Assay Detail
Binding
CHEMBL5357334
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Plasmodium falciparum DHFR N51I/C59R/S108N/I164L quadruple mutant 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 | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 8.44 | 9.27 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3040038 | — | — | 1 | 9.27 |
| CHEMBL5415214 | — | — | 1 | 9.24 |
| CHEMBL5397904 | — | — | 1 | 9.09 |
| CHEMBL5421199 | — | — | 1 | 8.98 |
| CHEMBL5417784 | — | — | 1 | 8.71 |
| CHEMBL5406769 | — | — | 1 | 8.68 |
| CHEMBL5432011 | — | — | 1 | 8.48 |
| CHEMBL5440218 | — | — | 1 | 7.38 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | 7.31 |
| CHEMBL5404134 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3040038 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL5415214 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL5397904 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL5421199 | — | Ki | = | 1.04 | nM | 8.98 |
| CHEMBL5417784 | — | Ki | = | 1.96 | nM | 8.71 |
| CHEMBL5406769 | — | Ki | = | 2.11 | nM | 8.68 |
| CHEMBL5432011 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL5440218 | — | Ki | = | 41.73 | nM | 7.38 |
| CHEMBL22 | TRIMETHOPRIM | Ki | = | 49.07 | nM | 7.31 |
| CHEMBL5404134 | — | Ki | = | 61.12 | nM | 7.21 |