Reaction Details |
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Target | Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
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Ligand | BDBM27217 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1794525 (CHEMBL4266642) |
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IC50 | 1300±n/a nM |
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Citation | Jarhad, DB; Mashelkar, KK; Kim, HR; Noh, M; Jeong, LS Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A (DYRK1A) Inhibitors as Potential Therapeutics. J Med Chem61:9791-9810 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
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Name: | Dual specificity tyrosine-phosphorylation-regulated kinase 1A |
Synonyms: | DYR1A_RAT | Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A | Dyrk | Dyrk1a |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 85573.59 |
Organism: | RAT |
Description: | Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A 0 RAT::Q63470 |
Residue: | 763 |
Sequence: | MHTGGETSACKPSSVRLAPSFSFHAAGLQMAAQMPHSHQYSDRRQPNISDQQVSALSYSD
QIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQ
QGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRV
EQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEM
LSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKR
SAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPL
FSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWSLKKTKDGKREYKPPGT
RKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFK
KTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGG
HFAAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHH
HHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSS
STTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTY
QFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
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BDBM27217 |
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n/a |
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Name | BDBM27217 |
Synonyms: | (2R)-2-{[4-(benzylamino)-8-(propan-2-yl)pyrazolo[1,5-a][1,3,5]triazin-2-yl]amino}butan-1-ol | GP0210 | pyrazolo[1,5-a]-1,3,5-triazine, 7a |
Type | Small organic molecule |
Emp. Form. | C19H26N6O |
Mol. Mass. | 354.4493 |
SMILES | CC[C@H](CO)Nc1nc(NCc2ccccc2)n2ncc(C(C)C)c2n1 |r| |
Structure |
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