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TargetDual-specificity tyrosine-phosphorylation regulated kinase 1A
LigandBDBM50444373
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1279586
IC50 8.0±n/a nM
Citation Anderson KChen YChen ZDominique RGlenn KHe YJanson CLuk KCLukacs CPolonskaia AQiao QRailkar ARossman PSun HXiang QVilenchik MWovkulich PZhang X Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors. Bioorg Med Chem Lett 23:6610-5 (2013) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Dual-specificity tyrosine-phosphorylation regulated kinase 1A
Name:Dual-specificity tyrosine-phosphorylation regulated kinase 1A
Synonyms:DYRK1A | Dual specificity YAK1-related kinase | Dual specificity YAK1-related kinase 1A (Dyrk1A) | Dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) | Dual-specificity tyrosine-regulated kinases 1A | HP86
Type:Enzyme
Mol. Mass.:85616.61
Organism:Homo sapiens (Human)
Description:Q13627
Residue:763
Sequence:
MHTGGETSACKPSSVRLAPSFSFHAAGLQMAGQMPHSHQYSDRRQPNISDQQVSALSYSD
QIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQ
QGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRV
EQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEM
LSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKR
SAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPL
FSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWNLKKTKDGKREYKPPGT
RKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFK
KTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGG
HFTAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHH
HHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSS
STTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTY
QFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50444373
n/a
NameBDBM50444373
Synonyms:CHEMBL3094454
TypeSmall organic molecule
Emp. Form.C24H21ClN6O4
Mol. Mass.492.914
SMILESCOc1ncc2cc(C(=O)Nc3cc(ccc3Cl)C(=O)NC(CN)c3ccccc3)c(=O)[nH]c2n1
Structure
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