General Information of the Protein
Protein ID
PT01592
Protein Name
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Secondarily
Protein Name
Dual specificity YAK1-related kinase
HP86
Protein kinase minibrain homolog
Gene Name
DYRK1A
Secondarily
Gene Name
DYRK
MNB
MNBH
Sequence
MHTGGETSACKPSSVRLAPSFSFHAAGLQMAGQMPHSHQYSDRRQPNISDQQVSALSYSDQIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQQGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRVEQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEMLSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKRSAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPLFSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWNLKKTKDGKREYKPPGTRKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFKKTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGGHFTAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHHHHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSSSTTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTYQFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
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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 (PubMed:21127067, PubMed:8769099, PubMed:30773093, PubMed:20981014, PubMed:23665168). Exhibits a substrate preference for proline at position P+1 and arginine at position P-3 (PubMed:23665168). Plays an important role in double-strand breaks (DSBs) repair following DNA damage (PubMed:31024071). Mechanistically, phosphorylates RNF169 and increases its ability to block accumulation of TP53BP1 at the DSB sites thereby promoting homologous recombination repair (HRR) (PubMed:30773093). 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 (PubMed:25620562, PubMed:29849146). May play a role in a signaling pathway regulating nuclear functions of cell proliferation (PubMed:14500717). Modulates alternative splicing by phosphorylating the splice factor SRSF6 (By similarity). Has pro-survival function and negatively regulates the apoptotic process (By similarity). Promotes cell survival upon genotoxic stress through phosphorylation of SIRT1 (By similarity). This in turn inhibits p53/TP53 activity and apoptosis (By similarity). Phosphorylates SEPTIN4, SEPTIN5 and SF3B1 at 'Thr-434' (By similarity).
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Uniprot ID
Primary ID:
Q13627

Secondarily ID:
O60769
Q92582
Q92810
Q9UNM5
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Ensembl ID
ENSG00000157540
HGNC ID
HGNC:3091
Subcellular Location
Nucleus
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
CP0073979
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 = 153 nM
   TI
   LI
   LO
   TS
CP0099035
(3E)-3-(1,3-benzothiazol-6-ylmethylidene)oxolan-2-one
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C12H9NO2S
 1
1
IC50 = 200 nM
   TI
   LI
   LO
   TS
CP0019844
7-methoxy-1-methyl-9H-beta-carboline;hydrochloride
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C13H12N2O
 1
1
IC50 = 400 nM
   TI
   LI
   LO
   TS
CP0546502
4-[5-[(2-aminophenyl)methylcarbamoyl]thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H17N3O2S2
 1
1
IC50 = 1100 nM
   TI
   LI
   LO
   TS
CP0102176
(5Z)-5-(quinolin-6-ylmethylidene)-2-sulfanylidene-1,3-thiazolidin-4-one
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C13H8N2OS2
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0672481
SID90341202
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C12H7N3O2S
 1
1
IC50 = 1600 nM
   TI
   LI
   LO
   TS
CP0546860
4-[5-[(2-aminophenyl)methylcarbamoyl]thiophen-2-yl]-5-chloro-1-benzothiophene-2-carboxamide
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C21H16ClN3O2S2
 1
1
IC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0835393
CmpdA
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C20H14ClN3O2S2
 1
1
IC50 = 2000 nM
   TI
   LI
   LO
   TS
CP0075817
(5Z)-5-(1,3-benzothiazol-6-ylmethylidene)-2-sulfanylidene-1,3-thiazolidin-4-one
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C11H6N2OS3
 1
1
IC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0102174
(3E)-3-(2,3-dihydro-1-benzofuran-5-ylmethylidene)-5-methyloxolan-2-one
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C14H14O3
 1
1
IC50 = 2100 nM
   TI
   LI
   LO
   TS
CP0550092
4-[5-[(4-aminophenyl)methylcarbamoyl]thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H17N3O2S2
 1
1
IC50 = 2700 nM
   TI
   LI
   LO
   TS
CP0567741
4-[5-[(2-hydroxyphenyl)methylcarbamoyl]thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H16N2O3S2
 1
1
IC50 = 4400 nM
   TI
   LI
   LO
   TS
CP0569737
4-[5-(benzylcarbamoyl)thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H16N2O2S2
 1
1
IC50 = 4600 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0542659
4-[2-methyl-3-(2-phenoxyethyl)imidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C20H20N6O
 1
1 IC50 = 1 nM
CP0574232
4-(2,3-dimethyl-1-benzofuran-5-yl)pyridine-2,6-diamine
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C15H15N3O
 1
1 IC50 = 1 nM
CP0546343
4-(3-butyl-2-methylimidazo[4,5-b]pyridin-5-yl)pyridine-2,6-diamine
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C16H20N6
 1
1 IC50 = 2 nM
CP0546345
4-[2-methyl-3-(2,2,2-trifluoroethyl)imidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C14H13F3N6
 1
1 IC50 = 2 nM
CP0546346
4-[3-[2-(6-bromopyridin-2-yl)oxyethyl]-2-methylimidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C19H18BrN7O
 1
1 IC50 = 2 nM
CP0275949
4-[4-(1,3-benzodioxol-5-yl)-2-methyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl]pyridin-2-amine
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C19H15N5O2
 2
1 IC50 = 3 nM
2 IC50 = 10 nM
CP0542662
4-[3-[2-(6-chloropyridin-2-yl)oxyethyl]-2-methylimidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C19H18ClN7O
 1
1 IC50 = 3 nM
CP0573622
4-[3-(2,2-difluoroethyl)-2-methylimidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C14H14F2N6
 1
1 IC50 = 3 nM
CP0574231
4-[3-[2-(furan-2-yl)ethyl]-2-methylimidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C18H18N6O
 1
1 IC50 = 3 nM
CP0275948
5-(2-aminopyridin-4-yl)-N-[(2,6-difluorophenyl)methyl]-2-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C19H16F2N6
 2
1 IC50 = 4 nM
2 IC50 = 7 nM
CP0546344
4-[3-(2-cyclohexylethyl)-2-methylimidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C20H26N6
 1
1 IC50 = 4 nM
CP0284287
5-(2-aminopyridin-4-yl)-N-[(3-fluoropyridin-2-yl)methyl]-2-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C18H16FN7
 2
1 IC50 = 5 nM
2 IC50 = 8 nM
CP0567799
4-[3-[(2R)-2-(6-bromopyridin-2-yl)oxypropyl]-2-methylimidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C20H20BrN7O
 1
1 IC50 = 5 nM
CP0569842
4-[3-(3-methoxypropyl)-2-methylimidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C16H20N6O
 1
1 IC50 = 6 nM
CP0572103
4-[2-methyl-3-(4,4,4-trifluorobutyl)imidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C16H17F3N6
 1
1 IC50 = 6 nM
CP0579328
4-[2-methyl-3-(2-pyridin-2-yloxyethyl)imidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C19H19N7O
 1
1 IC50 = 6 nM
CP0324832
10-iodo-11H-indolo[3,2-c]quinoline-6-carboxylic acid
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C16H9IN2O2
 1
1 IC50 = 6 nM
CP0175586
4-(3-cyclopropyl-2-methylimidazo[4,5-b]pyridin-5-yl)pyridine-2,6-diamine
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C15H16N6
 2
1 IC50 = 7 nM
2 IC50 = 11 nM
CP0542660
4-[2-methyl-3-[(2R)-2-pyridin-2-yloxypropyl]imidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C20H21N7O
 1
1 IC50 = 7 nM
CP0573621
4-(3-tert-butyl-2-methylimidazo[4,5-b]pyridin-5-yl)pyridine-2,6-diamine
