Assay Detail
Functional
CHEMBL5533716
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Antitrypanosomal activity against bloodstream forms of Trypanosoma brucei gambiense 130R assessed as growth inhibition incubated for 68 hrs followed by treated with resazurin 4 to 6 hrs by resazurin based fluorescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Trypanosoma brucei gambiense |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Target
Trypanosoma brucei gambiense (CHEMBL613768) ↗| Type | ORGANISM |
| Organism | Trypanosoma brucei gambiense |
Publication
Discovery of an orally active nitrothiophene-based antitrypanosomal agent.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 6.90 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL166 | MELARSOPROL | 3.0 | 1 | 8.00 |
| CHEMBL5573874 | — | — | 1 | 7.52 |
| CHEMBL5573369 | — | — | 1 | 7.22 |
| CHEMBL5571920 | — | — | 1 | 7.22 |
| CHEMBL4642933 | — | — | 1 | 7.16 |
| CHEMBL5579771 | — | — | 1 | 6.89 |
| CHEMBL5564036 | — | — | 1 | 6.70 |
| CHEMBL5564546 | — | — | 1 | 6.60 |
| CHEMBL5571750 | — | — | 1 | 6.50 |
| CHEMBL5572856 | — | — | 1 | 6.33 |
| CHEMBL5563629 | — | — | 1 | 5.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL166 | MELARSOPROL | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5573874 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5573369 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5571920 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL4642933 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5579771 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5564036 | — | EC50 | = | 200.0 | nM | 6.70 |
| CHEMBL5564546 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5571750 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5572856 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5563629 | — | EC50 | = | 1880.0 | nM | 5.73 |