Assay Detail
Binding
CHEMBL4008874
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDHK1 in human PC3 cells assessed as decrease in phosphorylation of E1alpha subunit at serine 293 residue after 1 hr by ELISA
13
Total Activities
13
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
Application of Off-Rate Screening in the Identification of Novel Pan-Isoform Inhibitors of Pyruvate Dehydrogenase Kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 5.82 | 7.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1231132 | — | — | 1 | 7.39 |
| CHEMBL316388 | — | — | 1 | 7.18 |
| CHEMBL3727577 | — | — | 1 | 6.24 |
| CHEMBL3732469 | — | — | 1 | 5.76 |
| CHEMBL3715902 | — | — | 1 | 5.74 |
| CHEMBL3727843 | — | — | 1 | 5.67 |
| CHEMBL3716663 | — | — | 1 | 5.57 |
| CHEMBL4100504 | — | — | 1 | 5.56 |
| CHEMBL3717621 | — | — | 1 | 5.56 |
| CHEMBL3718319 | — | — | 1 | 5.52 |
| CHEMBL3731789 | — | — | 1 | 5.25 |
| CHEMBL3717438 | — | — | 1 | 5.24 |
| CHEMBL3732579 | — | — | 1 | 4.97 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1231132 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL316388 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL3727577 | — | IC50 | = | 573.0 | nM | 6.24 |
| CHEMBL3732469 | — | IC50 | = | 1720.0 | nM | 5.76 |
| CHEMBL3715902 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL3727843 | — | IC50 | = | 2150.0 | nM | 5.67 |
| CHEMBL3716663 | — | IC50 | = | 2680.0 | nM | 5.57 |
| CHEMBL4100504 | — | IC50 | = | 2740.0 | nM | 5.56 |
| CHEMBL3717621 | — | IC50 | = | 2780.0 | nM | 5.56 |
| CHEMBL3718319 | — | IC50 | = | 3010.0 | nM | 5.52 |
| CHEMBL3731789 | — | IC50 | = | 5650.0 | nM | 5.25 |
| CHEMBL3717438 | — | IC50 | = | 5770.0 | nM | 5.24 |
| CHEMBL3732579 | — | IC50 | = | 10600.0 | nM | 4.97 |