Assay Detail
Binding
CHEMBL4413205
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His-tagged PDK3 expressed in Escherichia coli using PDH E1 as substrate measured after 30 mins by Kinase-Glo luminescence assay
4
Total Activities
4
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 3, mitochondrial (CHEMBL3893) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
High-throughput screening of novel pyruvate dehydrogenase kinases inhibitors and biological evaluation of their in vitro and in vivo antiproliferative activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.66 | 7.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3727577 | — | — | 1 | 7.00 |
| CHEMBL4434895 | — | — | 1 | 5.31 |
| CHEMBL4476534 | — | — | 1 | 5.24 |
| CHEMBL4434775 | — | — | 1 | 5.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3727577 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4434895 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4476534 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4434775 | — | IC50 | = | 8300.0 | nM | 5.08 |