Assay Detail
Binding
CHEMBL4121604
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Inhibition of Toxoplasma gondii 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 | Toxoplasma gondii |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
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 | 6.13 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL222649 | — | — | 1 | 8.70 |
| CHEMBL4126546 | — | — | 1 | 6.96 |
| CHEMBL4125776 | — | — | 1 | 6.92 |
| CHEMBL4126172 | — | — | 1 | 6.92 |
| CHEMBL4128887 | — | — | 1 | 6.80 |
| CHEMBL4129611 | — | — | 1 | 6.75 |
| CHEMBL4130087 | — | — | 1 | 6.60 |
| CHEMBL4129470 | — | — | 1 | 6.46 |
| CHEMBL4128244 | — | — | 1 | 6.44 |
| CHEMBL4130249 | — | — | 1 | 6.40 |
| CHEMBL4126824 | — | — | 1 | 6.38 |
| CHEMBL4126741 | — | — | 1 | 6.28 |
| CHEMBL4128116 | — | — | 1 | 6.27 |
| CHEMBL4129822 | — | — | 1 | 6.18 |
| CHEMBL4126455 | — | — | 1 | 5.92 |
| CHEMBL4128869 | — | — | 1 | 5.92 |
| CHEMBL4126611 | — | — | 1 | 5.85 |
| CHEMBL4129884 | — | — | 1 | 5.85 |
| CHEMBL4129022 | — | — | 1 | 5.70 |
| CHEMBL565079 | — | — | 1 | 5.70 |
| CHEMBL4130028 | — | — | 1 | 5.62 |
| CHEMBL4127618 | — | — | 1 | 5.40 |
| CHEMBL4127142 | — | — | 1 | 5.34 |
| CHEMBL4127007 | — | — | 1 | 5.21 |
| CHEMBL4126675 | — | — | 1 | 5.18 |
| CHEMBL4130234 | — | — | 1 | 5.01 |
| CHEMBL4128058 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL222649 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4126546 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL4125776 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4126172 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4128887 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4129611 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4130087 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4129470 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4128244 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL4130249 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4126824 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL4126741 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL4128116 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL4129822 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4126455 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4128869 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4126611 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4129884 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4129022 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL565079 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4130028 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4127618 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4127142 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL4127007 | — | IC50 | = | 6100.0 | nM | 5.21 |
| CHEMBL4126675 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL4130234 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL4128058 | — | IC50 | = | 14000.0 | nM | 4.85 |