Target
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial
Ligand
BDBM467115
Substrate
n/a
Meas. Tech.
Inhibitory Action of PDHK1 Activity In Vitro
IC50
<3.00±n/a nM
Citation
 Maeba, TSuzawa, KKotoku, MMasuo, RMotoda, DYamaoka, N Nitrogen-containing heterocyclic amide compound and pharmaceutical use thereof US Patent  US10800784 Publication Date 10/13/2020 
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:
BDBM467115
Synonyms:
US10800784, Example 101
Type:
Small organic molecule
Emp. Form.:
C18H17F3N4O3
Mol. Mass.:
394.3478
SMILES:
C[C@H]1CN(Cc2onc(c12)[C@@](C)(O)C(F)(F)F)C(=O)c1n[nH]c2ccccc12 |r|
Structure:
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