Assay Detail
Functional
CHEMBL3383482
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Trypanocidal activity against bloodstream forms of Trypanosoma brucei brucei Lister 427 clone 221a overexpressing type I nitroreductase assessed as inhibition of proliferation after 3 days by resazurin assay in presence of tetracycline
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Trypanosoma brucei brucei |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Novel nitro(triazole/imidazole)-based heteroarylamides/sulfonamides as potential antitrypanosomal agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.58 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL166 | MELARSOPROL | 3.0 | 1 | 8.47 |
| CHEMBL3358486 | — | — | 1 | 7.16 |
| CHEMBL290960 | NIFURTIMOX | 4.0 | 1 | 6.89 |
| CHEMBL3358487 | — | — | 1 | 6.80 |
| CHEMBL3358475 | — | — | 1 | 6.72 |
| CHEMBL3358473 | — | — | 1 | 6.66 |
| CHEMBL2070694 | — | — | 1 | 6.64 |
| CHEMBL3358479 | — | — | 1 | 6.54 |
| CHEMBL3358480 | — | — | 1 | 6.51 |
| CHEMBL3358478 | — | — | 1 | 6.48 |
| CHEMBL3358488 | — | — | 1 | 6.44 |
| CHEMBL3358474 | — | — | 1 | 6.28 |
| CHEMBL3358472 | — | — | 1 | 6.26 |
| CHEMBL110 | BENZNIDAZOLE | 4.0 | 1 | 5.66 |
| CHEMBL3358485 | — | — | 1 | 5.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL166 | MELARSOPROL | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3358486 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL290960 | NIFURTIMOX | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3358487 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL3358475 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL3358473 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2070694 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3358479 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL3358480 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3358478 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3358488 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL3358474 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL3358472 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL110 | BENZNIDAZOLE | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3358485 | — | IC50 | = | 5660.0 | nM | 5.25 |