Assay Detail
Functional
CHEMBL5586211
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Antimalarial activity against PYR-sensitive Plasmodium falciparum TM4/8.2 expressing wild type DHFR incubated for 24 hrs by [3H]-hypoxanthine incorporation assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Plasmodium falciparum |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Novel flexible biphenyl <i>Pf</i>DHFR inhibitors with improved antimalarial activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.33 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5598041 | — | — | 1 | 8.70 |
| CHEMBL5597280 | — | — | 1 | 7.72 |
| CHEMBL5596188 | — | — | 1 | 7.58 |
| CHEMBL5597152 | — | — | 1 | 7.54 |
| CHEMBL5598010 | — | — | 1 | 7.31 |
| CHEMBL5590041 | — | — | 1 | 6.65 |
| CHEMBL5597998 | — | — | 1 | 6.58 |
| CHEMBL5597854 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5598041 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5597280 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5596188 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5597152 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5598010 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5590041 | — | IC50 | = | 225.0 | nM | 6.65 |
| CHEMBL5597998 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5597854 | — | IC50 | = | 260.0 | nM | 6.58 |