Assay Detail
Binding
CHEMBL4181677
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Plasmodium falciparum DHFR
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Discovery of new antimalarial agents: Second-generation dual inhibitors against FP-2 and PfDHFR via fragments assembely.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 7.38 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL138060 | — | — | 1 | 9.41 |
| CHEMBL545921 | — | — | 1 | 9.24 |
| CHEMBL544227 | CHLORCYCLOGUANIL HYDROCHLORIDE | — | 1 | 8.82 |
| CHEMBL2387269 | — | — | 1 | 8.34 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 7.24 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 7.08 |
| CHEMBL3819601 | — | — | 1 | 6.64 |
| CHEMBL1939368 | — | — | 1 | 5.20 |
| CHEMBL549325 | — | — | 1 | 4.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL138060 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL545921 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL544227 | CHLORCYCLOGUANIL HYDROCHLORIDE | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL2387269 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL3819601 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL1939368 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL549325 | — | IC50 | = | 35500.0 | nM | 4.45 |