Assay Detail
Functional
CHEMBL4808302
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| EC50 | 34 | 7.13 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4867453 | — | — | 1 | 8.00 |
| CHEMBL4878158 | — | — | 1 | 7.85 |
| CHEMBL4876632 | — | — | 1 | 7.72 |
| CHEMBL4867913 | — | — | 1 | 7.60 |
| CHEMBL4871150 | — | — | 1 | 7.52 |
| CHEMBL4858171 | — | — | 1 | 7.50 |
| CHEMBL4876492 | — | — | 1 | 7.48 |
| CHEMBL4857085 | — | — | 1 | 7.47 |
| CHEMBL4855178 | — | — | 1 | 7.44 |
| CHEMBL4878369 | — | — | 1 | 7.42 |
| CHEMBL4857723 | — | — | 1 | 7.40 |
| CHEMBL414173 | — | — | 1 | 7.40 |
| CHEMBL4876350 | — | — | 1 | 7.39 |
| CHEMBL4862772 | — | — | 1 | 7.36 |
| CHEMBL4857851 | — | — | 1 | 7.35 |
| CHEMBL4879061 | — | — | 1 | 7.33 |
| CHEMBL4860998 | — | — | 1 | 7.19 |
| CHEMBL4858007 | — | — | 1 | 7.17 |
| CHEMBL4863977 | — | — | 1 | 7.16 |
| CHEMBL4859698 | — | — | 1 | 7.16 |
| CHEMBL4849012 | — | — | 1 | 7.03 |
| CHEMBL4876128 | — | — | 1 | 7.02 |
| CHEMBL4876569 | — | — | 1 | 7.02 |
| CHEMBL4845895 | — | — | 1 | 7.00 |
| CHEMBL4869716 | — | — | 1 | 6.97 |
| CHEMBL4856918 | — | — | 1 | 6.85 |
| CHEMBL4865796 | — | — | 1 | 6.72 |
| CHEMBL4855339 | — | — | 1 | 6.66 |
| CHEMBL4870656 | — | — | 1 | 6.51 |
| CHEMBL4861483 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4867453 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4878158 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4876632 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4867913 | — | EC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4871150 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4858171 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4876492 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4857085 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4855178 | — | EC50 | = | 36.0 | nM | 7.44 |
| CHEMBL4878369 | — | EC50 | = | 38.0 | nM | 7.42 |
| CHEMBL4857723 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL414173 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4876350 | — | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4862772 | — | EC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4857851 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4879061 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL4860998 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL4858007 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL4863977 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4859698 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4849012 | — | EC50 | = | 94.0 | nM | 7.03 |
| CHEMBL4876128 | — | EC50 | = | 96.0 | nM | 7.02 |
| CHEMBL4876569 | — | EC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4845895 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4869716 | — | EC50 | = | 106.0 | nM | 6.97 |
| CHEMBL4856918 | — | EC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4865796 | — | EC50 | = | 192.0 | nM | 6.72 |
| CHEMBL4855339 | — | EC50 | = | 221.0 | nM | 6.66 |
| CHEMBL4870656 | — | EC50 | = | 311.0 | nM | 6.51 |
| CHEMBL4861483 | — | EC50 | = | 361.0 | nM | 6.44 |
| CHEMBL4854245 | — | EC50 | = | 367.0 | nM | 6.43 |
| CHEMBL4870831 | — | EC50 | = | 391.0 | nM | 6.41 |
| CHEMBL4863381 | — | EC50 | = | 454.0 | nM | 6.34 |
| CHEMBL4879304 | — | EC50 | = | 571.0 | nM | 6.24 |