Assay Detail
Functional
CHEMBL5239934
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Antiplasmodial activity against liver stage Plasmodium berghei ANKA sporozoites expressing GFP infected in HepG2 cells pre-infected with cells for 1 hr prior to compound addition and measured after 48 hrs by flow cytometry analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium berghei |
| Cell Type | HepG2 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Novel 3-Trifluoromethyl-1,2,4-oxadiazole Analogues of Astemizole with Multi-stage Antiplasmodium Activity and <i>In Vivo</i> Efficacy in a <i>Plasmodium berghei</i> Mouse Malaria Infection Model.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.11 | 6.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5267563 | — | — | 1 | 6.68 |
| CHEMBL5273140 | — | — | 1 | 6.31 |
| CHEMBL296419 | ASTEMIZOLE | 4.0 | 1 | 6.23 |
| CHEMBL506 | PRIMAQUINE | 4.0 | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5267563 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5273140 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL296419 | ASTEMIZOLE | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL506 | PRIMAQUINE | IC50 | = | 6000.0 | nM | 5.22 |