Assay Detail
Functional
CHEMBL4808300
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 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 | 8.40 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4878158 | — | — | 1 | 9.30 |
| CHEMBL4857723 | — | — | 1 | 9.00 |
| CHEMBL4867453 | — | — | 1 | 9.00 |
| CHEMBL414173 | — | — | 1 | 8.96 |
| CHEMBL4879061 | — | — | 1 | 8.85 |
| CHEMBL4876632 | — | — | 1 | 8.82 |
| CHEMBL4858171 | — | — | 1 | 8.80 |
| CHEMBL4860998 | — | — | 1 | 8.68 |
| CHEMBL4859698 | — | — | 1 | 8.62 |
| CHEMBL4858007 | — | — | 1 | 8.60 |
| CHEMBL4867913 | — | — | 1 | 8.60 |
| CHEMBL4871150 | — | — | 1 | 8.57 |
| CHEMBL4857851 | — | — | 1 | 8.47 |
| CHEMBL4878369 | — | — | 1 | 8.42 |
| CHEMBL4855178 | — | — | 1 | 8.42 |
| CHEMBL4869716 | — | — | 1 | 8.42 |
| CHEMBL4857085 | — | — | 1 | 8.39 |
| CHEMBL4876492 | — | — | 1 | 8.38 |
| CHEMBL4862772 | — | — | 1 | 8.37 |
| CHEMBL4849012 | — | — | 1 | 8.37 |
| CHEMBL4876350 | — | — | 1 | 8.36 |
| CHEMBL4845895 | — | — | 1 | 8.25 |
| CHEMBL4863977 | — | — | 1 | 8.24 |
| CHEMBL4876128 | — | — | 1 | 8.22 |
| CHEMBL4865796 | — | — | 1 | 8.19 |
| CHEMBL4855339 | — | — | 1 | 8.19 |
| CHEMBL4870656 | — | — | 1 | 8.17 |
| CHEMBL4870831 | — | — | 1 | 8.07 |
| CHEMBL4856918 | — | — | 1 | 8.02 |
| CHEMBL4876569 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4878158 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4857723 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4867453 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL414173 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4879061 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL4876632 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4858171 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4860998 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4859698 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4858007 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4867913 | — | EC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4871150 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4857851 | — | EC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4869716 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4855178 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4878369 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4857085 | — | EC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4876492 | — | EC50 | = | 4.2 | nM | 8.38 |
| CHEMBL4862772 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4849012 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL4876350 | — | EC50 | = | 4.4 | nM | 8.36 |
| CHEMBL4845895 | — | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL4863977 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL4876128 | — | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4865796 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4855339 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4870656 | — | EC50 | = | 6.8 | nM | 8.17 |
| CHEMBL4870831 | — | EC50 | = | 8.6 | nM | 8.07 |
| CHEMBL4856918 | — | EC50 | = | 9.6 | nM | 8.02 |
| CHEMBL4876569 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4861483 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4863381 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4879304 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4854245 | — | EC50 | = | 22.0 | nM | 7.66 |