Assay Detail
Binding
CHEMBL2210541
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Inhibition of APN in human ES2 cell surface assessed as inhibition of L-Leu-p-nitroanilide substrate hydrolysis incubated for 5 mins before substrate addition by UV-Vis spectrophotometric analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | ES2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Synthetic Aminopeptidase N/CD13 Inhibitors to Overcome Cancer Metastasis and Angiogenesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.76 | 6.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2204959 | — | — | 1 | 6.38 |
| CHEMBL2204943 | — | — | 1 | 6.32 |
| CHEMBL2204950 | — | — | 1 | 6.10 |
| CHEMBL2204954 | — | — | 1 | 6.04 |
| CHEMBL2204947 | — | — | 1 | 6.03 |
| CHEMBL2204949 | — | — | 1 | 5.96 |
| CHEMBL2204953 | — | — | 1 | 5.82 |
| CHEMBL2204951 | — | — | 1 | 5.52 |
| CHEMBL2204945 | — | — | 1 | 5.19 |
| CHEMBL2204952 | — | — | 1 | 5.16 |
| CHEMBL29292 | UBENIMEX | 2.0 | 1 | 4.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2204959 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2204943 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL2204950 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL2204954 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL2204947 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL2204949 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2204953 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2204951 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL2204945 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL2204952 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL29292 | UBENIMEX | IC50 | = | 16000.0 | nM | 4.80 |