Assay Detail
Binding
CHEMBL4775348
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Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Galpha(i1)-RlucII(91) assessed as induction of dissociation of Galpha(i1) from G-beta-gamma subunits incubated for 5 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 | 8.29 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4791583 | — | — | 1 | 8.96 |
| CHEMBL3184840 | — | — | 1 | 8.96 |
| CHEMBL4797921 | — | — | 1 | 8.92 |
| CHEMBL4777690 | — | — | 1 | 8.64 |
| CHEMBL4789289 | — | — | 1 | 8.62 |
| CHEMBL4790636 | — | — | 1 | 8.55 |
| CHEMBL4781348 | — | — | 1 | 8.42 |
| CHEMBL4791473 | — | — | 1 | 8.40 |
| CHEMBL4793361 | — | — | 1 | 8.35 |
| CHEMBL4788480 | — | — | 1 | 8.34 |
| CHEMBL4795339 | — | — | 1 | 8.29 |
| CHEMBL4796315 | — | — | 1 | 8.28 |
| CHEMBL4791398 | — | — | 1 | 8.24 |
| CHEMBL4787249 | — | — | 1 | 8.24 |
| CHEMBL4792840 | — | — | 1 | 8.19 |
| CHEMBL4797169 | — | — | 1 | 8.16 |
| CHEMBL4785339 | — | — | 1 | 8.15 |
| CHEMBL4788436 | — | — | 1 | 8.10 |
| CHEMBL4779171 | — | — | 1 | 7.96 |
| CHEMBL4795334 | — | — | 1 | 7.85 |
| CHEMBL4794333 | — | — | 1 | 7.77 |
| CHEMBL4780010 | — | — | 1 | 7.72 |
| CHEMBL4778604 | — | — | 1 | 7.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4791583 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3184840 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL4797921 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL4777690 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4789289 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4790636 | — | EC50 | = | 2.8 | nM | 8.55 |
| CHEMBL4781348 | — | EC50 | = | 3.8 | nM | 8.42 |
| CHEMBL4791473 | — | EC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4793361 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL4788480 | — | EC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4795339 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4796315 | — | EC50 | = | 5.3 | nM | 8.28 |
| CHEMBL4791398 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4787249 | — | EC50 | = | 5.8 | nM | 8.24 |
| CHEMBL4792840 | — | EC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4797169 | — | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL4785339 | — | EC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4788436 | — | EC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4779171 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4795334 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4794333 | — | EC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4780010 | — | EC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4778604 | — | EC50 | = | 23.0 | nM | 7.64 |