Reaction Details |
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Target | [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial |
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Ligand | BDBM227593 |
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Substrate/Competitor | n/a |
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Meas. Tech. | PDK Inhibition Assay |
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pH | 7.5±0 |
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Temperature | 298.15±0 K |
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IC50 | 1.10e+3± 2.1e+2 nM |
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Citation | Tso, SC; Qi, X; Gui, WJ; Wu, CY; Chuang, JL; Wernstedt-Asterholm, I; Morlock, LK; Owens, KR; Scherer, PE; Williams, NS; Tambar, UK; Wynn, RM; Chuang, DT Structure-guided development of specific pyruvate dehydrogenase kinase inhibitors targeting the ATP-binding pocket. J Biol Chem289:4432-43 (2014) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial |
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Name: | [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 4, mitochondrial |
Synonyms: | PDHK4 | PDK4 | PDK4_HUMAN | Pyruvate dehydrogenase kinase | Pyruvate dehydrogenase kinase 4 (PDK4) | Pyruvate dehydrogenase kinase isoform 4 |
Type: | Enzyme |
Mol. Mass.: | 46469.71 |
Organism: | Homo sapiens (Human) |
Description: | Q16654 |
Residue: | 411 |
Sequence: | MKAARFVLRSAGSLNGAGLVPREVEHFSRYSPSPLSMKQLLDFGSENACERTSFAFLRQE
LPVRLANILKEIDILPTQLVNTSSVQLVKSWYIQSLMDLVEFHEKSPDDQKALSDFVDTL
IKVRNRHHNVVPTMAQGIIEYKDACTVDPVTNQNLQYFLDRFYMNRISTRMLMNQHILIF
SDSQTGNPSHIGSIDPNCDVVAVVQDAFECSRMLCDQYYLSSPELKLTQVNGKFPDQPIH
IVYVPSHLHHMLFELFKNAMRATVEHQENQPSLTPIEVIVVLGKEDLTIKISDRGGGVPL
RIIDRLFSYTYSTAPTPVMDNSRNAPLAGFGYGLPISRLYAKYFQGDLNLYSLSGYGTDA
IIYLKALSSESIEKLPVFNKSAFKHYQMSSEADDWCIPSREPKNLAKEVAM
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BDBM227593 |
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n/a |
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Name | BDBM227593 |
Synonyms: | PS8 |
Type | Small organic molecule |
Emp. Form. | C14H13NO5S |
Mol. Mass. | 307.322 |
SMILES | Oc1ccc2CN(Cc2c1)S(=O)(=O)c1ccc(O)cc1O |
Structure |
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