Assay Detail
Functional
CHEMBL3614900
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Trypanocidal activity against wild type bloodstream form of Trypanosoma brucei brucei s427 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 | 6.54 | 9.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL55 | PENTAMIDINE | 4.0 | 1 | 9.96 |
| CHEMBL35241 | DIMINAZENE | 2.0 | 1 | 7.92 |
| CHEMBL3613560 | — | — | 1 | 6.66 |
| CHEMBL3613557 | — | — | 1 | 6.33 |
| CHEMBL3613555 | — | — | 1 | 6.28 |
| CHEMBL3613561 | — | — | 1 | 6.24 |
| CHEMBL534524 | — | — | 1 | 6.08 |
| CHEMBL3613554 | — | — | 1 | 6.01 |
| CHEMBL3613562 | — | — | 1 | 5.98 |
| CHEMBL3613556 | — | — | 1 | 5.88 |
| CHEMBL3613559 | — | — | 1 | 5.80 |
| CHEMBL3613558 | — | — | 1 | 5.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL55 | PENTAMIDINE | EC50 | = | 0.11 | nM | 9.96 |
| CHEMBL35241 | DIMINAZENE | EC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3613560 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3613557 | — | EC50 | = | 470.0 | nM | 6.33 |
| CHEMBL3613555 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3613561 | — | EC50 | = | 580.0 | nM | 6.24 |
| CHEMBL534524 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL3613554 | — | EC50 | = | 970.0 | nM | 6.01 |
| CHEMBL3613562 | — | EC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL3613556 | — | EC50 | = | 1320.0 | nM | 5.88 |
| CHEMBL3613559 | — | EC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL3613558 | — | EC50 | = | 4220.0 | nM | 5.38 |