Assay Detail
Functional
CHEMBL769484
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antimalarial activity against Plasmodium falciparum Csl-2 triple DHFR mutant (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 | 5.07 | 5.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL279948 | — | — | 1 | 5.58 |
| CHEMBL120123 | — | — | 1 | 5.54 |
| CHEMBL274031 | — | — | 1 | 5.48 |
| CHEMBL416373 | — | — | 1 | 5.47 |
| CHEMBL22137 | — | — | 1 | 5.46 |
| CHEMBL119224 | — | — | 1 | 5.45 |
| CHEMBL118602 | — | — | 1 | 5.27 |
| CHEMBL291931 | — | — | 1 | 5.24 |
| CHEMBL22138 | — | — | 1 | 5.17 |
| CHEMBL22139 | — | — | 1 | 5.11 |
| CHEMBL22901 | — | — | 1 | 4.88 |
| CHEMBL21395 | — | — | 1 | 4.84 |
| CHEMBL56146 | — | — | 1 | 4.82 |
| CHEMBL416376 | — | — | 1 | 4.70 |
| CHEMBL22146 | — | — | 1 | 4.59 |
| CHEMBL22811 | — | — | 1 | 4.51 |
| CHEMBL325533 | — | — | 1 | 4.04 |
| CHEMBL419055 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL279948 | — | IC50 | = | 2640.0 | nM | 5.58 |
| CHEMBL120123 | — | IC50 | = | 2850.0 | nM | 5.54 |
| CHEMBL274031 | — | IC50 | = | 3330.0 | nM | 5.48 |
| CHEMBL416373 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL22137 | — | IC50 | = | 3460.0 | nM | 5.46 |
| CHEMBL119224 | — | IC50 | = | 3517.0 | nM | 5.45 |
| CHEMBL118602 | — | IC50 | = | 5370.0 | nM | 5.27 |
| CHEMBL291931 | — | IC50 | = | 5730.0 | nM | 5.24 |
| CHEMBL22138 | — | IC50 | = | 6750.0 | nM | 5.17 |
| CHEMBL22139 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL22901 | — | IC50 | = | 13150.0 | nM | 4.88 |
| CHEMBL21395 | — | IC50 | = | 14360.0 | nM | 4.84 |
| CHEMBL56146 | — | IC50 | = | 15260.0 | nM | 4.82 |
| CHEMBL416376 | — | IC50 | = | 19850.0 | nM | 4.70 |
| CHEMBL22146 | — | IC50 | = | 25610.0 | nM | 4.59 |
| CHEMBL22811 | — | IC50 | = | 30580.0 | nM | 4.51 |
| CHEMBL325533 | — | IC50 | = | 90810.0 | nM | 4.04 |
| CHEMBL419055 | — | IC50 | > | 50000.0 | nM | - |