Assay Detail
Functional
CHEMBL769492
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antimalarial activity against Plasmodium falciparum K1CB1 double DHFR mutant (C59R/S108N)
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 | 5.05 | 5.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL274031 | — | — | 1 | 5.45 |
| CHEMBL119224 | — | — | 1 | 5.43 |
| CHEMBL291931 | — | — | 1 | 5.42 |
| CHEMBL22137 | — | — | 1 | 5.38 |
| CHEMBL22139 | — | — | 1 | 5.37 |
| CHEMBL279948 | — | — | 1 | 5.36 |
| CHEMBL22901 | — | — | 1 | 5.30 |
| CHEMBL416373 | — | — | 1 | 4.99 |
| CHEMBL22138 | — | — | 1 | 4.84 |
| CHEMBL118602 | — | — | 1 | 4.79 |
| CHEMBL21395 | — | — | 1 | 4.78 |
| CHEMBL56146 | — | — | 1 | 4.77 |
| CHEMBL416376 | — | — | 1 | 4.70 |
| CHEMBL120123 | — | — | 1 | 4.60 |
| CHEMBL22811 | — | — | 1 | 4.56 |
| CHEMBL419055 | — | — | 1 | - |
| CHEMBL22146 | — | — | 1 | - |
| CHEMBL325533 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL274031 | — | IC50 | = | 3520.0 | nM | 5.45 |
| CHEMBL119224 | — | IC50 | = | 3690.0 | nM | 5.43 |
| CHEMBL291931 | — | IC50 | = | 3830.0 | nM | 5.42 |
| CHEMBL22137 | — | IC50 | = | 4180.0 | nM | 5.38 |
| CHEMBL22139 | — | IC50 | = | 4290.0 | nM | 5.37 |
| CHEMBL279948 | — | IC50 | = | 4380.0 | nM | 5.36 |
| CHEMBL22901 | — | IC50 | = | 5010.0 | nM | 5.30 |
| CHEMBL416373 | — | IC50 | = | 10160.0 | nM | 4.99 |
| CHEMBL22138 | — | IC50 | = | 14580.0 | nM | 4.84 |
| CHEMBL118602 | — | IC50 | = | 16260.0 | nM | 4.79 |
| CHEMBL21395 | — | IC50 | = | 16590.0 | nM | 4.78 |
| CHEMBL56146 | — | IC50 | = | 17140.0 | nM | 4.77 |
| CHEMBL416376 | — | IC50 | = | 19880.0 | nM | 4.70 |
| CHEMBL120123 | — | IC50 | = | 25240.0 | nM | 4.60 |
| CHEMBL22811 | — | IC50 | = | 27760.0 | nM | 4.56 |
| CHEMBL419055 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL22146 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL325533 | — | IC50 | > | 100000.0 | nM | - |