Assay Detail
Binding
CHEMBL5357326
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Inhibition of wild type Plasmodium falciparum DHFR using DHF as substrate assessed as inhibition constant in presence of NADPH by UV-Vis spectrometry analysis
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Plasmodium falciparum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Bifunctional dihydrofolate reductase-thymidylate synthase (CHEMBL1939) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum K1 |
Publication
Discovery of rigid biphenyl <i>Plasmodium falciparum</i> DHFR inhibitors using a fragment linking strategy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 9.37 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5415214 | — | — | 1 | 9.68 |
| CHEMBL5397904 | — | — | 1 | 9.64 |
| CHEMBL5421199 | — | — | 1 | 9.60 |
| CHEMBL5406769 | — | — | 1 | 9.54 |
| CHEMBL5417784 | — | — | 1 | 9.54 |
| CHEMBL3040038 | — | — | 1 | 9.37 |
| CHEMBL5432011 | — | — | 1 | 9.32 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 9.23 |
| CHEMBL5440218 | — | — | 1 | 8.97 |
| CHEMBL5404134 | — | — | 1 | 8.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5415214 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL5397904 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL5421199 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL5406769 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL5417784 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL3040038 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL5432011 | — | Ki | = | 0.48 | nM | 9.32 |
| CHEMBL22 | TRIMETHOPRIM | Ki | = | 0.59 | nM | 9.23 |
| CHEMBL5440218 | — | Ki | = | 1.06 | nM | 8.97 |
| CHEMBL5404134 | — | Ki | = | 1.59 | nM | 8.80 |