Assay Detail
Binding
CHEMBL2045551
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Inhibition of Trypanosoma brucei brucei LAPT1 assessed as [3H]-pentamidine uptake after 120 secs by scintillation counting
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Trypanosoma brucei brucei |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 12 | 4.80 | 5.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL539632 | — | — | 1 | 5.66 |
| CHEMBL2041828 | — | — | 1 | 5.44 |
| CHEMBL2041805 | — | — | 1 | 5.14 |
| CHEMBL2041806 | — | — | 1 | 5.02 |
| CHEMBL2041796 | — | — | 1 | 4.72 |
| CHEMBL2041795 | — | — | 1 | 4.70 |
| CHEMBL2041807 | — | — | 1 | 4.60 |
| CHEMBL2041841 | — | — | 1 | 4.60 |
| CHEMBL601708 | — | — | 1 | 4.41 |
| CHEMBL601066 | — | — | 1 | 4.31 |
| CHEMBL55 | PENTAMIDINE | 4.0 | 1 | 4.25 |
| CHEMBL596746 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL539632 | — | Ki | = | 2200.0 | nM | 5.66 |
| CHEMBL2041828 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL2041805 | — | Ki | = | 7200.0 | nM | 5.14 |
| CHEMBL2041806 | — | Ki | = | 9500.0 | nM | 5.02 |
| CHEMBL2041796 | — | Ki | = | 19000.0 | nM | 4.72 |
| CHEMBL2041795 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL2041807 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL2041841 | — | Ki | = | 25000.0 | nM | 4.60 |
| CHEMBL601708 | — | Ki | = | 39000.0 | nM | 4.41 |
| CHEMBL601066 | — | Ki | = | 49000.0 | nM | 4.31 |
| CHEMBL55 | PENTAMIDINE | Ki | = | 56200.0 | nM | 4.25 |
| CHEMBL596746 | — | Ki | > | 250000.0 | nM | - |