Assay Detail
Binding
CHEMBL948330
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Displacement of [125I]Angiotensin 4 from human recombinant IRAP expressed in CHOK1 cells
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Ligands to the (IRAP)/AT4 receptor encompassing a 4-hydroxydiphenylmethane scaffold replacing Tyr2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.47 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL261120 | ANGIOTENSIN IV | — | 1 | 8.15 |
| CHEMBL355434 | — | — | 1 | 6.00 |
| CHEMBL448920 | — | — | 1 | 5.85 |
| CHEMBL499779 | — | — | 1 | 5.64 |
| CHEMBL501693 | — | — | 1 | 5.60 |
| CHEMBL450452 | — | — | 1 | 5.51 |
| CHEMBL469483 | — | — | 1 | 5.41 |
| CHEMBL504736 | — | — | 1 | 5.17 |
| CHEMBL448184 | — | — | 1 | 5.05 |
| CHEMBL499984 | — | — | 1 | 4.92 |
| CHEMBL501326 | — | — | 1 | 4.89 |
| CHEMBL447726 | — | — | 1 | 4.85 |
| CHEMBL470072 | — | — | 1 | 4.07 |
| CHEMBL487435 | — | — | 1 | - |
| CHEMBL488627 | — | — | 1 | - |
| CHEMBL469484 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL261120 | ANGIOTENSIN IV | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL355434 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL448920 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL499779 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL501693 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL450452 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL469483 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL504736 | — | Ki | = | 6800.0 | nM | 5.17 |
| CHEMBL448184 | — | Ki | = | 8900.0 | nM | 5.05 |
| CHEMBL499984 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL501326 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL447726 | — | Ki | = | 14000.0 | nM | 4.85 |
| CHEMBL470072 | — | Ki | = | 86000.0 | nM | 4.07 |
| CHEMBL487435 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL488627 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL469484 | — | Ki | > | 100000.0 | nM | - |