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C16H20N6
 1
1 IC50 = 7 nM
CP0344179
4-[2-methyl-3-[(2R)-2-phenoxypropyl]imidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C21H22N6O
 2
1 IC50 = 8 nM
2 IC50 = 12 nM
CP0275945
5-(2-aminopyrimidin-4-yl)-N-[(2,6-difluorophenyl)methyl]-2-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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C18H15F2N7
 2
1 IC50 = 8 nM
2 IC50 = 10 nM
CP0571356
4-[2-methyl-3-[(2S)-2-phenoxypropyl]imidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C21H22N6O
 1
1 IC50 = 8 nM
CP0574230
4-(2,3-dibutylimidazo[4,5-b]pyridin-5-yl)pyridine-2,6-diamine
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C19H26N6
 1
1 IC50 = 8 nM
CP0019844
7-methoxy-1-methyl-9H-beta-carboline;hydrochloride
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C13H12N2O
 10
1 IC50 = 8.81 nM
2 IC50 = 21.83 nM
3 IC50 = 27 nM
4 IC50 = 29 nM
5 IC50 = 30 nM
6 IC50 = 32 nM
7 IC50 = 33 nM
8 IC50 = 56 nM
9 IC50 = 60 nM
10 IC50 = 80 nM
CP0567798
4-(3-butyl-2-ethylimidazo[4,5-b]pyridin-5-yl)pyridine-2,6-diamine
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C17H22N6
 1
1 IC50 = 11 nM
CP0578032
4-(3-cyclopentyl-2-methylimidazo[4,5-b]pyridin-5-yl)pyridine-2,6-diamine
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C17H20N6
 1
1 IC50 = 13 nM
CP0573620
4-(1-benzofuran-5-yl)pyridine-2,6-diamine
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C13H11N3O
 1
1 IC50 = 14 nM
CP0576679
4-(2,3-dimethylimidazo[4,5-b]pyridin-5-yl)pyridine-2,6-diamine
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C13H14N6
 1
1 IC50 = 15 nM
CP0579329
4-[2-methyl-3-[(2S)-2-pyridin-2-yloxypropyl]imidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C20H21N7O
 1
1 IC50 = 16 nM
CP0542658
4-[3-[(4-fluorophenyl)methyl]-2-methylimidazo[4,5-b]pyridin-5-yl]pyridine-2,6-diamine
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C19H17FN6
 1
1 IC50 = 32 nM
CP0576298
4-(2-methyl-1-benzofuran-5-yl)pyridine-2,6-diamine
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C14H13N3O
 1
1 IC50 = 34 nM
CP0578545
2-N-benzyl-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)thieno[3,2-d]pyrimidine-2,4-diamine
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C19H18N6S
 1
1 IC50 = 903 nM
CP0073979
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 = 30000 nM
2 Ki = 4.4 nM
CP0034962
16-hydroxy-16-(hydroxymethyl)-15-methyl-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8(13),9,11,20(25),21,23-nonaen-3-one
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C26H21N3O4
 1
1 Kd = 20 nM
CP0567741
4-[5-[(2-hydroxyphenyl)methylcarbamoyl]thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H16N2O3S2
 1
1 Ki = 9.9 nM
CP0550092
4-[5-[(4-aminophenyl)methylcarbamoyl]thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H17N3O2S2
 1
1 Ki = 26.8 nM
CP0546860
4-[5-[(2-aminophenyl)methylcarbamoyl]thiophen-2-yl]-5-chloro-1-benzothiophene-2-carboxamide
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C21H16ClN3O2S2
 1
1 Ki = 36.2 nM
CP0569737
4-[5-(benzylcarbamoyl)thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H16N2O2S2
 1
1 Ki = 56.9 nM
CP0546502
4-[5-[(2-aminophenyl)methylcarbamoyl]thiophen-2-yl]-1-benzothiophene-2-carboxamide
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C21H17N3O2S2
 1
1 Ki = 67.8 nM
CP0835393
CmpdA
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C20H14ClN3O2S2
 1
1 Ki = 85.9 nM
Clinical Information about the Protein
Target 1 ( Dual-specificity tyrosine-phosphorylation regulated kinase 1A (DYRK1A) )
Target Type Patented-recorded Target
Disease 1 Target-related Disease  1
1 Cytomegalovirus Disease [ICD-11: 1D82]
Patented Agent(s) 1 Patented Agent  1
1 Benzimidazole Investigative
Cytomegalovirus Disease