Assay Detail
Binding
CHEMBL5041569
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]-[Nle75,Tyr77][Pyr1]-Ape13 from YFP-tagged human APJ expressed in HEK293 cell membranes assessed as inhibition constant incubated for 1 hr by scintillation counting method
33
Total Activities
33
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
Size-Reduced Macrocyclic Analogues of [Pyr<sup>1</sup>]-apelin-13 Showing Negative Gα<sub>12</sub> Bias Still Produce Prolonged Cardiac Effects.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 33 | 7.72 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5094438 | — | — | 1 | 9.70 |
| CHEMBL5091501 | — | — | 1 | 9.22 |
| CHEMBL5087847 | — | — | 1 | 9.22 |
| CHEMBL5078149 | — | — | 1 | 9.05 |
| CHEMBL5092962 | — | — | 1 | 8.77 |
| CHEMBL5091081 | — | — | 1 | 8.77 |
| CHEMBL5072626 | — | — | 1 | 8.60 |
| CHEMBL4083079 | — | — | 1 | 8.52 |
| CHEMBL5080649 | — | — | 1 | 8.37 |
| CHEMBL5079665 | — | — | 1 | 8.34 |
| CHEMBL5074959 | — | — | 1 | 8.28 |
| CHEMBL5085866 | — | — | 1 | 8.24 |
| CHEMBL5092604 | — | — | 1 | 8.07 |
| CHEMBL5082518 | — | — | 1 | 7.85 |
| CHEMBL5089609 | — | — | 1 | 7.80 |
| CHEMBL5079005 | — | — | 1 | 7.55 |
| CHEMBL5093180 | — | — | 1 | 7.48 |
| CHEMBL5093858 | — | — | 1 | 7.41 |
| CHEMBL5076304 | — | — | 1 | 7.21 |
| CHEMBL5090040 | — | — | 1 | 7.07 |
| CHEMBL5074666 | — | — | 1 | 7.07 |
| CHEMBL5088099 | — | — | 1 | 6.96 |
| CHEMBL5082011 | — | — | 1 | 6.84 |
| CHEMBL5091385 | — | — | 1 | 6.77 |
| CHEMBL5070767 | — | — | 1 | 6.70 |
| CHEMBL5091291 | — | — | 1 | 6.46 |
| CHEMBL5079790 | — | — | 1 | 6.40 |
| CHEMBL5081025 | — | — | 1 | 5.69 |
| CHEMBL5079641 | — | — | 1 | 5.57 |
| CHEMBL5075292 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5094438 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL5091501 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL5087847 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL5078149 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL5092962 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL5091081 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL5072626 | — | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL4083079 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL5080649 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL5079665 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL5074959 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL5085866 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL5092604 | — | Ki | = | 8.6 | nM | 8.07 |
| CHEMBL5082518 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5089609 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL5079005 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL5093180 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL5093858 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL5076304 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL5090040 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL5074666 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL5088099 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL5082011 | — | Ki | = | 143.0 | nM | 6.84 |
| CHEMBL5091385 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL5070767 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL5091291 | — | Ki | = | 343.0 | nM | 6.46 |
| CHEMBL5079790 | — | Ki | = | 396.0 | nM | 6.40 |
| CHEMBL5081025 | — | Ki | = | 2044.0 | nM | 5.69 |
| CHEMBL5079641 | — | Ki | = | 2670.0 | nM | 5.57 |
| CHEMBL5075292 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5077256 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5094794 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5075513 | — | Ki | > | 10000.0 | nM | - |