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Target
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial
Ligand
BDBM50467739
Substrate
n/a
Meas. Tech.
ChEMBL_1796742 (CHEMBL4268859)
Kd
1290±n/a nM
Citation
 Zhang, SL; Yang, Z; Hu, X; Tam, KY Dichloroacetophenones targeting at pyruvate dehydrogenase kinase 1 with improved selectivity and antiproliferative activity: Synthesis and structure-activity relationships. Bioorg Med Chem Lett 28:3441-3445 (2018) [PubMed]  Article 
Target
Name:
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial
Synonyms:
PDHK1 | PDK1 | PDK1_HUMAN | Pyruvate dehydrogenase kinase | Pyruvate dehydrogenase kinase 1 (PDK1) | Pyruvate dehydrogenase kinase isoform 1
Type:
Protein
Mol. Mass.:
49255.23
Organism:
Homo sapiens (Human)
Description:
Q15118
Residue:
436
Sequence:
MRLARLLRGAALAGPGPGLRAAGFSRSFSSDSGSSPASERGVPGQVDFYARFSPSPLSMKQFLDFGSVNACEKTSFMFLRQELPVRLANIMKEISLLPDNLLRTPSVQLVQSWYIQSLQELLDFKDKSAEDAKAIYDFTDTVIRIRNRHNDVIPTMAQGVIEYKESFGVDPVTSQNVQYFLDRFYMSRISIRMLLNQHSLLFGGKGKGSPSHRKHIGSINPNCNVLEVIKDGYENARRLCDLYYINSPELELEELNAKSPGQPIQVVYVPSHLYHMVFELFKNAMRATMEHHANRGVYPPIQVHVTLGNEDLTVKMSDRGGGVPLRKIDRLFNYMYSTAPRPRVETSRAVPLAGFGYGLPISRLYAQYFQGDLKLYSLEGYGTDAVIYIKALSTDSIERLPVYNKAAWKHYNTNHEADDWCVPSREPKDMTTFRSA
  
Inhibitor
Name:
BDBM50467739
Synonyms:
CHEMBL4288385
Type:
Small organic molecule
Emp. Form.:
C10H9Cl2NO3
Mol. Mass.:
262.089
SMILES:
CCc1ccc(cc1[N+]([O-])=O)C(=O)C(Cl)Cl
Structure:
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