Assay Detail
Binding
CHEMBL4121605
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Inhibition of human cathepsin L using Z-L-R-AMC as substrate preincubated for 5 mins followed by substrate addition measured over 5 mins by spectrophotometric method
27
Total Activities
27
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
Optimization of dipeptidic inhibitors of cathepsin L for improved Toxoplasma gondii selectivity and CNS permeability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 6.76 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222649 | — | — | 1 | 8.52 |
| CHEMBL4129611 | — | — | 1 | 7.82 |
| CHEMBL4126611 | — | — | 1 | 7.38 |
| CHEMBL565079 | — | — | 1 | 7.36 |
| CHEMBL4128244 | — | — | 1 | 7.32 |
| CHEMBL4125776 | — | — | 1 | 7.11 |
| CHEMBL4128887 | — | — | 1 | 7.08 |
| CHEMBL4127007 | — | — | 1 | 7.07 |
| CHEMBL4126455 | — | — | 1 | 7.04 |
| CHEMBL4126546 | — | — | 1 | 7.03 |
| CHEMBL4130028 | — | — | 1 | 6.96 |
| CHEMBL4129470 | — | — | 1 | 6.96 |
| CHEMBL4129884 | — | — | 1 | 6.89 |
| CHEMBL4126741 | — | — | 1 | 6.85 |
| CHEMBL4130249 | — | — | 1 | 6.85 |
| CHEMBL4126824 | — | — | 1 | 6.72 |
| CHEMBL4127142 | — | — | 1 | 6.62 |
| CHEMBL4128116 | — | — | 1 | 6.55 |
| CHEMBL4130087 | — | — | 1 | 6.55 |
| CHEMBL4126172 | — | — | 1 | 6.50 |
| CHEMBL4129822 | — | — | 1 | 6.23 |
| CHEMBL4126675 | — | — | 1 | 5.92 |
| CHEMBL4129022 | — | — | 1 | 5.92 |
| CHEMBL4127618 | — | — | 1 | 5.60 |
| CHEMBL4128869 | — | — | 1 | 5.46 |
| CHEMBL4130234 | — | — | 1 | 5.39 |
| CHEMBL4128058 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222649 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4129611 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4126611 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL565079 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4128244 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL4125776 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL4128887 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4127007 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL4126455 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL4126546 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL4130028 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4129470 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4129884 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL4126741 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4130249 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL4126824 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL4127142 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL4128116 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4130087 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL4126172 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4129822 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL4126675 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4129022 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4127618 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4128869 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL4130234 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4128058 | — | IC50 | = | 816000.0 | nM | - |