Assay Detail
Functional
CHEMBL1667347
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antimalarial activity against pyrimethamine-resistant Plasmodium falciparum V1S expressing DHFR quadruple mutant with point mutations at codons 108, 51, 59 and 164 gene 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 | 7.48 | 10.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL129788 | — | — | 1 | 10.20 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 7.61 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.40 |
| CHEMBL92583 | CHLORCYCLOGUANIL | — | 1 | 7.04 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 5.16 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL129788 | — | IC50 | = | 0.063 | nM | 10.20 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 24.8 | nM | 7.61 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL92583 | CHLORCYCLOGUANIL | IC50 | = | 92.3 | nM | 7.04 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 6929.14 | nM | 5.16 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 101754.0 | nM | - |