Assay Detail
Binding
CHEMBL5538418
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged recombinant human full length PDK3 (1 to 406 residues) expressed in baculovirus infected Sf9 cells using PDHA1 as substrate incubated for 1 hrs in presence of ATP by ADP-Glo luminescence assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 3, mitochondrial (CHEMBL3893) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Targeting the pyruvate dehydrogenase complex/pyruvate dehydrogenase kinase (PDC/PDK) axis to discover potent PDK inhibitors through structure-based virtual screening and pharmacological evaluation.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 6.63 | 6.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1231132 | — | — | 1 | 6.92 |
| CHEMBL5563199 | — | — | 1 | 6.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1231132 | — | IC50 | = | 120.5 | nM | 6.92 |
| CHEMBL5563199 | — | IC50 | = | 458.7 | nM | 6.34 |