Assay Detail
Binding
CHEMBL3242425
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Displacement of [125I]-pE13F from human apelin receptor expressed in CHO cell membranes after 1 hr by gamma counting analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-activity relationship studies toward the discovery of selective apelin receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 6.38 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3234446 | — | — | 1 | 10.40 |
| CHEMBL3234454 | — | — | 1 | 7.05 |
| CHEMBL3234461 | — | — | 1 | 6.75 |
| CHEMBL3234462 | — | — | 1 | 6.57 |
| CHEMBL3234452 | — | — | 1 | 6.51 |
| CHEMBL3234453 | — | — | 1 | 6.40 |
| CHEMBL3234445 | — | — | 1 | 6.37 |
| CHEMBL3234458 | — | — | 1 | 6.35 |
| CHEMBL3350781 | — | — | 1 | 6.16 |
| CHEMBL3234464 | — | — | 1 | 6.07 |
| CHEMBL3350785 | — | — | 1 | 6.02 |
| CHEMBL3234457 | — | — | 1 | 6.01 |
| CHEMBL3234460 | — | — | 1 | 6.01 |
| CHEMBL3234459 | — | — | 1 | 5.92 |
| CHEMBL3234448 | — | — | 1 | 5.85 |
| CHEMBL3350783 | — | — | 1 | 5.82 |
| CHEMBL3350782 | — | — | 1 | 5.52 |
| CHEMBL3350784 | — | — | 1 | 5.05 |
| CHEMBL3234456 | — | — | 1 | - |
| CHEMBL3234455 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3234446 | — | Ki | = | 0.04 | nM | 10.40 |
| CHEMBL3234454 | — | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL3234461 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL3234462 | — | Ki | = | 270.0 | nM | 6.57 |
| CHEMBL3234452 | — | Ki | = | 310.0 | nM | 6.51 |
| CHEMBL3234453 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL3234445 | — | Ki | = | 430.0 | nM | 6.37 |
| CHEMBL3234458 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL3350781 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL3234464 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL3350785 | — | Ki | = | 960.0 | nM | 6.02 |
| CHEMBL3234457 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL3234460 | — | Ki | = | 980.0 | nM | 6.01 |
| CHEMBL3234459 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL3234448 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL3350783 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL3350782 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL3350784 | — | Ki | = | 9000.0 | nM | 5.05 |
| CHEMBL3234456 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL3234455 | — | Ki | > | 100000.0 | nM | - |