Reaction Details |
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Target | [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial |
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Ligand | BDBM227594 |
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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 | 8.0e+2±n/a 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 2, mitochondrial |
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Name: | [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial |
Synonyms: | PDHK2 | PDK2 | PDK2_HUMAN | Pyruvate dehydrogenase kinase 2 (PDK2) | Pyruvate dehydrogenase kinase isoenzyme 1 (PDK2) |
Type: | Enzyme |
Mol. Mass.: | 46153.78 |
Organism: | Homo sapiens (Human) |
Description: | Q15119 |
Residue: | 407 |
Sequence: | MRWVWALLKNASLAGAPKYIEHFSKFSPSPLSMKQFLDFGSSNACEKTSFTFLRQELPVR
LANIMKEINLLPDRVLSTPSVQLVQSWYVQSLLDIMEFLDKDPEDHRTLSQFTDALVTIR
NRHNDVVPTMAQGVLEYKDTYGDDPVSNQNIQYFLDRFYLSRISIRMLINQHTLIFDGST
NPAHPKHIGSIDPNCNVSEVVKDAYDMAKLLCDKYYMASPDLEIQEINAANSKQPIHMVY
VPSHLYHMLFELFKNAMRATVESHESSLILPPIKVMVALGEEDLSIKMSDRGGGVPLRKI
ERLFSYMYSTAPTPQPGTGGTPLAGFGYGLPISRLYAKYFQGDLQLFSMEGFGTDAVIYL
KALSTDSVERLPVYNKSAWRHYQTIQEAGDWCVPSTEPKNTSTYRVS
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BDBM227594 |
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n/a |
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Name | BDBM227594 |
Synonyms: | PS10 |
Type | Small organic molecule |
Emp. Form. | C14H13NO6S |
Mol. Mass. | 323.321 |
SMILES | Oc1ccc(c(O)c1)S(=O)(=O)N1Cc2cc(O)cc(O)c2C1 |
Structure |
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