Assay Detail
Binding
CHEMBL5372399
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDK1 (unknown origin) incubated for 30 mins in presence of ATP by kinase glo luminescent kinase assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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
Reprogramming Energy Metabolism with Synthesized PDK Inhibitors Based on Dichloroacetate Derivatives and Targeted Delivery Systems for Enhanced Cancer Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 20 | 5.85 | 7.21 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3727577 | — | — | 1 | 7.21 |
| CHEMBL5424355 | — | — | 1 | 7.17 |
| CHEMBL5422377 | — | — | 1 | 6.72 |
| CHEMBL5402490 | — | — | 1 | 6.21 |
| CHEMBL5425301 | — | — | 1 | 6.19 |
| CHEMBL5417465 | — | — | 1 | 6.03 |
| CHEMBL5436563 | — | — | 1 | 6.00 |
| CHEMBL5439850 | — | — | 1 | 5.92 |
| CHEMBL5405743 | — | — | 1 | 5.89 |
| CHEMBL5419996 | — | — | 1 | 5.80 |
| CHEMBL5394529 | — | — | 1 | 5.72 |
| CHEMBL5419257 | — | — | 1 | 5.72 |
| CHEMBL5423077 | — | — | 1 | 5.58 |
| CHEMBL5423379 | — | — | 1 | 5.54 |
| CHEMBL5423915 | — | — | 1 | 5.50 |
| CHEMBL5403973 | — | — | 1 | 5.33 |
| CHEMBL5440159 | — | — | 1 | 5.02 |
| CHEMBL3290761 | — | — | 1 | 4.92 |
| CHEMBL5289763 | — | — | 1 | 4.77 |
| CHEMBL13960 | DICHLOROACETIC ACID | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3727577 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL5424355 | — | EC50 | = | 68.0 | nM | 7.17 |
| CHEMBL5422377 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL5402490 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5425301 | — | EC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5417465 | — | EC50 | = | 930.0 | nM | 6.03 |
| CHEMBL5436563 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5439850 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5405743 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5419996 | — | EC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5394529 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5419257 | — | EC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL5423077 | — | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL5423379 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL5423915 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5403973 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL5440159 | — | EC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL3290761 | — | EC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL5289763 | — | EC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL13960 | DICHLOROACETIC ACID | EC50 | > | 50000.0 | nM | - |