Assay Detail
Binding
CHEMBL4023903
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-[Nle75, Tyr77] Pyr1-apelin-13 from YFP-tagged human APJ receptor expressed in HEK293 cell membranes after 1 hr by gamma-counting method
34
Total Activities
34
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 |
|---|---|---|---|
| Ki | 34 | 7.85 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4076049 | — | — | 1 | 10.00 |
| CHEMBL4094033 | — | — | 1 | 9.82 |
| CHEMBL4076652 | — | — | 1 | 9.52 |
| CHEMBL3184840 | — | — | 1 | 9.15 |
| CHEMBL3417291 | — | — | 1 | 9.10 |
| CHEMBL4076755 | — | — | 1 | 8.96 |
| CHEMBL4078407 | — | — | 1 | 8.85 |
| CHEMBL4072080 | — | — | 1 | 8.72 |
| CHEMBL4093319 | — | — | 1 | 8.68 |
| CHEMBL4072606 | — | — | 1 | 8.64 |
| CHEMBL4077162 | — | — | 1 | 8.60 |
| CHEMBL4075302 | — | — | 1 | 8.57 |
| CHEMBL4083756 | — | — | 1 | 8.54 |
| CHEMBL4083079 | — | — | 1 | 8.52 |
| CHEMBL4104256 | — | — | 1 | 8.41 |
| CHEMBL4100822 | — | — | 1 | 8.35 |
| CHEMBL4076140 | — | — | 1 | 8.24 |
| CHEMBL4101053 | — | — | 1 | 8.04 |
| CHEMBL4087671 | — | — | 1 | 7.85 |
| CHEMBL4080763 | — | — | 1 | 7.39 |
| CHEMBL4093831 | — | — | 1 | 7.39 |
| CHEMBL4067504 | — | — | 1 | 6.73 |
| CHEMBL4063462 | — | — | 1 | 6.71 |
| CHEMBL4075293 | — | — | 1 | 6.69 |
| CHEMBL4094924 | — | — | 1 | 6.57 |
| CHEMBL4075988 | — | — | 1 | 6.51 |
| CHEMBL4075835 | — | — | 1 | 6.35 |
| CHEMBL4075499 | — | — | 1 | 6.31 |
| CHEMBL4075634 | — | — | 1 | 6.29 |
| CHEMBL4067669 | — | — | 1 | 6.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4076049 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL4094033 | — | Ki | = | 0.15 | nM | 9.82 |
| CHEMBL4076652 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL3184840 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL3417291 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL4076755 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4078407 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL4072080 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL4093319 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4072606 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL4077162 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL4075302 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL4083756 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL4083079 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL4104256 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL4100822 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL4076140 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL4101053 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL4087671 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4080763 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL4093831 | — | Ki | = | 41.0 | nM | 7.39 |
| CHEMBL4067504 | — | Ki | = | 188.0 | nM | 6.73 |
| CHEMBL4063462 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL4075293 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL4094924 | — | Ki | = | 268.0 | nM | 6.57 |
| CHEMBL4075988 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL4075835 | — | Ki | = | 445.0 | nM | 6.35 |
| CHEMBL4075499 | — | Ki | = | 489.0 | nM | 6.31 |
| CHEMBL4075634 | — | Ki | = | 509.0 | nM | 6.29 |
| CHEMBL4067669 | — | Ki | = | 523.0 | nM | 6.28 |
| CHEMBL4073382 | — | Ki | = | 917.0 | nM | 6.04 |
| CHEMBL4071989 | — | Ki | = | 6074.0 | nM | 5.22 |
| CHEMBL4075607 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4104774 | — | Ki | > | 10000.0 | nM | - |