Assay Detail
Binding
CHEMBL4132610
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Inhibition of recombinant human C-terminal His10-tagged APN (Lys69 to Lys967 residues) using Ala-AMC as substrate measured for 30 mins by fluorescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Puromycin based inhibitors of aminopeptidases for the potential treatment of hematologic malignancies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.87 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4169814 | — | — | 1 | 6.57 |
| CHEMBL4165328 | — | — | 1 | 6.55 |
| CHEMBL3244800 | — | — | 1 | 6.38 |
| CHEMBL2103847 | TOSEDOSTAT | 2.0 | 1 | 6.17 |
| CHEMBL29292 | UBENIMEX | 2.0 | 1 | 6.10 |
| CHEMBL3244799 | — | — | 1 | 5.96 |
| CHEMBL4173240 | — | — | 1 | 5.50 |
| CHEMBL4161892 | — | — | 1 | 5.25 |
| CHEMBL469912 | PUROMYCIN | 2.0 | 1 | 4.39 |
| CHEMBL4161496 | — | — | 1 | - |
| CHEMBL4161744 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4169814 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4165328 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL3244800 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2103847 | TOSEDOSTAT | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL29292 | UBENIMEX | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL3244799 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4173240 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL4161892 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL469912 | PUROMYCIN | IC50 | = | 41000.0 | nM | 4.39 |
| CHEMBL4161496 | — | IC50 | - | — | - | |
| CHEMBL4161744 | — | IC50 | - | — | - |