Assay Detail
Binding
CHEMBL5544307
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Cathepsin D using MCA labeled GKPILFFRLK(DNP)-D-R-NH2 as substrate preincubated for 10 mins followed by substrate addition by FRET assay
8
Total Activities
8
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
Synthesis and biological evaluation of selective Pepstatin based trifluoromethylated inhibitors of Cathepsin D.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.87 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5569371 | — | — | 1 | 9.40 |
| CHEMBL5571122 | — | — | 1 | 8.70 |
| CHEMBL5570548 | — | — | 1 | 7.55 |
| CHEMBL5573834 | — | — | 1 | 7.24 |
| CHEMBL5594826 | — | — | 1 | 7.19 |
| CHEMBL5569502 | — | — | 1 | 7.14 |
| CHEMBL296588 | PEPSTATIN | 2.0 | 1 | - |
| CHEMBL5572049 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5569371 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL5571122 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5570548 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5573834 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL5594826 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5569502 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL296588 | PEPSTATIN | IC50 | = | 5.0 | nM | - |
| CHEMBL5572049 | — | IC50 | > | 2000.0 | nM | - |