Assay Detail
Binding
CHEMBL998901
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of pyrimethamine-resistant form-2 Plasmodium falciparum N51I, C59R, S108N, I164L, K96N mutant expressed in Escherichia coli BL21(DE3) by Michaelis-Menten based competitive inhibition assay
2
Total Activities
2
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 (CHEMBL4296323) ↗| Type | SINGLE PROTEIN |
| Organism | Plasmodium falciparum (isolate 3D7) |
Publication
Conflicting requirements of Plasmodium falciparum dihydrofolate reductase mutations conferring resistance to pyrimethamine-WR99210 combination.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 7.80 | 9.07 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 9.07 |
| CHEMBL129788 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL36 | PYRIMETHAMINE | Ki | = | 0.85 | nM | 9.07 |
| CHEMBL129788 | — | Ki | = | 292.3 | nM | 6.53 |