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Target
Dual specificity tyrosine-phosphorylation-regulated kinase 1B
Ligand
BDBM50081183
Substrate
n/a
Meas. Tech.
ChEMBL_1475745 (CHEMBL3424978)
IC50
34±n/a nM
Citation
 Kettle, JG; Ballard, P; Bardelle, C; Cockerill, M; Colclough, N; Critchlow, SE; Debreczeni, J; Fairley, G; Fillery, S; Graham, MA; Goodwin, L; Guichard, S; Hudson, K; Ward, RA; Whittaker, D Discovery and optimization of a novel series of Dyrk1B kinase inhibitors to explore a MEK resistance hypothesis. J Med Chem 58:2834-44 (2015) [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:
BDBM50081183
Synonyms:
CHEMBL3421965
Type:
Small organic molecule
Emp. Form.:
C25H27N7O2
Mol. Mass.:
457.5276
SMILES:
COc1cc(ccc1Nc1cc(ncn1)-c1cn(C)c2cnccc12)N1CCN(CC1)C(C)=O
Structure:
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