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Target[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial
LigandBDBM15365
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1441710 (CHEMBL3378281)
IC50 648000±n/a nM
Citation Meng, T; Zhang, D; Xie, Z; Yu, T; Wu, S; Wyder, L; Regenass, U; Hilpert, K; Huang, M; Geng, M; Shen, J Discovery and optimization of 4,5-diarylisoxazoles as potent dual inhibitors of pyruvate dehydrogenase kinase and heat shock protein 90. J Med Chem57:9832-43 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial
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:
MRLARLLRGAALAGPGPGLRAAGFSRSFSSDSGSSPASERGVPGQVDFYARFSPSPLSMK
QFLDFGSVNACEKTSFMFLRQELPVRLANIMKEISLLPDNLLRTPSVQLVQSWYIQSLQE
LLDFKDKSAEDAKAIYDFTDTVIRIRNRHNDVIPTMAQGVIEYKESFGVDPVTSQNVQYF
LDRFYMSRISIRMLLNQHSLLFGGKGKGSPSHRKHIGSINPNCNVLEVIKDGYENARRLC
DLYYINSPELELEELNAKSPGQPIQVVYVPSHLYHMVFELFKNAMRATMEHHANRGVYPP
IQVHVTLGNEDLTVKMSDRGGGVPLRKIDRLFNYMYSTAPRPRVETSRAVPLAGFGYGLP
ISRLYAQYFQGDLKLYSLEGYGTDAVIYIKALSTDSIERLPVYNKAAWKHYNTNHEADDW
CVPSREPKDMTTFRSA
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  Blast E-value cutoff:
BDBM15365
n/a
NameBDBM15365
Synonyms:3-(2,4-Dihydroxyphenyl)-4-(4-methoxyphenyl)-5-methyl-1H-pyrazole | 4-[4-(4-methoxyphenyl)-5-methyl-1H-pyrazol-3-yl]benzene-1,3-diol | CCT018159 analog 4
TypeSmall organic molecule
Emp. Form.C17H16N2O3
Mol. Mass.296.3205
SMILESCOc1ccc(cc1)-c1c(C)[nH]nc1-c1ccc(O)cc1O
Structure
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