Assay Detail
Functional
CHEMBL1788078
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Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum W2 synchronized ring stage parasites infected in erythrocytes assessed as reduction in parasitemia after 48 hrs by Giemsa staining
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 1 — Organism |
| 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 | 11 | 7.98 | 8.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1782073 | — | — | 1 | 8.68 |
| CHEMBL1783729 | — | — | 1 | 8.64 |
| CHEMBL1783730 | — | — | 1 | 8.40 |
| CHEMBL1783728 | — | — | 1 | 8.39 |
| CHEMBL1783732 | — | — | 1 | 8.38 |
| CHEMBL1783731 | — | — | 1 | 8.32 |
| CHEMBL1208264 | ARTELINIC ACID | — | 1 | 8.25 |
| CHEMBL269671 | ARTEMISININ | 3.0 | 1 | 7.92 |
| CHEMBL76 | CHLOROQUINE | 4.0 | 1 | 7.11 |
| CHEMBL374508 | E-64 | — | 1 | 5.71 |
| CHEMBL1783733 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1782073 | — | IC50 | = | 2.08 | nM | 8.68 |
| CHEMBL1783729 | — | IC50 | = | 2.27 | nM | 8.64 |
| CHEMBL1783730 | — | IC50 | = | 3.94 | nM | 8.40 |
| CHEMBL1783728 | — | IC50 | = | 4.09 | nM | 8.39 |
| CHEMBL1783732 | — | IC50 | = | 4.21 | nM | 8.38 |
| CHEMBL1783731 | — | IC50 | = | 4.81 | nM | 8.32 |
| CHEMBL1208264 | ARTELINIC ACID | IC50 | = | 5.66 | nM | 8.25 |
| CHEMBL269671 | ARTEMISININ | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL76 | CHLOROQUINE | IC50 | = | 78.1 | nM | 7.11 |
| CHEMBL374508 | E-64 | IC50 | = | 1955.0 | nM | 5.71 |
| CHEMBL1783733 | — | IC50 | > | 10000.0 | nM | - |