Assay Detail
Functional
CHEMBL4605504
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Antimalarial activity against Plasmodium falciparum 3D70087/N9 infected in po dosed NOD-SCID IL2Rgamma null mouse assessed as reduction in parasitemia administered once daily for 4 days by flow cytometric analysis
8
Total Activities
3
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| fEC50 | 3 | - | - |
| EC50 | 3 | 7.96 | 8.22 |
| ED90 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1956285 | DSM-265 | 2.0 | 2 | 8.22 |
| CHEMBL4557830 | — | — | 3 | 7.85 |
| CHEMBL4633246 | — | — | 3 | 7.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1956285 | DSM-265 | EC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4557830 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4633246 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4633246 | — | fEC50 | = | 0.0077 | uM | - |
| CHEMBL1956285 | DSM-265 | fEC50 | = | 0.001 | uM | - |
| CHEMBL4633246 | — | ED90 | = | 50.0 | mg/kg/day | - |
| CHEMBL4557830 | — | ED90 | = | 2.6 | mg/kg/day | - |
| CHEMBL4557830 | — | fEC50 | = | 0.007 | uM | - |