Assay Detail
Binding
CHEMBL948331
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Inhibition of human recombinant IRAP expressed in HEK293 cells
16
Total Activities
16
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
Ligands to the (IRAP)/AT4 receptor encompassing a 4-hydroxydiphenylmethane scaffold replacing Tyr2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 5.34 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL261120 | ANGIOTENSIN IV | — | 1 | 7.22 |
| CHEMBL504736 | — | — | 1 | 5.92 |
| CHEMBL448184 | — | — | 1 | 5.89 |
| CHEMBL499984 | — | — | 1 | 5.89 |
| CHEMBL355434 | — | — | 1 | 5.85 |
| CHEMBL499779 | — | — | 1 | 5.75 |
| CHEMBL448920 | — | — | 1 | 5.48 |
| CHEMBL469483 | — | — | 1 | 5.43 |
| CHEMBL450452 | — | — | 1 | 5.41 |
| CHEMBL501693 | — | — | 1 | 5.20 |
| CHEMBL447726 | — | — | 1 | 5.13 |
| CHEMBL501326 | — | — | 1 | 4.92 |
| CHEMBL470072 | — | — | 1 | 4.80 |
| CHEMBL488627 | — | — | 1 | 4.46 |
| CHEMBL487435 | — | — | 1 | 4.12 |
| CHEMBL469484 | — | — | 1 | 4.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL261120 | ANGIOTENSIN IV | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL504736 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL448184 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL499984 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL355434 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL499779 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL448920 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL469483 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL450452 | — | Ki | = | 3900.0 | nM | 5.41 |
| CHEMBL501693 | — | Ki | = | 6300.0 | nM | 5.20 |
| CHEMBL447726 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL501326 | — | Ki | = | 12000.0 | nM | 4.92 |
| CHEMBL470072 | — | Ki | = | 16000.0 | nM | 4.80 |
| CHEMBL488627 | — | Ki | = | 35000.0 | nM | 4.46 |
| CHEMBL487435 | — | Ki | = | 76000.0 | nM | 4.12 |
| CHEMBL469484 | — | Ki | = | 97000.0 | nM | 4.01 |