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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
Ligand
BDBM50324735
Substrate
n/a
Meas. Tech.
ChEMBL_1560173 (CHEMBL3778244)
IC50
80±n/a nM
Citation
 Mariano, M; Hartmann, RW; Engel, M Systematic diversification of benzylidene heterocycles yields novel inhibitor scaffolds selective for Dyrk1A, Clk1 and CK2. Eur J Med Chem 112:209-16 (2016) [PubMed]  Article
Target
Name:
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
Synonyms:
DYR1B_HUMAN | DYRK1B | Dual specificity tyrosine-phosphorylation-regulated kinase 1B | Dual-specificity tyrosine-regulated kinases 1B | MIRK
Type:
Enzyme
Mol. Mass.:
69222.24
Organism:
Homo sapiens (Human)
Description:
Q9Y463
Residue:
629
Sequence:
MAVPPGHGPFSGFPGPQEHTQVLPDVRLLPRRLPLAFRDATSAPLRKLSVDLIKTYKHINEVYYAKKKRRAQQAPPQDSSNKKEKKVLNHGYDDDNHDYIVRSGERWLERYEIDSLIGKGSFGQVVKAYDHQTQELVAIKIIKNKKAFLNQAQIELRLLELMNQHDTEMKYYIVHLKRHFMFRNHLCLVFELLSYNLYDLLRNTHFRGVSLNLTRKLAQQLCTALLFLATPELSIIHCDLKPENILLCNPKRSAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGTPYDLAIDMWSLGCILVEMHTGEPLFSGSNEVDQMNRIVEVLGIPPAAMLDQAPKARKYFERLPGGGWTLRRTKELRKDYQGPGTRRLQEVLGVQTGGPGGRRAGEPGHSPADYLRFQDLVLRMLEYEPAARISPLGALQHGFFRRTADEATNTGPAGSSASTSPAPLDTCPSSSTASSISSSGGSSGSSSDNRTYRYSNRYCGGPGPPITDCEMNSPQVPPSQPLRPWAGGDVPHKTHQAPASASSLPGTGAQLPPQPRYLGRPPSPTSPPPPELMDVSLVGGPADCSPPHPAPAPQHPAASALRTRMTGGRPPLPPPDDPATLGPHLGLRGVPQSTAASS
  
Inhibitor
Name:
BDBM50324735
Synonyms:
(5E)-5-(QUINOXALIN-6-YLMETHYLENE)-1,3-THIAZOLIDINE-2,4-DIONE | 5-(quinoxalin-6-ylmethylene)thiazolidine-2,4-dione | AS-605240 | AS605240 | CHEMBL568150
Type:
Small organic molecule
Emp. Form.:
C12H7N3O2S
Mol. Mass.:
257.268
SMILES:
OC1=NC(=O)C(S1)=Cc1ccc2nccnc2c1 |w:7.8,t:1|
Structure:
Search PDB for entries with ligand similarity: