Assay Detail
Binding
CHEMBL4808299
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I] [NIe75,Tyr77]Pyr-apelin-13 from YFP-tagged human APJ receptor expressed in HEK293 cells incubated for 1 hr by gamma counting analysis
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
Constraining the Side Chain of C-Terminal Amino Acids in Apelin-13 Greatly Increases Affinity, Modulates Signaling, and Improves the Pharmacokinetic Profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 9.14 | 10.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4878158 | — | — | 1 | 10.70 |
| CHEMBL4876632 | — | — | 1 | 10.40 |
| CHEMBL4867453 | — | — | 1 | 10.15 |
| CHEMBL4855178 | — | — | 1 | 10.10 |
| CHEMBL4876492 | — | — | 1 | 10.10 |
| CHEMBL4867913 | — | — | 1 | 10.10 |
| CHEMBL4858171 | — | — | 1 | 10.05 |
| CHEMBL4876350 | — | — | 1 | 9.92 |
| CHEMBL4879304 | — | — | 1 | 9.92 |
| CHEMBL4857085 | — | — | 1 | 9.80 |
| CHEMBL4878369 | — | — | 1 | 9.74 |
| CHEMBL4857851 | — | — | 1 | 9.72 |
| CHEMBL4859698 | — | — | 1 | 9.44 |
| CHEMBL4849012 | — | — | 1 | 9.43 |
| CHEMBL4862772 | — | — | 1 | 9.40 |
| CHEMBL4863977 | — | — | 1 | 9.39 |
| CHEMBL4869716 | — | — | 1 | 9.34 |
| CHEMBL414173 | — | — | 1 | 9.15 |
| CHEMBL4865796 | — | — | 1 | 9.00 |
| CHEMBL4876128 | — | — | 1 | 9.00 |
| CHEMBL4876569 | — | — | 1 | 8.96 |
| CHEMBL4858007 | — | — | 1 | 8.96 |
| CHEMBL4861483 | — | — | 1 | 8.80 |
| CHEMBL4855339 | — | — | 1 | 8.77 |
| CHEMBL4845895 | — | — | 1 | 8.68 |
| CHEMBL4870831 | — | — | 1 | 8.55 |
| CHEMBL4863381 | — | — | 1 | 8.38 |
| CHEMBL4870656 | — | — | 1 | 8.37 |
| CHEMBL4871150 | — | — | 1 | 8.21 |
| CHEMBL4856918 | — | — | 1 | 8.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4878158 | — | Ki | = | 0.02 | nM | 10.70 |
| CHEMBL4876632 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL4867453 | — | Ki | = | 0.07 | nM | 10.15 |
| CHEMBL4855178 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL4876492 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL4867913 | — | Ki | = | 0.08 | nM | 10.10 |
| CHEMBL4858171 | — | Ki | = | 0.09 | nM | 10.05 |
| CHEMBL4876350 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL4879304 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL4857085 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL4878369 | — | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL4857851 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL4859698 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL4849012 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL4862772 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL4863977 | — | Ki | = | 0.41 | nM | 9.39 |
| CHEMBL4869716 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL414173 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL4865796 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL4876128 | — | Ki | = | 1.01 | nM | 9.00 |
| CHEMBL4876569 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4858007 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL4861483 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL4855339 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL4845895 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL4870831 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL4863381 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL4870656 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL4871150 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL4856918 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL4854245 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4879061 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL4860998 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL4857723 | — | Ki | = | 37.0 | nM | 7.43 |