Assay Detail
Functional
CHEMBL3383481
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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 absence 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 | 5.61 | 8.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL166 | MELARSOPROL | 3.0 | 1 | 8.47 |
| CHEMBL3358475 | — | — | 1 | 6.34 |
| CHEMBL3358487 | — | — | 1 | 6.32 |
| CHEMBL3358486 | — | — | 1 | 5.89 |
| CHEMBL3358488 | — | — | 1 | 5.86 |
| CHEMBL290960 | NIFURTIMOX | 4.0 | 1 | 5.77 |
| CHEMBL3358480 | — | — | 1 | 5.60 |
| CHEMBL3358473 | — | — | 1 | 5.37 |
| CHEMBL2070694 | — | — | 1 | 5.36 |
| CHEMBL3358478 | — | — | 1 | 5.20 |
| CHEMBL3358485 | — | — | 1 | 5.16 |
| CHEMBL3358474 | — | — | 1 | 4.77 |
| CHEMBL3358472 | — | — | 1 | 4.67 |
| CHEMBL3358479 | — | — | 1 | 4.67 |
| CHEMBL110 | BENZNIDAZOLE | 4.0 | 1 | 4.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL166 | MELARSOPROL | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL3358475 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL3358487 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3358486 | — | IC50 | = | 1290.0 | nM | 5.89 |
| CHEMBL3358488 | — | IC50 | = | 1390.0 | nM | 5.86 |
| CHEMBL290960 | NIFURTIMOX | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL3358480 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL3358473 | — | IC50 | = | 4250.0 | nM | 5.37 |
| CHEMBL2070694 | — | IC50 | = | 4340.0 | nM | 5.36 |
| CHEMBL3358478 | — | IC50 | = | 6340.0 | nM | 5.20 |
| CHEMBL3358485 | — | IC50 | = | 6990.0 | nM | 5.16 |
| CHEMBL3358474 | — | IC50 | = | 16960.0 | nM | 4.77 |
| CHEMBL3358472 | — | IC50 | = | 21580.0 | nM | 4.67 |
| CHEMBL3358479 | — | IC50 | = | 21180.0 | nM | 4.67 |
| CHEMBL110 | BENZNIDAZOLE | IC50 | = | 21800.0 | nM | 4.66 |