Assay Detail
Binding
CHEMBL1788076
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Inhibition of Plasmodium falciparum recombinant falcipain-2 incubated for 30 mins at room temperature before addition of substrate benzoxycarbonyl-Leu-Arg-7-amino-4-methyl-coumarin by spectrofluorometry
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 5.58 | 7.08 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL374508 | E-64 | — | 1 | 7.08 |
| CHEMBL1783733 | — | — | 1 | 6.68 |
| CHEMBL1783732 | — | — | 1 | 6.46 |
| CHEMBL1782073 | — | — | 1 | 5.30 |
| CHEMBL1783730 | — | — | 1 | 5.04 |
| CHEMBL1783728 | — | — | 1 | 4.78 |
| CHEMBL1783731 | — | — | 1 | 4.67 |
| CHEMBL1783729 | — | — | 1 | 4.65 |
| CHEMBL269671 | ARTEMISININ | 3.0 | 1 | - |
| CHEMBL1208264 | ARTELINIC ACID | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL374508 | E-64 | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL1783733 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL1783732 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1782073 | — | IC50 | = | 4950.0 | nM | 5.30 |
| CHEMBL1783730 | — | IC50 | = | 9220.0 | nM | 5.04 |
| CHEMBL1783728 | — | IC50 | = | 16500.0 | nM | 4.78 |
| CHEMBL1783731 | — | IC50 | = | 21600.0 | nM | 4.67 |
| CHEMBL1783729 | — | IC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL269671 | ARTEMISININ | IC50 | - | — | - | |
| CHEMBL1208264 | ARTELINIC ACID | IC50 | - | — | - |