Assay Detail
Functional
CHEMBL769485
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In vitro antimalarial activity against Plasmodium falciparum Csl-2 triple DHFR mutant (C59R/S108N/I164L) relative to trimethoprim
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 | 7.14 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL120123 | — | — | 1 | 7.70 |
| CHEMBL279948 | — | — | 1 | 7.70 |
| CHEMBL416373 | — | — | 1 | 7.52 |
| CHEMBL274031 | — | — | 1 | 7.52 |
| CHEMBL119224 | — | — | 1 | 7.52 |
| CHEMBL22137 | — | — | 1 | 7.52 |
| CHEMBL291931 | — | — | 1 | 7.30 |
| CHEMBL118602 | — | — | 1 | 7.30 |
| CHEMBL22139 | — | — | 1 | 7.22 |
| CHEMBL22138 | — | — | 1 | 7.22 |
| CHEMBL22901 | — | — | 1 | 6.96 |
| CHEMBL21395 | — | — | 1 | 6.92 |
| CHEMBL56146 | — | — | 1 | 6.89 |
| CHEMBL416376 | — | — | 1 | 6.77 |
| CHEMBL22146 | — | — | 1 | 6.68 |
| CHEMBL22811 | — | — | 1 | 6.58 |
| CHEMBL325533 | — | — | 1 | 6.12 |
| CHEMBL419055 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL120123 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL279948 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL416373 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL274031 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL119224 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL22137 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL291931 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL118602 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL22139 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL22138 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL22901 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL21395 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL56146 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL416376 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL22146 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL22811 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL325533 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL419055 | — | IC50 | > | 420.0 | nM | - |