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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
Ligand
BDBM50594790
Substrate
n/a
Meas. Tech.
ChEMBL_2214247 (CHEMBL5127379)
IC50
20±n/a nM
Citation
 Tahtouh, T; Durieu, E; Villiers, B; Bruyère, C; Nguyen, TL; Fant, X; Ahn, KH; Khurana, L; Deau, E; Lindberg, MF; Sévère, E; Miege, F; Roche, D; Limanton, E; L'Helgoual'ch, JM; Burgy, G; Guiheneuf, S; Herault, Y; Kendall, DA; Carreaux, F; Bazureau, JP; Meijer, L Structure-Activity Relationship in the Leucettine Family of Kinase Inhibitors. J Med Chem 65:1396-1417 (2022) [PubMed] 
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:
BDBM50594790
Synonyms:
CHEMBL5200518
Type:
Small organic molecule
Emp. Form.:
C22H25N5O3
Mol. Mass.:
407.4656
SMILES:
COc1cc(\C=C2/N=C(Nc3ccc(cc3)N3CCN(C)CC3)NC2=O)ccc1O |t:7|
Structure:
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