Assay Detail
Functional
CHEMBL4049097
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antitrypanosomal activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 assessed as parasite growth inhibition after 72 hrs by Alamar blue assay
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Trypanosoma brucei rhodesiense |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Target
Trypanosoma brucei rhodesiense (CHEMBL612348) ↗| Type | ORGANISM |
| Organism | Trypanosoma brucei rhodesiense |
Publication
2 H-1,2,3-Triazole-Based Dipeptidyl Nitriles: Potent, Selective, and Trypanocidal Rhodesain Inhibitors by Structure-Based Design.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 7.84 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4085387 | — | — | 1 | 9.70 |
| CHEMBL4099235 | — | — | 1 | 9.22 |
| CHEMBL4081213 | — | — | 1 | 9.00 |
| CHEMBL4093144 | — | — | 1 | 9.00 |
| CHEMBL4074099 | — | — | 1 | 8.52 |
| CHEMBL166 | MELARSOPROL | 3.0 | 1 | 8.40 |
| CHEMBL4101430 | — | — | 1 | 8.40 |
| CHEMBL4065829 | — | — | 1 | 8.40 |
| CHEMBL4065483 | — | — | 1 | 8.40 |
| CHEMBL4080286 | — | — | 1 | 8.30 |
| CHEMBL4099905 | — | — | 1 | 8.22 |
| CHEMBL4093712 | — | — | 1 | 8.22 |
| CHEMBL4095566 | — | — | 1 | 8.22 |
| CHEMBL4060895 | — | — | 1 | 8.22 |
| CHEMBL4073014 | — | — | 1 | 8.15 |
| CHEMBL4102351 | — | — | 1 | 8.10 |
| CHEMBL4078079 | — | — | 1 | 8.10 |
| CHEMBL4100863 | — | — | 1 | 8.05 |
| CHEMBL4104507 | — | — | 1 | 8.05 |
| CHEMBL55 | PENTAMIDINE | 4.0 | 1 | 8.05 |
| CHEMBL4075154 | — | — | 1 | 7.89 |
| CHEMBL4081905 | — | — | 1 | 7.72 |
| CHEMBL4096787 | — | — | 1 | 7.66 |
| CHEMBL4064430 | — | — | 1 | 7.64 |
| CHEMBL4083441 | — | — | 1 | 7.57 |
| CHEMBL4084048 | — | — | 1 | 7.57 |
| CHEMBL4094298 | — | — | 1 | 7.57 |
| CHEMBL4069564 | — | — | 1 | 7.55 |
| CHEMBL4093444 | — | — | 1 | 7.40 |
| CHEMBL265502 | SURAMIN | 3.0 | 1 | 7.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4085387 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4099235 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL4081213 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4093144 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL4074099 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL166 | MELARSOPROL | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4101430 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4065829 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4065483 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4080286 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4099905 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4093712 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4095566 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4060895 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4073014 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4102351 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4078079 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4100863 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL55 | PENTAMIDINE | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4104507 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4075154 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4081905 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4096787 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4064430 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4083441 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4084048 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4094298 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4069564 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4093444 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL265502 | SURAMIN | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL4089084 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL290960 | NIFURTIMOX | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL1631694 | FEXINIDAZOLE | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL4102031 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL830 | EFLORNITHINE | IC50 | = | 3800.0 | nM | 5.42 |