Assay Detail
Functional
CHEMBL958384
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Antimalarial activity against chloroquine-resistant Plasmodium falciparum TM6
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis, antimalarial activity, and preclinical pharmacology of a novel series of 4'-fluoro and 4'-chloro analogues of amodiaquine. Identification of a suitable "back-up" compound for N-tert-butyl isoquine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.73 | 8.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL523677 | — | — | 1 | 8.38 |
| CHEMBL523342 | — | — | 1 | 8.35 |
| CHEMBL446386 | — | — | 1 | 8.30 |
| CHEMBL475811 | — | — | 1 | 8.19 |
| CHEMBL1630 | — | — | 1 | 8.14 |
| CHEMBL492326 | — | — | 1 | 8.03 |
| CHEMBL492914 | — | — | 1 | 7.99 |
| CHEMBL492722 | — | — | 1 | 7.99 |
| CHEMBL453384 | — | — | 1 | 7.66 |
| CHEMBL492307 | — | — | 1 | 7.61 |
| CHEMBL502137 | — | — | 1 | 7.22 |
| CHEMBL76 | CHLOROQUINE | 4.0 | 1 | 7.02 |
| CHEMBL492913 | — | — | 1 | 7.02 |
| CHEMBL475810 | — | — | 1 | 6.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL523677 | — | IC50 | = | 4.2 | nM | 8.38 |
| CHEMBL523342 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL446386 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL475811 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL1630 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL492326 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL492914 | — | IC50 | = | 10.3 | nM | 7.99 |
| CHEMBL492722 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL453384 | — | IC50 | = | 21.9 | nM | 7.66 |
| CHEMBL492307 | — | IC50 | = | 24.4 | nM | 7.61 |
| CHEMBL502137 | — | IC50 | = | 60.8 | nM | 7.22 |
| CHEMBL76 | CHLOROQUINE | IC50 | = | 95.1 | nM | 7.02 |
| CHEMBL492913 | — | IC50 | = | 96.3 | nM | 7.02 |
| CHEMBL475810 | — | IC50 | = | 500.0 | nM | 6.30 |