General Information of the Protein
Protein ID
PT02826
Protein Name
Ketohexokinase
Secondarily
Protein Name
Hepatic fructokinase
Gene Name
KHK
Sequence
MEEKQILCVGLVVLDVISLVDKYPKEDSEIRCLSQRWQRGGNASNSCTVLSLLGAPCAFMGSMAPGHVADFLVADFRRRGVDVSQVAWQSKGDTPSSCCIINNSNGNRTIVLHDTSLPDVSATDFEKVDLTQFKWIHIEGRNASEQVKMLQRIDAHNTRQPPEQKIRVSVEVEKPREELFQLFGYGDVVFVSKDVAKHLGFQSAEEALRGLYGRVRKGAVLVCAWAEEGADALGPDGKLLHSDAFPPPRVVDTLGAGDTFNASVIFSLSQGRSVQEALRFGCQVAGKKCGLQGFDGIV
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Transferase
Function
Catalyzes the phosphorylation of the ketose sugar fructose to fructose-1-phosphate.
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Uniprot ID
Primary ID:
P50053

Secondarily ID:
Q6IBK2
Q99532
Q9BRJ3
Q9UMN1
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Ensembl ID
ENSG00000138030
HGNC ID
HGNC:6315
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: CL000063 , Hep-G2
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0441365
 Compound Info 
4-N-(2-methylsulfanylphenyl)-2-piperazin-1-ylpyrimido[5,4-d]pyrimidine-4,8-diamine
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C17H20N8S
  1
1
IC50 = 78 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0383686
 Compound Info 
8-N-(2-methoxyethyl)-4-N-(2-methylsulfanylphenyl)-2-piperazin-1-ylpyrimido[5,4-d]pyrimidine-4,8-diamine
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C20H26N8OS
  1
1
IC50 = 140 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0383687
 Compound Info 
4-N-(2-methylsulfanylphenyl)-2-piperazin-1-yl-8-N-(pyridin-2-ylmethyl)pyrimido[5,4-d]pyrimidine-4,8-diamine
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C23H25N9S
  1
1
IC50 = 270 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0492288
 Compound Info 
4-N-(2-methylsulfanylphenyl)-2-piperazin-1-yl-8-N-(1,3-thiazol-2-ylmethyl)pyrimido[5,4-d]pyrimidine-4,8-diamine
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C21H23N9S2
  1
1
IC50 = 270 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0027395
 Compound Info 
8-N-(cyclopropylmethyl)-2-(2,6-diazaspiro[3.3]heptan-2-yl)-4-N-(2-methylsulfanylphenyl)pyrimido[5,4-d]pyrimidine-4,8-diamine
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C22H26N8S
  1
1
IC50 = 360 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0019676
 Compound Info 
8-N-(cyclopropylmethyl)-4-N-(2-methylsulfanylphenyl)-2-piperazin-1-ylpyrimido[5,4-d]pyrimidine-4,8-diamine
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C21H26N8S
  1
1
IC50 = 400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0417207
 Compound Info 
2-[3-(aminomethyl)azetidin-1-yl]-8-N-(cyclopropylmethyl)-4-N-(2-methylsulfanylphenyl)pyrimido[5,4-d]pyrimidine-4,8-diamine
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C21H26N8S
  1
1
IC50 = 590 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0462208
 Compound Info 
8-N-(cyclopropylmethyl)-4-N-(2-methylphenyl)-2-piperazin-1-ylpyrimido[5,4-d]pyrimidine-4,8-diamine
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C21H26N8
  1
1
IC50 = 2400 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0221859
 Compound Info 
8-N-(cyclopropylmethyl)-2-(2,6-diazaspiro[3.4]octan-6-yl)-4-N-(2-methylsulfanylphenyl)pyrimido[5,4-d]pyrimidine-4,8-diamine
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C23H28N8S
  1
1 IC50 = 2 nM
CP0027395
 Compound Info 
8-N-(cyclopropylmethyl)-2-(2,6-diazaspiro[3.3]heptan-2-yl)-4-N-(2-methylsulfanylphenyl)pyrimido[5,4-d]pyrimidine-4,8-diamine
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C22H26N8S
  1
1 IC50 = 8 nM
CP0019676
 Compound Info 
8-N-(cyclopropylmethyl)-4-N-(2-methylsulfanylphenyl)-2-piperazin-1-ylpyrimido[5,4-d]pyrimidine-4,8-diamine
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C21H26N8S
  1
1 IC50 = 12 nM
Clinical Information about the Protein
Target 1 ( Ketohexokinase (KHK) )
Target Type Literature-reported Target