Assay Detail
Functional
CHEMBL825162
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro antiprotozoal activity against Trypanosoma brucei rhodesiense strain STIB900
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Trypanosoma brucei rhodesiense |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Target
Trypanosoma brucei rhodesiense (CHEMBL612348) ↗| Type | ORGANISM |
| Organism | Trypanosoma brucei rhodesiense |
Publication
Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.59 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL55 | PENTAMIDINE | 4.0 | 1 | 8.64 |
| CHEMBL24057 | FURAMIDINE | -1.0 | 1 | 8.37 |
| CHEMBL189424 | — | — | 1 | 8.14 |
| CHEMBL192282 | — | — | 1 | 7.90 |
| CHEMBL190969 | — | — | 1 | 7.77 |
| CHEMBL363001 | — | — | 1 | 7.62 |
| CHEMBL363717 | — | — | 1 | 7.39 |
| CHEMBL365264 | — | — | 1 | 7.17 |
| CHEMBL365295 | — | — | 1 | 6.89 |
| CHEMBL370274 | — | — | 1 | 6.54 |
| CHEMBL192807 | — | — | 1 | 6.09 |
| CHEMBL191313 | — | — | 1 | 6.05 |
| CHEMBL189383 | — | — | 1 | 5.60 |
| CHEMBL190394 | — | — | 1 | 5.54 |
| CHEMBL190005 | — | — | 1 | 5.10 |
| CHEMBL190681 | — | — | 1 | 4.89 |
| CHEMBL191371 | — | — | 1 | 4.67 |
| CHEMBL192722 | — | — | 1 | 4.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL55 | PENTAMIDINE | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL24057 | FURAMIDINE | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL189424 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL192282 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL190969 | — | IC50 | = | 16.9 | nM | 7.77 |
| CHEMBL363001 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL363717 | — | IC50 | = | 40.4 | nM | 7.39 |
| CHEMBL365264 | — | IC50 | = | 66.9 | nM | 7.17 |
| CHEMBL365295 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL370274 | — | IC50 | = | 292.0 | nM | 6.54 |
| CHEMBL192807 | — | IC50 | = | 814.0 | nM | 6.09 |
| CHEMBL191313 | — | IC50 | = | 894.0 | nM | 6.05 |
| CHEMBL189383 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL190394 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL190005 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL190681 | — | IC50 | = | 12900.0 | nM | 4.89 |
| CHEMBL191371 | — | IC50 | = | 21200.0 | nM | 4.67 |
| CHEMBL192722 | — | IC50 | = | 47500.0 | nM | 4.32 |