Assay Detail
Binding
CHEMBL4352728
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Inhibition of Plasmodium falciparum N-terminal His6-tagged falcipain-2 (35 residues) expressed in Escherichia coli M15 pREP4 using Z-Lue-Arg-AMC as substrate measured after 30 mins by spectrofluorometric method
20
Total Activities
20
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
Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.81 | 7.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4434685 | — | — | 1 | 7.54 |
| CHEMBL4467013 | — | — | 1 | 7.51 |
| CHEMBL4439637 | — | — | 1 | 7.48 |
| CHEMBL4442854 | — | — | 1 | 7.24 |
| CHEMBL4472824 | — | — | 1 | 7.23 |
| CHEMBL4564002 | — | — | 1 | 7.22 |
| CHEMBL1458713 | — | — | 1 | 7.17 |
| CHEMBL4442674 | — | — | 1 | 7.08 |
| CHEMBL4527228 | — | — | 1 | 6.81 |
| CHEMBL4516951 | — | — | 1 | 6.77 |
| CHEMBL4437416 | — | — | 1 | 6.63 |
| CHEMBL4456644 | — | — | 1 | 6.57 |
| CHEMBL4555968 | — | — | 1 | 6.34 |
| CHEMBL4475837 | — | — | 1 | 6.33 |
| CHEMBL4473513 | — | — | 1 | 5.51 |
| CHEMBL4594166 | — | — | 1 | 5.45 |
| CHEMBL269671 | ARTEMISININ | 3.0 | 1 | - |
| CHEMBL76 | CHLOROQUINE | 4.0 | 1 | - |
| CHEMBL4562998 | — | — | 1 | - |
| CHEMBL4555310 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4434685 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4467013 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL4439637 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4442854 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4472824 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4564002 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1458713 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4442674 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4527228 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL4516951 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL4437416 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL4456644 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL4555968 | — | IC50 | = | 455.0 | nM | 6.34 |
| CHEMBL4475837 | — | IC50 | = | 464.0 | nM | 6.33 |
| CHEMBL4473513 | — | IC50 | = | 3097.0 | nM | 5.51 |
| CHEMBL4594166 | — | IC50 | = | 3523.0 | nM | 5.45 |
| CHEMBL269671 | ARTEMISININ | IC50 | - | — | - | |
| CHEMBL76 | CHLOROQUINE | IC50 | - | — | - | |
| CHEMBL4562998 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL4555310 | — | IC50 | > | 50000.0 | nM | - |