Assay Detail
Binding
CHEMBL4403262
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PDHK4 (unknown origin) by radiometric biochemical kinase assay
31
Total Activities
31
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 4, mitochondrial (CHEMBL4141) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of Novel Resorcinol Amide Derivatives as Potent and Specific Pyruvate Dehydrogenase Kinase (PDHK) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.66 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4591977 | — | — | 1 | 8.30 |
| CHEMBL4551410 | — | — | 1 | 8.10 |
| CHEMBL4519504 | — | — | 1 | 7.96 |
| CHEMBL4575355 | — | — | 1 | 7.89 |
| CHEMBL4461160 | — | — | 1 | 7.70 |
| CHEMBL3727577 | — | — | 1 | 7.68 |
| CHEMBL4540811 | — | — | 1 | 7.47 |
| CHEMBL4558837 | — | — | 1 | 7.28 |
| CHEMBL4558944 | — | — | 1 | 7.28 |
| CHEMBL3729572 | — | — | 1 | 7.18 |
| CHEMBL4570690 | — | — | 1 | 7.16 |
| CHEMBL4587341 | — | — | 1 | 7.09 |
| CHEMBL4452536 | — | — | 1 | 7.06 |
| CHEMBL4513465 | — | — | 1 | 7.05 |
| CHEMBL4539698 | — | — | 1 | 7.00 |
| CHEMBL4534284 | — | — | 1 | 6.77 |
| CHEMBL4533214 | — | — | 1 | 6.63 |
| CHEMBL4470843 | — | — | 1 | 6.56 |
| CHEMBL4470078 | — | — | 1 | 6.51 |
| CHEMBL4434941 | — | — | 1 | 6.41 |
| CHEMBL4561336 | — | — | 1 | 6.40 |
| CHEMBL4579724 | — | — | 1 | 6.11 |
| CHEMBL4572038 | — | — | 1 | 5.74 |
| CHEMBL4462727 | — | — | 1 | 5.70 |
| CHEMBL4589513 | — | — | 1 | 5.33 |
| CHEMBL4543303 | — | — | 1 | 5.27 |
| CHEMBL4453146 | — | — | 1 | 5.24 |
| CHEMBL4577025 | — | — | 1 | 5.11 |
| CHEMBL4459434 | — | — | 1 | 4.91 |
| CHEMBL4470063 | — | — | 1 | 4.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4591977 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4551410 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4519504 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4575355 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4461160 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3727577 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4540811 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4558837 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4558944 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3729572 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4570690 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4587341 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL4452536 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4513465 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4539698 | — | IC50 | = | 99.0 | nM | 7.00 |
| CHEMBL4534284 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL4533214 | — | IC50 | = | 234.0 | nM | 6.63 |
| CHEMBL4470843 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL4470078 | — | IC50 | = | 311.0 | nM | 6.51 |
| CHEMBL4434941 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4561336 | — | IC50 | = | 399.0 | nM | 6.40 |
| CHEMBL4579724 | — | IC50 | = | 775.0 | nM | 6.11 |
| CHEMBL4572038 | — | IC50 | = | 1810.0 | nM | 5.74 |
| CHEMBL4462727 | — | IC50 | = | 1980.0 | nM | 5.70 |
| CHEMBL4589513 | — | IC50 | = | 4670.0 | nM | 5.33 |
| CHEMBL4543303 | — | IC50 | = | 5330.0 | nM | 5.27 |
| CHEMBL4453146 | — | IC50 | = | 5793.0 | nM | 5.24 |
| CHEMBL4577025 | — | IC50 | = | 7840.0 | nM | 5.11 |
| CHEMBL4459434 | — | IC50 | = | 12260.0 | nM | 4.91 |
| CHEMBL4470063 | — | IC50 | = | 14750.0 | nM | 4.83 |
| CHEMBL4444315 | — | IC50 | > | 10000.0 | nM | - |