Assay Detail
Functional
CHEMBL760281
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In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase A16V/S108T (T9/94RC17) mutant
15
Total Activities
15
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 | 15 | 7.01 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL346982 | — | — | 1 | 8.40 |
| CHEMBL161451 | — | — | 1 | 8.40 |
| CHEMBL346963 | — | — | 1 | 8.40 |
| CHEMBL329687 | — | — | 1 | 7.70 |
| CHEMBL161034 | — | — | 1 | 7.40 |
| CHEMBL161757 | — | — | 1 | 7.30 |
| CHEMBL161117 | — | — | 1 | 7.22 |
| CHEMBL348151 | — | — | 1 | 6.75 |
| CHEMBL354011 | — | — | 1 | 6.72 |
| CHEMBL7130 | — | — | 1 | 6.48 |
| CHEMBL159052 | — | — | 1 | 6.43 |
| CHEMBL158570 | — | — | 1 | 6.41 |
| CHEMBL352195 | — | — | 1 | 6.38 |
| CHEMBL161673 | — | — | 1 | 5.72 |
| CHEMBL747 | CYCLOGUANIL | 2.0 | 1 | 5.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL346982 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL161451 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL346963 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL329687 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL161034 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL161757 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL161117 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL348151 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL354011 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL7130 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL159052 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL158570 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL352195 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL161673 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL747 | CYCLOGUANIL | IC50 | = | 3700.0 | nM | 5.43 |