General Information of the Protein
Protein ID
PT06527
Protein Name
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Secondarily
Protein Name
Dual specificity YAK1-related kinase
MP86
Protein kinase minibrain homolog
Gene Name
DYRK1A
Secondarily
Gene Name
Dyrk
Sequence
MHTGGETSACKPSSVRLAPSFSFHAAGLQMAAQMPHSHQYSDRRQPSISDQQVSALPYSDQIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQQGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRVEQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEMLSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKRSAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPLFSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWSLKKTKDGKREYKPPGTRKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFKKTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGGHFAAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHHHHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSSSTTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTYQFSANTGPAHYMTEGHLAMRQGADREESPMTGVCVQQSPVASS
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Organism
Mus musculus, Mouse
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 (PubMed:18938227, PubMed:20123978). Exhibits a substrate preference for proline at position P+1 and arginine at position P-3 (By similarity). Plays an important role in double-strand breaks (DSBs) repair following DNA damage (By similarity). Mechanistically, phosphorylates RNF169 and increases its ability to block accumulation of TP53BP1 at the DSB sites thereby promoting homologous recombination repair (HRR) (By similarity). Also acts as a positive regulator of transcription by acting as a CTD kinase that mediates phosphorylation of the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAP II) POLR2A (By similarity). May play a role in a signaling pathway regulating nuclear functions of cell proliferation (By similarity). Modulates alternative splicing by phosphorylating the splice factor SRSF6 (By similarity). Has pro-survival function and negatively regulates the apoptotic process (PubMed:20167603). Promotes cell survival upon genotoxic stress through phosphorylation of SIRT1 (PubMed:20167603). This in turn inhibits p53/TP53 activity and apoptosis (PubMed:20167603). Phosphorylates SEPTIN4, SEPTIN5 and SF3B1 at 'Thr-434' (PubMed:18938227).
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Uniprot ID
Q61214
Ensembl ID
ENSG00000157540
Subcellular Location
Nucleus speckle
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: CL000006 , HEK293
Compound ID Compound Name Compound Formula
CP0640301
4-(4-hydroxy-3-methoxybenzylidene)-1-(3,4-dichlorophenyl)pyrazolidine-3,5-dione
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C17H12Cl2N2O4
 1
1
IC50 = 2500 nM
   TI
   LI
   LO
   TS
CP0001111
(2R)-2-[[6-(benzylamino)-9-isopropyl-purin-2-yl]amino]butan-1-ol
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C19H26N6O
 1
1
IC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0017065
1-(3-methoxyphenyl)-3-(5-(pyridin-4-yl)-1,3,4-thiadiazol-2-yl)urea
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C15H13N5O2S
 1
1
IC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0401719
2-N-(4-bromophenyl)-4-N-(furan-2-ylmethyl)quinazoline-2,4-diamine
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C19H15BrN4O
 1
1
IC50 = 5000 nM
   TI
   LI
   LO
   TS
CP0464310
diethyl 4-(4-acetamidoanilino)quinoline-3,6-dicarboxylate
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C23H23N3O5
 1
1
IC50 = 10000 nM
   TI
   LI
   LO
   TS
CP0084005
2-(5-(2-chlorophenyl)-1H-pyrazol-3-yl)-4-methoxyphenol
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C16H13ClN2O2
 1
1
IC50 = 20000 nM
   TI
   LI
   LO
   TS
CP0897617
5-(5-(2-(allyloxy)-5-bromobenzylidene)-4-oxo-4,5-dihydrothiazol-2-ylamino)-2-chlorobenzoic acid
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C20H14BrClN2O4S
 1
1
IC50 = 20000 nM
   TI
   LI
   LO
   TS
CP0262317
diethyl 4-(3-bromo-4-methylanilino)quinoline-3,6-dicarboxylate
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C22H21BrN2O4
 1
1
IC50 = 50000 nM
   TI
   LI
   LO
   TS
CP0501958
4-(2-methylimidazo[1,2-a]pyrimidin-3-yl)-N-m-tolylthiazol-2-amine
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C17H15N5S
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0522281
3-ethyl 6-methyl 4-(3-acetylphenylamino)quinoline-3,6-dicarboxylate
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C22H20N2O5
 1
1
IC50 = 50000 nM
   TI
   LI
   LO
   TS
CP0897621
4-(4-hydroxy-3-methoxybenzylidene)-1-(3-chlorophenyl)pyrazolidine-3,5-dione
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C17H13ClN2O4
 1
1
IC50 > 50000 nM
   TI
   LI
   LO
   TS
CP0897645
(Z)-3-(2-(4-fluorophenylamino)-4-oxothiazol-5(4H)-ylidene)-1-methylindolin-2-one
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C18H12FN3O2S
 1
1
IC50 = 50000 nM
   TI
   LI
   LO
   TS