Assay Detail
Binding
CHEMBL4041124
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Inhibition of recombinant Plasmodium falciparum falcipain-2 expressed in Escherichia coli M15(pREP4) using Cbz-Phe-Arg-AMC as substrate by fluorescence assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of Novel Peptide-Based Michael Acceptors Targeting Rhodesain and Falcipain-2 for the Treatment of Neglected Tropical Diseases (NTDs).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.90 | 6.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4096388 | — | — | 1 | 6.96 |
| CHEMBL374508 | E-64 | — | 1 | 6.60 |
| CHEMBL4072275 | — | — | 1 | 6.60 |
| CHEMBL4083754 | — | — | 1 | 6.11 |
| CHEMBL4062015 | — | — | 1 | 6.11 |
| CHEMBL4070637 | — | — | 1 | 5.88 |
| CHEMBL4078345 | — | — | 1 | 5.52 |
| CHEMBL2402204 | — | — | 1 | 5.13 |
| CHEMBL4101714 | — | — | 1 | 5.02 |
| CHEMBL4100751 | — | — | 1 | 5.02 |
| CHEMBL4093034 | — | — | 1 | - |
| CHEMBL4082758 | — | — | 1 | - |
| CHEMBL4081250 | — | — | 1 | - |
| CHEMBL4099269 | — | — | 1 | - |
| CHEMBL4090306 | — | — | 1 | - |
| CHEMBL4060936 | — | — | 1 | - |
| CHEMBL4074432 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4096388 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL374508 | E-64 | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4072275 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL4083754 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4062015 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL4070637 | — | IC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL4078345 | — | IC50 | = | 3010.0 | nM | 5.52 |
| CHEMBL2402204 | — | IC50 | = | 7330.0 | nM | 5.13 |
| CHEMBL4101714 | — | IC50 | = | 9530.0 | nM | 5.02 |
| CHEMBL4100751 | — | IC50 | = | 9630.0 | nM | 5.02 |
| CHEMBL4093034 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4082758 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4081250 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4099269 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4090306 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4060936 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4074432 | — | IC50 | > | 50000.0 | nM | - |