An EC 2.7.11.* (protein-serine/threonine kinase) inhibitor that interferes with the action of pyruvate dehydrogenase (acetyl-transferring) kinase (EC 2.7.11.2).
ChEBI ID: 176961
| Member | Definition | Class |
|---|---|---|
| azd 7545 | A sulfone that is benzene substituted by [4-(dimethylcarbamoyl)phenyl]sulfonyl, chloro and [(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino groups at positions 1, 3 and 4, respectively. It is a potent and non-ATP-competitive inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2) with IC50 of 6.4 nM and exhibits glucose-lowering activity. Also inhibits PDHK1 at higher levels (IC50 = 36.8 nM). | AZD7545 |
| Timeframe | Studies, Drugs with This Role(%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (18.18) | 29.6817 |
| 2010's | 10 (45.45) | 24.3611 |
| 2020's | 8 (36.36) | 2.80 |
| Publication Type | Studies, Drugs with this Role (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 22 (100.00%) | 84.16% |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 6.7412 | 1 | 2 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 15.0916 | 1 | 1 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 37.9083 | 1 | 1 |
| EWS/FLI fusion protein | Homo sapiens (human) | Potency | 21.0236 | 3 | 3 |
| G | Vesicular stomatitis virus | Potency | 6.7412 | 1 | 2 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 6.7412 | 1 | 2 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 6.7412 | 1 | 4 |
| Interferon beta | Homo sapiens (human) | Potency | 6.7412 | 1 | 2 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial | Homo sapiens (human) | IC50 | 0.0410 | 1 | 1 |
| [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial | Homo sapiens (human) | IC50 | 0.0800 | 1 | 1 |
| Bile salt export pump | Homo sapiens (human) | IC50 | 12.8500 | 1 | 1 |
| Chain A [Pyruvate dehydrogenase [lipoamide]] kinase isozyme 1 | Homo sapiens (human) | IC50 | 0.0870 | 1 | 1 |
| Chain A [Pyruvate dehydrogenase [lipoamide]] kinase isozyme 3 | Homo sapiens (human) | IC50 | 0.0870 | 1 | 1 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Drugs |
|---|---|---|---|---|---|
| [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial | Homo sapiens (human) | EC50 | 0.0800 | 1 | 1 |