Assay Detail
Binding
CHEMBL5544306
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of porcine gastric mucosa Pepsin 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 | Sus scrofa |
| Tissue | Gastric mucosa |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 7.01 | 7.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5571122 | — | — | 1 | 7.68 |
| CHEMBL5569371 | — | — | 1 | 7.51 |
| CHEMBL5570548 | — | — | 1 | 7.32 |
| CHEMBL296588 | PEPSTATIN | 2.0 | 1 | 7.30 |
| CHEMBL5569502 | — | — | 1 | 6.71 |
| CHEMBL5594826 | — | — | 1 | 6.43 |
| CHEMBL5573834 | — | — | 1 | 6.11 |
| CHEMBL5572049 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5571122 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5569371 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5570548 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL296588 | PEPSTATIN | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5569502 | — | IC50 | = | 193.0 | nM | 6.71 |
| CHEMBL5594826 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL5573834 | — | IC50 | = | 775.0 | nM | 6.11 |
| CHEMBL5572049 | — | IC50 | > | 4000.0 | nM | - |