Assay Detail
Functional
CHEMBL3614901
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Trypanocidal activity against diminazene/pentamidine/melaminophenyl arsenicals-resistant bloodstream form of Trypanosoma brucei brucei B48 trypomastigotes after 70 hrs by Alamar Blue assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Trypanosoma brucei brucei |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Lowering the pKa of a bisimidazoline lead with halogen atoms results in improved activity and selectivity against Trypanosoma brucei in vitro.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 5.96 | 6.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3613560 | — | — | 1 | 6.44 |
| CHEMBL55 | PENTAMIDINE | 4.0 | 1 | 6.26 |
| CHEMBL3613557 | — | — | 1 | 6.19 |
| CHEMBL3613555 | — | — | 1 | 6.16 |
| CHEMBL35241 | DIMINAZENE | 2.0 | 1 | 6.11 |
| CHEMBL3613561 | — | — | 1 | 6.10 |
| CHEMBL3613554 | — | — | 1 | 6.08 |
| CHEMBL534524 | — | — | 1 | 6.06 |
| CHEMBL3613559 | — | — | 1 | 5.67 |
| CHEMBL3613556 | — | — | 1 | 5.61 |
| CHEMBL3613562 | — | — | 1 | 5.49 |
| CHEMBL3613558 | — | — | 1 | 5.36 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3613560 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL55 | PENTAMIDINE | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3613557 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL3613555 | — | EC50 | = | 690.0 | nM | 6.16 |
| CHEMBL35241 | DIMINAZENE | EC50 | = | 780.0 | nM | 6.11 |
| CHEMBL3613561 | — | EC50 | = | 790.0 | nM | 6.10 |
| CHEMBL3613554 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL534524 | — | EC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3613559 | — | EC50 | = | 2160.0 | nM | 5.67 |
| CHEMBL3613556 | — | EC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL3613562 | — | EC50 | = | 3230.0 | nM | 5.49 |
| CHEMBL3613558 | — | EC50 | = | 4350.0 | nM | 5.36 |