Assay Detail
Binding
CHEMBL1100889
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Inhibition of catalytic activity of human aminopeptidase N transfected in HEK293 cells assessed as formation of p-nitroaniline
23
Total Activities
12
Compounds Tested
2
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
The replacement of His(4) in angiotensin IV by conformationally constrained residues provides highly potent and selective analogues.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 7.18 | 8.07 |
| Activity | 11 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1077583 | — | — | 2 | 8.07 |
| CHEMBL1077582 | — | — | 2 | 7.90 |
| CHEMBL259019 | — | — | 2 | 7.56 |
| CHEMBL1077592 | — | — | 2 | 7.30 |
| CHEMBL1077586 | — | — | 2 | 7.28 |
| CHEMBL1077585 | — | — | 2 | 7.26 |
| CHEMBL261120 | ANGIOTENSIN IV | — | 1 | 7.25 |
| CHEMBL260622 | — | — | 2 | 7.00 |
| CHEMBL1077584 | — | — | 2 | 6.89 |
| CHEMBL1077591 | — | — | 2 | 6.74 |
| CHEMBL1077590 | — | — | 2 | 6.66 |
| CHEMBL1077589 | — | — | 2 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1077583 | — | Ki | = | 8.511 | nM | 8.07 |
| CHEMBL1077582 | — | Ki | = | 12.59 | nM | 7.90 |
| CHEMBL259019 | — | Ki | = | 27.54 | nM | 7.56 |
| CHEMBL1077592 | — | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1077586 | — | Ki | = | 52.48 | nM | 7.28 |
| CHEMBL1077585 | — | Ki | = | 54.95 | nM | 7.26 |
| CHEMBL261120 | ANGIOTENSIN IV | Ki | = | 56.23 | nM | 7.25 |
| CHEMBL260622 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL1077584 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL1077591 | — | Ki | = | 181.97 | nM | 6.74 |
| CHEMBL1077590 | — | Ki | = | 218.78 | nM | 6.66 |
| CHEMBL1077589 | — | Ki | = | 512.86 | nM | 6.29 |
| CHEMBL1077589 | — | Activity | - | — | - | |
| CHEMBL1077590 | — | Activity | - | — | - | |
| CHEMBL1077591 | — | Activity | - | — | - | |
| CHEMBL1077592 | — | Activity | - | — | - | |
| CHEMBL1077582 | — | Activity | - | — | - | |
| CHEMBL1077583 | — | Activity | - | — | - | |
| CHEMBL1077584 | — | Activity | - | — | - | |
| CHEMBL1077585 | — | Activity | - | — | - | |
| CHEMBL1077586 | — | Activity | - | — | - | |
| CHEMBL259019 | — | Activity | - | — | - | |
| CHEMBL260622 | — | Activity | - | — | - |