Assay Detail
Binding
CHEMBL4775351
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Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to APJ incubated for 30 mins by BRET assay
23
Total Activities
23
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
Structure-Activity Relationship and Bioactivity of Short Analogues of ELABELA as Agonists of the Apelin Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 6.73 | 7.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4796315 | — | — | 1 | 7.35 |
| CHEMBL4777690 | — | — | 1 | 7.28 |
| CHEMBL3184840 | — | — | 1 | 7.22 |
| CHEMBL4797921 | — | — | 1 | 7.10 |
| CHEMBL4791583 | — | — | 1 | 7.06 |
| CHEMBL4781348 | — | — | 1 | 6.97 |
| CHEMBL4790636 | — | — | 1 | 6.92 |
| CHEMBL4793361 | — | — | 1 | 6.91 |
| CHEMBL4788480 | — | — | 1 | 6.83 |
| CHEMBL4791473 | — | — | 1 | 6.82 |
| CHEMBL4785339 | — | — | 1 | 6.81 |
| CHEMBL4791398 | — | — | 1 | 6.76 |
| CHEMBL4797169 | — | — | 1 | 6.76 |
| CHEMBL4795339 | — | — | 1 | 6.74 |
| CHEMBL4792840 | — | — | 1 | 6.72 |
| CHEMBL4788436 | — | — | 1 | 6.51 |
| CHEMBL4787249 | — | — | 1 | 6.43 |
| CHEMBL4780010 | — | — | 1 | 6.42 |
| CHEMBL4789289 | — | — | 1 | 6.40 |
| CHEMBL4778604 | — | — | 1 | 6.27 |
| CHEMBL4795334 | — | — | 1 | 6.27 |
| CHEMBL4779171 | — | — | 1 | 6.24 |
| CHEMBL4794333 | — | — | 1 | 6.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4796315 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4777690 | — | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL3184840 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4797921 | — | EC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4791583 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL4781348 | — | EC50 | = | 107.0 | nM | 6.97 |
| CHEMBL4790636 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4793361 | — | EC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4788480 | — | EC50 | = | 149.0 | nM | 6.83 |
| CHEMBL4791473 | — | EC50 | = | 151.0 | nM | 6.82 |
| CHEMBL4785339 | — | EC50 | = | 155.0 | nM | 6.81 |
| CHEMBL4791398 | — | EC50 | = | 175.0 | nM | 6.76 |
| CHEMBL4797169 | — | EC50 | = | 172.0 | nM | 6.76 |
| CHEMBL4795339 | — | EC50 | = | 182.0 | nM | 6.74 |
| CHEMBL4792840 | — | EC50 | = | 189.0 | nM | 6.72 |
| CHEMBL4788436 | — | EC50 | = | 309.0 | nM | 6.51 |
| CHEMBL4787249 | — | EC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4780010 | — | EC50 | = | 381.0 | nM | 6.42 |
| CHEMBL4789289 | — | EC50 | = | 401.0 | nM | 6.40 |
| CHEMBL4778604 | — | EC50 | = | 537.0 | nM | 6.27 |
| CHEMBL4795334 | — | EC50 | = | 533.0 | nM | 6.27 |
| CHEMBL4779171 | — | EC50 | = | 581.0 | nM | 6.24 |
| CHEMBL4794333 | — | EC50 | = | 940.0 | nM | 6.03 |