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TargetDual specificity tyrosine-phosphorylation-regulated kinase 1A
LigandBDBM50347388
Substrate/Competitorn/a
Meas. Tech.ChEMBL_754583 (CHEMBL1806286)
IC50 2100±n/a nM
Citation Heathcote, DAPatel, HKroll, SHHazel, PPeriyasamy, MAlikian, MKanneganti, SKJogalekar, ASScheiper, BBarbazanges, MBlum, ABrackow, JSiwicka, APace, RDFuchter, MJSnyder, JPLiotta, DCFreemont, PSAboagye, EOCoombes, RCBarrett, AGAli, S A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1, 2, and 9, which demonstrates antitumor effects in human tumor xenografts following oral administration. J Med Chem53:8508-22 (2010) [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:DYR1A_HUMAN | DYRK | DYRK1A | Dual specificity YAK1-related kinase | Dual specificity YAK1-related kinase 1A (Dyrk1A) | Dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A) | Dual-specificity tyrosine-phosphorylation regulated kinase 1A | Dual-specificity tyrosine-regulated kinases 1A | HP86 | MNB | MNBH
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:
BDBM50347388
n/a
NameBDBM50347388
Synonyms:CHEMBL1234833
TypeSmall organic molecule
Emp. Form.C20H27N5O3
Mol. Mass.385.4601
SMILESCC(C)c1cnn2c(NCc3ccccc3)cc(N[C@@H](CO)[C@H](O)CO)nc12 |r|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: