General Information of the Protein
Protein ID
PT01056
Protein Name
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
Secondarily
Protein Name
Minibrain-related kinase
Mirk protein kinase
Gene Name
DYRK1B
Secondarily
Gene Name
MIRK
Sequence
MAVPPGHGPFSGFPGPQEHTQVLPDVRLLPRRLPLAFRDATSAPLRKLSVDLIKTYKHINEVYYAKKKRRAQQAPPQDSSNKKEKKVLNHGYDDDNHDYIVRSGERWLERYEIDSLIGKGSFGQVVKAYDHQTQELVAIKIIKNKKAFLNQAQIELRLLELMNQHDTEMKYYIVHLKRHFMFRNHLCLVFELLSYNLYDLLRNTHFRGVSLNLTRKLAQQLCTALLFLATPELSIIHCDLKPENILLCNPKRSAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGTPYDLAIDMWSLGCILVEMHTGEPLFSGSNEVDQMNRIVEVLGIPPAAMLDQAPKARKYFERLPGGGWTLRRTKELRKDYQGPGTRRLQEVLGVQTGGPGGRRAGEPGHSPADYLRFQDLVLRMLEYEPAARISPLGALQHGFFRRTADEATNTGPAGSSASTSPAPLDTCPSSSTASSISSSGGSSGSSSDNRTYRYSNRYCGGPGPPITDCEMNSPQVPPSQPLRPWAGGDVPHKTHQAPASASSLPGTGAQLPPQPRYLGRPPSPTSPPPPELMDVSLVGGPADCSPPHPAPAPQHPAASALRTRMTGGRPPLPPPDDPATLGPHLGLRGVPQSTAASS
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
CMGC protein kinase group
>
CMGC protein kinase DYRK family
>
CMGC protein kinase Dyrk1 subfamily
Function
Dual-specificity kinase which possesses both serine/threonine and tyrosine kinase activities. Plays an essential role in ribosomal DNA (rDNA) double-strand break repair and rDNA copy number maintenance (PubMed:33469661). During DNA damage, mediates transcription silencing in part via phosphorylating and enforcing DSB accumulation of the histone methyltransferase EHMT2 (PubMed:32611815). Enhances the transcriptional activity of TCF1/HNF1A and FOXO1. Inhibits epithelial cell migration. Mediates colon carcinoma cell survival in mitogen-poor environments. Inhibits the SHH and WNT1 pathways, thereby enhancing adipogenesis. In addition, promotes expression of the gluconeogenic enzyme glucose-6-phosphatase catalytic subunit 1 (G6PC1).
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Uniprot ID
Primary ID:
Q9Y463

Secondarily ID:
O75258
O75788
O75789
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Ensembl ID
ENSG00000105204
HGNC ID
HGNC:3092
Subcellular Location
Nucleus
Nucleus
Nucleolus
Chromosome
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: CL000109 , COS-1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0073979
 Compound Info 
N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(1-methylpyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine
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C24H27N7O
  1
1
IC50 = 42 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0390051
 Compound Info 
N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(7-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine
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C24H27N7O
  1
1
IC50 = 83 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0088578
 Compound Info 
N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine
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C23H25N7O
  1
1
IC50 = 85 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0072052
 Compound Info 
4-(1,7-dimethylpyrrolo[2,3-c]pyridin-3-yl)-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
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C25H29N7O
  1
1
IC50 = 168 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0072037
 Compound Info 
3-[2-[(E)-2-phenylethenyl]pyrimidin-4-yl]-1H-pyrrolo[2,3-c]pyridine
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C19H14N4
  1
1
IC50 = 192 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0380676
 Compound Info 
1-benzyl-3-(2-methylpyrimidin-4-yl)pyrrolo[2,3-c]pyridine
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C19H16N4
  1
1
IC50 = 194 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0388934
 Compound Info 
N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-6-(1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-4-amine
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C23H25N7O
  1
1
IC50 = 282 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0310598
 Compound Info 
3-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyrrolo[2,3-c]pyridine
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C14H10N4
  1
1
IC50 = 378 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0316807
 Compound Info 
N-[4-(4-methylpiperazin-1-yl)phenyl]-6-(1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-4-amine
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C22H23N7
  1
1
IC50 = 453 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0283349
 Compound Info 
1-methyl-3-[2-(4-methylsulfonylphenyl)pyrimidin-4-yl]pyrrolo[2,3-c]pyridine
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C19H16N4O2S
  1
1
IC50 = 810 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0084894
 Compound Info 
3-[2-(4-methylsulfonylphenyl)pyrimidin-4-yl]-1H-pyrrolo[2,3-c]pyridine
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C18H14N4O2S
  1
1
IC50 = 898 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0072038
 Compound Info 
7-methyl-3-[2-(4-methylsulfonylphenyl)pyrimidin-4-yl]-1H-pyrrolo[2,3-c]pyridine
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C19H16N4O2S
  1
1
IC50 = 2118 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0073977
 Compound Info 
3-(2-methylpyrimidin-4-yl)-1H-pyrrolo[2,3-c]pyridine
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C12H10N4
  1
1
IC50 = 3069 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
CP0072040
 Compound Info 
6-(1H-indol-3-yl)-N-[4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-4-amine
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C23H24N6
  1
1
IC50 = 9965 nM
 Bioactivity Info 
   TI
   LI
   LO
   TS
Cell Line ID: CL000025 , HEK-293T
 Cell Line Info 
Cell Line ID: CL000012 , Sf21
 Cell Line Info 
Cell Line ID: CL000013 , Sf9
 Cell Line Info 
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0388934
 Compound Info 
N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-6-(1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-4-amine
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C23H25N7O
  1
1 IC50 = 1 nM
CP0316807
 Compound Info 
N-[4-(4-methylpiperazin-1-yl)phenyl]-6-(1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-4-amine
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C22H23N7
  1
1 IC50 = 2 nM
CP0073979
 Compound Info 
N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(1-methylpyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine
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C24H27N7O
  2
1 IC50 = 3 nM
2 Ki = 11.2 nM
CP0310598
 Compound Info 
3-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyrrolo[2,3-c]pyridine
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C14H10N4
  1
1 IC50 = 3 nM
CP0088578
 Compound Info 
N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine
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C23H25N7O
  1
1 IC50 = 4 nM
CP0390051
 Compound Info 
N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]-4-(7-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine
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C24H27N7O
  1
1 IC50 = 5 nM
CP0072037
 Compound Info 
3-[2-[(E)-2-phenylethenyl]pyrimidin-4-yl]-1H-pyrrolo[2,3-c]pyridine
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C19H14N4
  1
1 IC50 = 7 nM
CP0380676
 Compound Info 
1-benzyl-3-(2-methylpyrimidin-4-yl)pyrrolo[2,3-c]pyridine
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C19H16N4
  1
1 IC50 = 7 nM
CP0072052
 Compound Info 
4-(1,7-dimethylpyrrolo[2,3-c]pyridin-3-yl)-N-[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-2-amine
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C25H29N7O
  1
1 IC50 = 9 nM
CP0283349
 Compound Info 
1-methyl-3-[2-(4-methylsulfonylphenyl)pyrimidin-4-yl]pyrrolo[2,3-c]pyridine
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C19H16N4O2S
  1
1 IC50 = 12 nM
CP0072038
 Compound Info 
7-methyl-3-[2-(4-methylsulfonylphenyl)pyrimidin-4-yl]-1H-pyrrolo[2,3-c]pyridine
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C19H16N4O2S
  1
1 IC50 = 14 nM
CP0073977
 Compound Info 
3-(2-methylpyrimidin-4-yl)-1H-pyrrolo[2,3-c]pyridine
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C12H10N4
  1
1 IC50 = 17 nM
CP0084894
 Compound Info 
3-[2-(4-methylsulfonylphenyl)pyrimidin-4-yl]-1H-pyrrolo[2,3-c]pyridine
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C18H14N4O2S
  1
1 IC50 = 21 nM
CP0072040
 Compound Info 
6-(1H-indol-3-yl)-N-[4-(4-methylpiperazin-1-yl)phenyl]pyrimidin-4-amine
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C23H24N6
  1
1 IC50 = 85 nM
CP0567741
 Compound Info 
4-[5-[(2-hydroxyphenyl)methylcarbamoyl]thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H16N2O3S2
  1
1 Ki = 65.3 nM
CP0550092
 Compound Info 
4-[5-[(4-aminophenyl)methylcarbamoyl]thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H17N3O2S2
  1
1 Ki = 186.6 nM
CP0546502
 Compound Info 
4-[5-[(2-aminophenyl)methylcarbamoyl]thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H17N3O2S2
  1
1 Ki = 237.9 nM
CP0569737
 Compound Info 
4-[5-(benzylcarbamoyl)thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H16N2O2S2
  1
1 Ki = 277.9 nM
CP0546860
 Compound Info 
4-[5-[(2-aminophenyl)methylcarbamoyl]thiophen-2-yl]-5-chloro-1-benzothiophene-2-carboxamide
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C21H16ClN3O2S2
  1
1 Ki = 576.9 nM
CP0835393
 Compound Info 
CmpdA
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C20H14ClN3O2S2
  1
1 Ki = 642.3 nM
Clinical Information about the Protein
Target 1 ( Dual-specificity tyrosine-phosphorylation regulated kinase 1B (DYRK1B) )
Target Type Patented-recorded Target