Assay Detail
Binding
CHEMBL748154
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Evaluated for inhibition constant (Ki mut) against A16V+S108T Mutant dihydrofolate reductase of Plasmodium falciparum
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
Development of a lead inhibitor for the A16V+S108T mutant of dihydrofolate reductase from the cycloguanil-resistant strain (T9/94) of Plasmodium falciparum.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 7.10 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL329687 | — | — | 1 | 8.00 |
| CHEMBL93974 | — | — | 1 | 7.96 |
| CHEMBL93889 | — | — | 1 | 7.31 |
| CHEMBL93893 | — | — | 1 | 7.05 |
| CHEMBL90703 | — | — | 1 | 6.97 |
| CHEMBL93888 | — | — | 1 | 6.90 |
| CHEMBL90292 | — | — | 1 | 6.78 |
| CHEMBL91345 | — | — | 1 | 6.77 |
| CHEMBL90018 | — | — | 1 | 6.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL329687 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL93974 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL93889 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL93893 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL90703 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL93888 | — | Ki | = | 127.0 | nM | 6.90 |
| CHEMBL90292 | — | Ki | = | 167.0 | nM | 6.78 |
| CHEMBL91345 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL90018 | — | Ki | = | 646.0 | nM | 6.19 |