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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
Ligand
BDBM50249773
Substrate
n/a
Meas. Tech.
ChEMBL_2012564 (CHEMBL4666142)
IC50
20±n/a nM
Citation
 Tazarki, H; Zeinyeh, W; Esvan, YJ; Knapp, S; Chatterjee, D; Schröder, M; Joerger, AC; Khiari, J; Josselin, B; Baratte, B; Bach, S; Ruchaud, S; Anizon, F; Giraud, F; Moreau, P New pyrido[3,4-g]quinazoline derivatives as CLK1 and DYRK1A inhibitors: synthesis, biological evaluation and binding mode analysis. Eur J Med Chem 166:304-317 (2019) [PubMed]  Article 
Target
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:
MHTGGETSACKPSSVRLAPSFSFHAAGLQMAAQMPHSHQYSDRRQPNISDQQVSALSYSDQIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQQGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRVEQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEMLSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKRSAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPLFSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWSLKKTKDGKREYKPPGTRKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFKKTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGGHFAAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHHHHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSSSTTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTYQFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
  
Inhibitor
Name:
BDBM50249773
Synonyms:
CHEMBL4763099
Type:
Small organic molecule
Emp. Form.:
C19H25N7
Mol. Mass.:
351.4487
SMILES:
CN1CCN(CCCNc2ncc3cc4cnccc4c(N)c3n2)CC1
Structure:
Search PDB for entries with ligand similarity: