Assay Detail
Functional
CHEMBL4684531
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Antitrypanosomal activity against bloodstream form Trypanosoma brucei brucei 427 infected in 449_Grx-roGFP2 cells assessed as cell viability after 24 hrs by propidium iodide staining based flow cytometric analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Trypanosoma brucei brucei |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Novel distamycin analogues that block the cell cycle of African trypanosomes with high selectivity and potency.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 6.73 | 8.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4786260 | — | — | 1 | 8.15 |
| CHEMBL4754957 | — | — | 1 | 7.93 |
| CHEMBL380216 | DIMINAZENE DIACETURATE | — | 1 | 7.39 |
| CHEMBL265502 | SURAMIN | 3.0 | 1 | 7.11 |
| CHEMBL4791077 | — | — | 1 | 6.08 |
| CHEMBL4791631 | — | — | 1 | 5.48 |
| CHEMBL290960 | NIFURTIMOX | 4.0 | 1 | 5.00 |
| CHEMBL4763479 | — | — | 1 | - |
| CHEMBL4794700 | — | — | 1 | - |
| CHEMBL4748206 | — | — | 1 | - |
| CHEMBL4758073 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4786260 | — | EC50 | = | 7.1 | nM | 8.15 |
| CHEMBL4754957 | — | EC50 | = | 11.8 | nM | 7.93 |
| CHEMBL380216 | DIMINAZENE DIACETURATE | EC50 | = | 41.0 | nM | 7.39 |
| CHEMBL265502 | SURAMIN | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL4791077 | — | EC50 | = | 827.0 | nM | 6.08 |
| CHEMBL4791631 | — | EC50 | = | 3325.0 | nM | 5.48 |
| CHEMBL290960 | NIFURTIMOX | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4763479 | — | EC50 | - | — | - | |
| CHEMBL4794700 | — | EC50 | - | — | - | |
| CHEMBL4748206 | — | EC50 | - | — | - | |
| CHEMBL4758073 | — | EC50 | - | — | - |