Assay Detail
Binding
CHEMBL811759
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Binding affinity was evaluated as inhibition of mutant (C59R + S108N) Plasmodium falciparum DHFR-TS.
4
Total Activities
4
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
Rational drug design approach for overcoming drug resistance: application to pyrimethamine resistance in malaria.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 7.85 | 8.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL278847 | — | — | 1 | 8.62 |
| CHEMBL29773 | — | — | 1 | 7.85 |
| CHEMBL2364573 | NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE | — | 1 | 7.84 |
| CHEMBL747 | CYCLOGUANIL | 2.0 | 1 | 7.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL278847 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL29773 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2364573 | NICOTINAMIDE ADENINE DINUCLEOTIDE PHOSPHATE | Ki | = | 14.5 | nM | 7.84 |
| CHEMBL747 | CYCLOGUANIL | Ki | = | 82.1 | nM | 7.09 |