Assay Detail
Functional
CHEMBL1676410
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Antimalarial activity against Plasmodium falciparum D6 harboring Plasmodium vivax DHFR S58R and S117N mutant infected in RBCs assessed as inhibition of [3H]hypoxanthine incorporation after 72 hrs
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Defining the role of mutations in Plasmodium vivax dihydrofolate reductase-thymidylate synthase gene using an episomal Plasmodium falciparum transfection system.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 8.84 | 9.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1213592 | CLOCIGUANIL | 2.0 | 1 | 9.23 |
| CHEMBL129788 | — | — | 1 | 9.16 |
| CHEMBL747 | CYCLOGUANIL | 2.0 | 1 | 8.77 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 8.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1213592 | CLOCIGUANIL | IC50 | = | 0.582 | nM | 9.23 |
| CHEMBL129788 | — | IC50 | = | 0.69 | nM | 9.16 |
| CHEMBL747 | CYCLOGUANIL | IC50 | = | 1.699 | nM | 8.77 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 6.26 | nM | 8.20 |