 | — | — | 1 | 7.70 |
| CHEMBL4076140 | — | — | 1 | 7.64 |
| CHEMBL4087671 | — | — | 1 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4077162 | — | EC50 | = | 0.4 | nM | 9.40 |
| CHEMBL4072606 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4076652 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3184840 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4094033 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4076049 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4093319 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4075302 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4083079 | — | EC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4083756 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4100822 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4072080 | — | EC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4101053 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4076755 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4078407 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4076140 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4087671 | — | EC50 | = | 30.0 | nM | 7.52 |