General Information of the Protein
Protein ID
PT01423
Protein Name
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial
Secondarily
Protein Name
Pyruvate dehydrogenase kinase isoform 1
Gene Name
PDK1
Secondarily
Gene Name
PDHK1
Sequence
MRLARLLRGAALAGPGPGLRAAGFSRSFSSDSGSSPASERGVPGQVDFYARFSPSPLSMKQFLDFGSVNACEKTSFMFLRQELPVRLANIMKEISLLPDNLLRTPSVQLVQSWYIQSLQELLDFKDKSAEDAKAIYDFTDTVIRIRNRHNDVIPTMAQGVIEYKESFGVDPVTSQNVQYFLDRFYMSRISIRMLLNQHSLLFGGKGKGSPSHRKHIGSINPNCNVLEVIKDGYENARRLCDLYYINSPELELEELNAKSPGQPIQVVYVPSHLYHMVFELFKNAMRATMEHHANRGVYPPIQVHVTLGNEDLTVKMSDRGGGVPLRKIDRLFNYMYSTAPRPRVETSRAVPLAGFGYGLPISRLYAQYFQGDLKLYSLEGYGTDAVIYIKALSTDSIERLPVYNKAAWKHYNTNHEADDWCVPSREPKDMTTFRSA
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
Atypical protein kinase group
>
Atypical protein kinase PDHK subfamily
Function
Kinase that plays a key role in regulation of glucose and fatty acid metabolism and homeostasis via phosphorylation of the pyruvate dehydrogenase subunits PDHA1 and PDHA2. This inhibits pyruvate dehydrogenase activity, and thereby regulates metabolite flux through the tricarboxylic acid cycle, down-regulates aerobic respiration and inhibits the formation of acetyl-coenzyme A from pyruvate. Plays an important role in cellular responses to hypoxia and is important for cell proliferation under hypoxia. Protects cells against apoptosis in response to hypoxia and oxidative stress.
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Uniprot ID
Primary ID:
Q15118

Secondarily ID:
B2R6T1
B7Z937
D3DPD8
E9PD65
Q308M4
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Ensembl ID
ENSG00000152256
HGNC ID
HGNC:8809
Subcellular Location
Mitochondrion matrix
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000048 , PC-3
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0135961
 Compound Info 
4-[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino]phenyl]sulfonyl-N,N-dimethylbenzamide
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C19H18ClF3N2O5S
  1
1
IC50 = 41 nM
 Bioactivity Info 
   TI
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CP0432059
 Compound Info 
4-[(2R,5S)-2,5-dimethyl-4-[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]piperazine-1-carbonyl]benzonitrile
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C18H20F3N3O3
  1
1
IC50 = 66 nM
 Bioactivity Info 
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CP0103729
 Compound Info 
N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxybenzamide
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C28H23ClF2N4O4
  1
1
IC50 = 573 nM
 Bioactivity Info 
   TI
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CP0103727
 Compound Info 
N-benzyl-N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-2,4-dihydroxybenzamide
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C25H20ClN3O3
  1
1
IC50 = 1720 nM
 Bioactivity Info 
   TI
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CP0081178
 Compound Info 
[(2S)-6-(2-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2-methyl-3,4-dihydro-2H-quinolin-1-yl]-(2,4-dihydroxyphenyl)methanone
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C23H19ClN4O3
  1
1
IC50 = 1820 nM
 Bioactivity Info 
   TI
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CP0081180
 Compound Info 
N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-2,4-dihydroxy-N-[[4-(pyrrolidin-1-ylmethyl)phenyl]methyl]benzamide
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C30H29ClN4O3
  1
1
IC50 = 2150 nM
 Bioactivity Info 
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CP0127155
 Compound Info 
(2,4-dihydroxyphenyl)-[(2S)-2-methyl-6-(3-methylquinolin-2-yl)-3,4-dihydro-2H-quinolin-1-yl]methanone
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C27H24N2O3
  1
1
IC50 = 2680 nM
 Bioactivity Info 
   TI
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CP0127157
 Compound Info 
[(2S)-6-(2-chloro-5-methylpyrimidin-4-yl)-2-methyl-3,4-dihydro-2H-quinolin-1-yl]-(2,4-dihydroxyphenyl)methanone
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C22H20ClN3O3
  1
1
IC50 = 2740 nM
 Bioactivity Info 
   TI
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CP0082749
 Compound Info 
[(2S)-6-(2-chlorothieno[3,2-d]pyrimidin-4-yl)-2-methyl-3,4-dihydro-2H-quinolin-1-yl]-(2,4-dihydroxyphenyl)methanone
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C23H18ClN3O3S
  1
1
IC50 = 2780 nM
