Assay Detail
Binding
CHEMBL2176198
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Inhibition of human recombinant Myc-His10-tagged cathepsin A expressed in baculovirus infected Sf9 cells using BodipyFL labeled bradykinin as substrate incubated for 15 mins prior to substrate addition measured after 15 mins by fluorimetric analysis
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| 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 | 33 | 7.06 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2171390 | — | — | 1 | 8.52 |
| CHEMBL2171392 | — | — | 1 | 8.30 |
| CHEMBL2171394 | — | — | 1 | 8.00 |
| CHEMBL2171397 | — | — | 1 | 7.82 |
| CHEMBL2171398 | — | — | 1 | 7.82 |
| CHEMBL3145342 | — | — | 1 | 7.60 |
| CHEMBL2171396 | — | — | 1 | 7.58 |
| CHEMBL2171399 | — | — | 1 | 7.52 |
| CHEMBL3145341 | — | — | 1 | 7.42 |
| CHEMBL2171393 | — | — | 1 | 7.30 |
| CHEMBL3145343 | — | — | 1 | 7.24 |
| CHEMBL3145344 | — | — | 1 | 7.23 |
| CHEMBL2171391 | — | — | 1 | 7.22 |
| CHEMBL2171395 | — | — | 1 | 7.16 |
| CHEMBL3145334 | — | — | 1 | 7.16 |
| CHEMBL3145345 | — | — | 1 | 7.12 |
| CHEMBL3145347 | — | — | 1 | 7.06 |
| CHEMBL3145346 | — | — | 1 | 7.00 |
| CHEMBL2171402 | — | — | 1 | 7.00 |
| CHEMBL3145349 | — | — | 1 | 6.99 |
| CHEMBL2171401 | — | — | 1 | 6.96 |
| CHEMBL2171400 | — | — | 1 | 6.96 |
| CHEMBL3145348 | — | — | 1 | 6.92 |
| CHEMBL3145350 | — | — | 1 | 6.70 |
| CHEMBL3145351 | — | — | 1 | 6.65 |
| CHEMBL3145340 | — | — | 1 | 6.60 |
| CHEMBL3145353 | — | — | 1 | 6.56 |
| CHEMBL3145336 | — | — | 1 | 6.45 |
| CHEMBL3145337 | — | — | 1 | 6.43 |
| CHEMBL3145338 | — | — | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2171390 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2171392 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2171394 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2171397 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL2171398 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3145342 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2171396 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2171399 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3145341 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL2171393 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3145343 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL3145344 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL2171391 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL2171395 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3145334 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3145345 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL3145347 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL3145346 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2171402 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3145349 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL2171401 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2171400 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3145348 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL3145350 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3145351 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL3145340 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL3145353 | — | IC50 | = | 274.0 | nM | 6.56 |
| CHEMBL3145336 | — | IC50 | = | 357.0 | nM | 6.45 |
| CHEMBL3145337 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL3145338 | — | IC50 | = | 803.0 | nM | 6.09 |
| CHEMBL3145339 | — | IC50 | = | 5380.0 | nM | 5.27 |
| CHEMBL3145335 | — | IC50 | = | 7800.0 | nM | 5.11 |
| CHEMBL3145333 | — | IC50 | > | 30000.0 | nM | - |