Assay Detail
Functional
CHEMBL760860
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In vitro anti-plasmodial activity against Plasmodium falciparum dihydrofolate reductase C59R+S108N/I164L (Csl-2) mutant
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 | 5.60 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL346963 | — | — | 1 | 6.85 |
| CHEMBL329687 | — | — | 1 | 6.60 |
| CHEMBL158639 | — | — | 1 | 6.54 |
| CHEMBL161009 | — | — | 1 | 6.31 |
| CHEMBL7130 | — | — | 1 | 6.28 |
| CHEMBL444605 | — | — | 1 | 5.75 |
| CHEMBL346932 | — | — | 1 | 5.72 |
| CHEMBL352441 | — | — | 1 | 5.72 |
| CHEMBL422005 | — | — | 1 | 5.72 |
| CHEMBL278847 | — | — | 1 | 5.60 |
| CHEMBL22693 | — | — | 1 | 5.57 |
| CHEMBL278813 | — | — | 1 | 5.57 |
| CHEMBL22403 | — | — | 1 | 5.54 |
| CHEMBL346982 | — | — | 1 | 5.54 |
| CHEMBL416552 | — | — | 1 | 5.52 |
| CHEMBL158570 | — | — | 1 | 5.51 |
| CHEMBL161451 | — | — | 1 | 5.48 |
| CHEMBL161117 | — | — | 1 | 5.47 |
| CHEMBL348151 | — | — | 1 | 5.47 |
| CHEMBL21921 | — | — | 1 | 5.44 |
| CHEMBL161757 | — | — | 1 | 5.41 |
| CHEMBL352195 | — | — | 1 | 5.40 |
| CHEMBL161673 | — | — | 1 | 5.39 |
| CHEMBL161034 | — | — | 1 | 5.32 |
| CHEMBL159052 | — | — | 1 | 5.28 |
| CHEMBL354011 | — | — | 1 | 5.12 |
| CHEMBL747 | CYCLOGUANIL | 2.0 | 1 | 4.42 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 4.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL346963 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL329687 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL158639 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL161009 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL7130 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL444605 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL346932 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL352441 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL422005 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL278847 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL22693 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL278813 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL22403 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL346982 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL416552 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL158570 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL161451 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL161117 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL348151 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL21921 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL161757 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL352195 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL161673 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL161034 | — | IC50 | = | 4800.0 | nM | 5.32 |
| CHEMBL159052 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL354011 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL747 | CYCLOGUANIL | IC50 | = | 37900.0 | nM | 4.42 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 41700.0 | nM | 4.38 |