Assay Detail
Functional
CHEMBL769668
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antimalarial activity relative to trimethoprim against Plasmodium falciparum Vl/S with quadruple DHFR mutant (N51I/C59R/S108N/I164L)
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL1939) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum K1 |
Publication
Target guided synthesis of 5-benzyl-2,4-diamonopyrimidines: their antimalarial activities and binding affinities to wild type and mutant dihydrofolate reductases from Plasmodium falciparum.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.50 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL419055 | — | — | 1 | 6.60 |
| CHEMBL291931 | — | — | 1 | 6.60 |
| CHEMBL325533 | — | — | 1 | 6.30 |
| CHEMBL22138 | — | — | 1 | - |
| CHEMBL56146 | — | — | 1 | - |
| CHEMBL22139 | — | — | 1 | - |
| CHEMBL274031 | — | — | 1 | - |
| CHEMBL119224 | — | — | 1 | - |
| CHEMBL22137 | — | — | 1 | - |
| CHEMBL416376 | — | — | 1 | - |
| CHEMBL118602 | — | — | 1 | - |
| CHEMBL22146 | — | — | 1 | - |
| CHEMBL22811 | — | — | 1 | - |
| CHEMBL22901 | — | — | 1 | - |
| CHEMBL120123 | — | — | 1 | - |
| CHEMBL279948 | — | — | 1 | - |
| CHEMBL416373 | — | — | 1 | - |
| CHEMBL21395 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL419055 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL291931 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL325533 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL22138 | — | IC50 | < | 40.0 | nM | - |
| CHEMBL56146 | — | IC50 | < | 110.0 | nM | - |
| CHEMBL22139 | — | IC50 | < | 50.0 | nM | - |
| CHEMBL274031 | — | IC50 | < | 60.0 | nM | - |
| CHEMBL119224 | — | IC50 | < | 150.0 | nM | - |
| CHEMBL22137 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL416376 | — | IC50 | < | 110.0 | nM | - |
| CHEMBL118602 | — | IC50 | < | 60.0 | nM | - |
| CHEMBL22146 | — | IC50 | < | 190.0 | nM | - |
| CHEMBL22811 | — | IC50 | < | 130.0 | nM | - |
| CHEMBL22901 | — | IC50 | < | 100.0 | nM | - |
| CHEMBL120123 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL279948 | — | IC50 | < | 20.0 | nM | - |
| CHEMBL416373 | — | IC50 | < | 130.0 | nM | - |
| CHEMBL21395 | — | IC50 | < | 80.0 | nM | - |