Assay Detail
Functional
CHEMBL954346
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Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 infected type A+ human erythrocytes after 24 hrs by [G-3H]hypoxanthine uptake
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.97 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL566534 | ARTEMETHER | 4.0 | 1 | 8.90 |
| CHEMBL190579 | — | — | 1 | 8.52 |
| CHEMBL99800 | — | — | 1 | 8.44 |
| CHEMBL450287 | — | — | 1 | 8.17 |
| CHEMBL495354 | — | — | 1 | 8.14 |
| CHEMBL504466 | — | — | 1 | 8.09 |
| CHEMBL493143 | — | — | 1 | 8.08 |
| CHEMBL522178 | — | — | 1 | 8.06 |
| CHEMBL269671 | ARTEMISININ | 3.0 | 1 | 8.02 |
| CHEMBL463645 | — | — | 1 | 7.96 |
| CHEMBL522484 | — | — | 1 | 7.90 |
| CHEMBL446090 | — | — | 1 | 7.88 |
| CHEMBL508318 | — | — | 1 | 7.84 |
| CHEMBL443384 | — | — | 1 | 7.79 |
| CHEMBL500803 | — | — | 1 | 7.71 |
| CHEMBL506042 | — | — | 1 | 7.69 |
| CHEMBL495353 | — | — | 1 | 7.58 |
| CHEMBL76 | CHLOROQUINE | 4.0 | 1 | 6.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL566534 | ARTEMETHER | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL190579 | — | IC50 | = | 3.02 | nM | 8.52 |
| CHEMBL99800 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL450287 | — | IC50 | = | 6.76 | nM | 8.17 |
| CHEMBL495354 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL504466 | — | IC50 | = | 8.22 | nM | 8.09 |
| CHEMBL493143 | — | IC50 | = | 8.32 | nM | 8.08 |
| CHEMBL522178 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL269671 | ARTEMISININ | IC50 | = | 9.54 | nM | 8.02 |
| CHEMBL463645 | — | IC50 | = | 11.1 | nM | 7.96 |
| CHEMBL522484 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL446090 | — | IC50 | = | 13.23 | nM | 7.88 |
| CHEMBL508318 | — | IC50 | = | 14.34 | nM | 7.84 |
| CHEMBL443384 | — | IC50 | = | 16.21 | nM | 7.79 |
| CHEMBL500803 | — | IC50 | = | 19.34 | nM | 7.71 |
| CHEMBL506042 | — | IC50 | = | 20.22 | nM | 7.69 |
| CHEMBL495353 | — | IC50 | = | 26.21 | nM | 7.58 |
| CHEMBL76 | CHLOROQUINE | IC50 | = | 187.34 | nM | 6.73 |