Assay Detail
Binding
CHEMBL2176197
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Inhibition of human recombinant NEP using Mca-RPPGFSAFK(Dnp)-OH as substrate incubated for 15 mins prior to substrate addition measured after 20 to 30 mins by fluorimetric analysis
9
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel β-amino acid derivatives as inhibitors of cathepsin A.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.60 | 6.52 |
| Inhibition | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3145333 | — | — | 1 | 6.52 |
| CHEMBL2171396 | — | — | 1 | 5.72 |
| CHEMBL2171398 | — | — | 1 | 4.57 |
| CHEMBL2171393 | — | — | 2 | - |
| CHEMBL2171392 | — | — | 2 | - |
| CHEMBL3145346 | — | — | 1 | - |
| CHEMBL3145341 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3145333 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2171396 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL2171398 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL2171393 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL2171392 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL3145346 | — | IC50 | < | 60.0 | nM | - |
| CHEMBL2171393 | — | Inhibition | - | % | - | |
| CHEMBL2171392 | — | Inhibition | - | % | - | |
| CHEMBL3145341 | — | Inhibition | - | % | - |