Assay Detail
Functional
CHEMBL1667255
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Antimalarial activity against Plasmodium falciparum Kenyan isolates expressing DHFR Ser108Asn, Asn51Ile and Cys59Arg triple mutant by [3H]hypoxanthine incorporation assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.12 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129788 | — | — | 1 | 10.00 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 7.68 |
| CHEMBL92583 | CHLORCYCLOGUANIL | — | 1 | 7.40 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.08 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 6.11 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 4.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129788 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 20.91 | nM | 7.68 |
| CHEMBL92583 | CHLORCYCLOGUANIL | IC50 | = | 39.99 | nM | 7.40 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 83.59 | nM | 7.08 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 778.28 | nM | 6.11 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 33655.0 | nM | 4.47 |