 Bioactivity Info 
   TI
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CP0153755
 Compound Info 
(2S)-1-(2,4-dihydroxybenzoyl)-N,2-dimethyl-N-(quinoxalin-6-ylmethyl)-3,4-dihydro-2H-quinoline-6-carboxamide
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C28H26N4O4
  1
1
IC50 = 3010 nM
 Bioactivity Info 
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CP0113292
 Compound Info 
N-benzyl-2,4-dihydroxy-N-[4-[methyl(quinoxalin-6-ylmethyl)carbamoyl]phenyl]benzamide
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C31H26N4O4
  1
1
IC50 = 5650 nM
 Bioactivity Info 
   TI
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CP0081175
 Compound Info 
[(2R)-6-(2-chloro-5-methylpyrimidin-4-yl)-2-pyridin-3-yl-3,4-dihydro-2H-quinolin-1-yl]-(2,4-dihydroxyphenyl)methanone
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C26H21ClN4O3
  1
1
IC50 = 5770 nM
 Bioactivity Info 
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CP0128004
 Compound Info 
N-benzyl-2,4-dihydroxy-N-[4-[(4-methoxyphenyl)methyl-methylcarbamoyl]phenyl]benzamide
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C30H28N2O5
  1
1
IC50 = 10600 nM
 Bioactivity Info 
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Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0081180
 Compound Info 
N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-2,4-dihydroxy-N-[[4-(pyrrolidin-1-ylmethyl)phenyl]methyl]benzamide
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C30H29ClN4O3
  4
1 IC50 = 10 nM
2 IC50 = 101 nM
3 Kd = 78 nM
4 Ki = 37 nM
CP0103727
 Compound Info 
N-benzyl-N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-2,4-dihydroxybenzamide
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C25H20ClN3O3
  5
1 IC50 = 10 nM
2 IC50 = 72 nM
3 Kd = 16 nM
4 Kd = 60 nM
5 Ki = 67 nM
CP0113292
 Compound Info 
N-benzyl-2,4-dihydroxy-N-[4-[methyl(quinoxalin-6-ylmethyl)carbamoyl]phenyl]benzamide
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C31H26N4O4
  4
1 IC50 = 10 nM
2 IC50 = 62.7 nM
3 Kd = 1 nM
4 Ki = 26 nM
CP0103729
 Compound Info 
N-[4-(2-chloro-5-methylpyrimidin-4-yl)phenyl]-N-[[4-[[(2,2-difluoroacetyl)amino]methyl]phenyl]methyl]-2,4-dihydroxybenzamide
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C28H23ClF2N4O4
  6
1 IC50 = 10 nM
2 IC50 = 35 nM
3 IC50 = 42 nM
4 IC50 = 95.7 nM
5 Kd = 150 nM
6 Ki = 28 nM
CP0081175
 Compound Info 
[(2R)-6-(2-chloro-5-methylpyrimidin-4-yl)-2-pyridin-3-yl-3,4-dihydro-2H-quinolin-1-yl]-(2,4-dihydroxyphenyl)methanone
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C26H21ClN4O3
  2
1 IC50 = 15 nM
2 Kd = 10 nM
CP0153755
 Compound Info 
(2S)-1-(2,4-dihydroxybenzoyl)-N,2-dimethyl-N-(quinoxalin-6-ylmethyl)-3,4-dihydro-2H-quinoline-6-carboxamide
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C28H26N4O4
  3
1 IC50 = 36 nM
2 Kd = 6 nM
3 Ki = 16 nM
CP0127157
 Compound Info 
[(2S)-6-(2-chloro-5-methylpyrimidin-4-yl)-2-methyl-3,4-dihydro-2H-quinolin-1-yl]-(2,4-dihydroxyphenyl)methanone
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C22H20ClN3O3
  4
1 IC50 = 63 nM
2 Kd = 19 nM
3 Kd = 32 nM
4 Ki = 37 nM
CP0128004
 Compound Info 
N-benzyl-2,4-dihydroxy-N-[4-[(4-methoxyphenyl)methyl-methylcarbamoyl]phenyl]benzamide
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C30H28N2O5
  4
1 IC50 = 100 nM
2 IC50 = 201 nM
3 Kd = 10 nM
4 Ki = 241 nM
CP0081178
 Compound Info 
[(2S)-6-(2-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-2-methyl-3,4-dihydro-2H-quinolin-1-yl]-(2,4-dihydroxyphenyl)methanone
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C23H19ClN4O3
  3
1 IC50 = 135 nM
2 Kd = 9 nM
3 Ki = 640 nM
CP0127155
 Compound Info 
(2,4-dihydroxyphenyl)-[(2S)-2-methyl-6-(3-methylquinolin-2-yl)-3,4-dihydro-2H-quinolin-1-yl]methanone
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C27H24N2O3
  4
1 IC50 = 139 nM
2 Kd = 115 nM
3 Kd = 153 nM
4 Ki = 124 nM
CP0082749
 Compound Info 
[(2S)-6-(2-chlorothieno[3,2-d]pyrimidin-4-yl)-2-methyl-3,4-dihydro-2H-quinolin-1-yl]-(2,4-dihydroxyphenyl)methanone
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C23H18ClN3O3S
  3
1 IC50 = 198 nM
2 Kd = 10 nM
3 Ki = 467 nM
Clinical Information about the Protein
Target 1 ( Pyruvate dehydrogenase kinase 1 (PDHK1) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Patented Agent(s) 1 Patented Agent  1
1 Indolinone derivative 1
 Drug Info 
Patented
Solid tumour/cancer