Assay Detail
Binding
CHEMBL767697
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In vitro inhibitory activity against Pyruvate dehydrogenase kinase by primary enzymatic assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 4 — Cell-line / Tissue |
| Curated By | Autocuration |
Publication
(R)-3,3,3-Trifluoro-2-hydroxy-2-methylpropionamides are orally active inhibitors of pyruvate dehydrogenase kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.31 | 7.78 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316388 | — | — | 1 | 7.78 |
| CHEMBL84231 | — | — | 1 | 7.68 |
| CHEMBL421689 | — | — | 1 | 7.26 |
| CHEMBL93805 | — | — | 1 | 7.11 |
| CHEMBL304292 | — | — | 1 | 7.10 |
| CHEMBL82385 | — | — | 1 | 7.09 |
| CHEMBL310927 | — | — | 1 | 7.05 |
| CHEMBL94231 | — | — | 1 | 6.96 |
| CHEMBL433391 | — | — | 1 | 6.92 |
| CHEMBL93045 | — | — | 1 | 6.52 |
| CHEMBL327693 | — | — | 1 | 5.82 |
| CHEMBL329794 | — | — | 1 | 5.21 |
| CHEMBL83151 | — | — | 1 | 5.17 |
| CHEMBL92700 | — | — | 1 | 5.03 |
| CHEMBL18861 | ZD-6169 | — | 1 | 5.03 |
| CHEMBL90360 | — | — | 1 | 5.01 |
| CHEMBL92640 | — | — | 1 | 4.46 |
| CHEMBL328892 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316388 | — | IC50 | = | 16.5 | nM | 7.78 |
| CHEMBL84231 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL421689 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL93805 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL304292 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL82385 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL310927 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL94231 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL433391 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL93045 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL327693 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL329794 | — | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL83151 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL92700 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL18861 | ZD-6169 | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL90360 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL92640 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL328892 | — | IC50 | = | 200000.0 | nM | - |