Reaction Details
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[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 2, mitochondrial
Ligand
BDBM227594
Substrate
n/a
Meas. Tech.
ChEMBL_1649543 (CHEMBL3998677)
IC50
456±n/a nM
Citation
Tso, SC; Lou, M; Wu, CY; Gui, WJ; Chuang, JL; Morlock, LK; Williams, NS; Wynn, RM; Qi, X; Chuang, DT Development of Dihydroxyphenyl Sulfonylisoindoline Derivatives as Liver-Targeting Pyruvate Dehydrogenase Kinase Inhibitors. J Med Chem 60:1142-1150 (2017) [PubMed] Article More Info.:
Target
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:
MRWVWALLKNASLAGAPKYIEHFSKFSPSPLSMKQFLDFGSSNACEKTSFTFLRQELPVRLANIMKEINLLPDRVLSTPSVQLVQSWYVQSLLDIMEFLDKDPEDHRTLSQFTDALVTIRNRHNDVVPTMAQGVLEYKDTYGDDPVSNQNIQYFLDRFYLSRISIRMLINQHTLIFDGSTNPAHPKHIGSIDPNCNVSEVVKDAYDMAKLLCDKYYMASPDLEIQEINAANSKQPIHMVYVPSHLYHMLFELFKNAMRATVESHESSLILPPIKVMVALGEEDLSIKMSDRGGGVPLRKIERLFSYMYSTAPTPQPGTGGTPLAGFGYGLPISRLYAKYFQGDLQLFSMEGFGTDAVIYLKALSTDSVERLPVYNKSAWRHYQTIQEAGDWCVPSTEPKNTSTYRVS
Inhibitor
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:
