Assay Detail
Functional
CHEMBL3598911
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Antitrypanosomal activity against Trypanosoma brucei brucei 427 assessed as inhibition of parasite proliferation measured as ATP levels after 48 hrs by luciferase-based assay
16
Total Activities
14
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Trypanosoma brucei brucei |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Evaluation of histone deacetylase inhibitors (HDACi) as therapeutic leads for human African trypanosomiasis (HAT).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 14 | 5.55 | 7.54 |
| EC90 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105763 | QUISINOSTAT | 2.0 | 1 | 7.54 |
| CHEMBL257991 | — | — | 1 | 6.05 |
| CHEMBL483254 | PANOBINOSTAT | 4.0 | 2 | 5.80 |
| CHEMBL408513 | BELINOSTAT | 4.0 | 2 | 5.67 |
| CHEMBL356066 | DACINOSTAT | 2.0 | 1 | 5.58 |
| CHEMBL2018302 | TUBASTATIN A | — | 1 | 5.56 |
| CHEMBL356769 | TUBACIN | — | 1 | 5.47 |
| CHEMBL314389 | OXAMFLATIN | — | 1 | 5.39 |
| CHEMBL99 | TRICHOSTATIN | 1.0 | 1 | 5.30 |
| CHEMBL189137 | — | — | 1 | 5.18 |
| CHEMBL3597022 | — | — | 1 | 5.16 |
| CHEMBL2103863 | ABEXINOSTAT | 3.0 | 1 | 5.07 |
| CHEMBL1851943 | PRACINOSTAT | 3.0 | 1 | 5.02 |
| CHEMBL1213492 | GIVINOSTAT | 4.0 | 1 | 4.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105763 | QUISINOSTAT | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL257991 | — | EC50 | = | 892.0 | nM | 6.05 |
| CHEMBL483254 | PANOBINOSTAT | EC50 | = | 1577.0 | nM | 5.80 |
| CHEMBL408513 | BELINOSTAT | EC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL356066 | DACINOSTAT | EC50 | = | 2601.0 | nM | 5.58 |
| CHEMBL2018302 | TUBASTATIN A | EC50 | = | 2751.0 | nM | 5.56 |
| CHEMBL356769 | TUBACIN | EC50 | = | 3379.0 | nM | 5.47 |
| CHEMBL314389 | OXAMFLATIN | EC50 | = | 4063.0 | nM | 5.39 |
| CHEMBL99 | TRICHOSTATIN | EC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL189137 | — | EC50 | = | 6553.0 | nM | 5.18 |
| CHEMBL3597022 | — | EC50 | = | 6999.0 | nM | 5.16 |
| CHEMBL2103863 | ABEXINOSTAT | EC50 | = | 8607.0 | nM | 5.07 |
| CHEMBL1851943 | PRACINOSTAT | EC50 | = | 9549.0 | nM | 5.02 |
| CHEMBL1213492 | GIVINOSTAT | EC50 | = | 10909.0 | nM | 4.96 |
| CHEMBL483254 | PANOBINOSTAT | EC90 | = | 4.861 | uM | - |
| CHEMBL408513 | BELINOSTAT | EC90 | = | 4.011 | uM | - |