Assay Detail
Functional
CHEMBL760283
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In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase C59R/S108N (K1CB1) mutant
17
Total Activities
17
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
Inhibitors of multiple mutants of Plasmodium falciparum dihydrofolate reductase and their antimalarial activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.84 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL158639 | — | — | 1 | 6.75 |
| CHEMBL7130 | — | — | 1 | 6.66 |
| CHEMBL346963 | — | — | 1 | 6.58 |
| CHEMBL329687 | — | — | 1 | 6.51 |
| CHEMBL161009 | — | — | 1 | 6.32 |
| CHEMBL346982 | — | — | 1 | 6.00 |
| CHEMBL747 | CYCLOGUANIL | 2.0 | 1 | 5.62 |
| CHEMBL161673 | — | — | 1 | 5.62 |
| CHEMBL158570 | — | — | 1 | 5.58 |
| CHEMBL161117 | — | — | 1 | 5.57 |
| CHEMBL348151 | — | — | 1 | 5.55 |
| CHEMBL161757 | — | — | 1 | 5.51 |
| CHEMBL161451 | — | — | 1 | 5.51 |
| CHEMBL161034 | — | — | 1 | 5.51 |
| CHEMBL352195 | — | — | 1 | 5.48 |
| CHEMBL354011 | — | — | 1 | 5.31 |
| CHEMBL159052 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL158639 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL7130 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL346963 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL329687 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL161009 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL346982 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL747 | CYCLOGUANIL | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL161673 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL158570 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL161117 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL348151 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL161757 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL161451 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL161034 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL352195 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL354011 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL159052 | — | IC50 | = | 7400.0 | nM | 5.13 |