Assay Detail
Functional
CHEMBL767695
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In vivo inhibion of pyruvate dehydrogenase kinase, increased oxidation of lactate
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| 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 |
|---|---|---|---|
| EC50 | 8 | 5.86 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL316388 | — | — | 1 | 7.24 |
| CHEMBL304292 | — | — | 1 | 6.60 |
| CHEMBL327693 | — | — | 1 | 6.23 |
| CHEMBL310927 | — | — | 1 | 5.85 |
| CHEMBL93045 | — | — | 1 | 5.27 |
| CHEMBL18861 | ZD-6169 | — | 1 | 5.08 |
| CHEMBL421689 | — | — | 1 | 4.77 |
| CHEMBL306823 | SODIUM DICHLOROACETATE | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL316388 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL304292 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL327693 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL310927 | — | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL93045 | — | EC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL18861 | ZD-6169 | EC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL421689 | — | EC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL306823 | SODIUM DICHLOROACETATE | EC50 | = | 130000.0 | nM | - |