Assay Detail
Functional
CHEMBL765486
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In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase wild type (TM4/8.2)
28
Total Activities
28
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 | 28 | 6.34 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL161673 | — | — | 1 | 7.70 |
| CHEMBL346963 | — | — | 1 | 7.40 |
| CHEMBL747 | CYCLOGUANIL | 2.0 | 1 | 7.40 |
| CHEMBL7130 | — | — | 1 | 7.30 |
| CHEMBL161009 | — | — | 1 | 7.22 |
| CHEMBL416552 | — | — | 1 | 7.22 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 7.10 |
| CHEMBL161034 | — | — | 1 | 6.92 |
| CHEMBL158639 | — | — | 1 | 6.75 |
| CHEMBL22693 | — | — | 1 | 6.68 |
| CHEMBL346982 | — | — | 1 | 6.60 |
| CHEMBL22403 | — | — | 1 | 6.46 |
| CHEMBL278813 | — | — | 1 | 6.39 |
| CHEMBL278847 | — | — | 1 | 6.38 |
| CHEMBL329687 | — | — | 1 | 6.25 |
| CHEMBL161451 | — | — | 1 | 6.19 |
| CHEMBL21921 | — | — | 1 | 6.17 |
| CHEMBL422005 | — | — | 1 | 5.96 |
| CHEMBL444605 | — | — | 1 | 5.80 |
| CHEMBL352441 | — | — | 1 | 5.72 |
| CHEMBL346932 | — | — | 1 | 5.68 |
| CHEMBL161117 | — | — | 1 | 5.66 |
| CHEMBL352195 | — | — | 1 | 5.55 |
| CHEMBL159052 | — | — | 1 | 5.52 |
| CHEMBL348151 | — | — | 1 | 5.50 |
| CHEMBL158570 | — | — | 1 | 5.41 |
| CHEMBL354011 | — | — | 1 | 5.40 |
| CHEMBL161757 | — | — | 1 | 5.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL161673 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL346963 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL747 | CYCLOGUANIL | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL7130 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL161009 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL416552 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL161034 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL158639 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL22693 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL346982 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL22403 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL278813 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL278847 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL329687 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL161451 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL21921 | — | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL422005 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL444605 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL352441 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL346932 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL161117 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL352195 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL159052 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL348151 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL158570 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL354011 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL161757 | — | IC50 | = | 5500.0 | nM | 5.26 |