Assay Detail
Binding
CHEMBL5538415
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant full-length human PDK1 (1 to 436 residues) expressed in baculovirus infected Sf9 insect cells using PDHA1 as substrate incubated for 1 hrs in presence of ATP by Kinase-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 1, mitochondrial (CHEMBL4766) ↗| 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 | 7.23 | 7.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1231132 | — | — | 1 | 7.49 |
| CHEMBL5563199 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1231132 | — | IC50 | = | 32.3 | nM | 7.49 |
| CHEMBL5563199 | — | IC50 | = | 109.3 | nM | 6.96 |