Reaction Details |
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Target | Dual specificity tyrosine-phosphorylation-regulated kinase 1B |
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Ligand | BDBM50081182 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1475745 (CHEMBL3424978) |
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IC50 | 9.0±n/a nM |
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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 Chem58:2834-44 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Dual specificity tyrosine-phosphorylation-regulated kinase 1B |
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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: | MAVPPGHGPFSGFPGPQEHTQVLPDVRLLPRRLPLAFRDATSAPLRKLSVDLIKTYKHIN
EVYYAKKKRRAQQAPPQDSSNKKEKKVLNHGYDDDNHDYIVRSGERWLERYEIDSLIGKG
SFGQVVKAYDHQTQELVAIKIIKNKKAFLNQAQIELRLLELMNQHDTEMKYYIVHLKRHF
MFRNHLCLVFELLSYNLYDLLRNTHFRGVSLNLTRKLAQQLCTALLFLATPELSIIHCDL
KPENILLCNPKRSAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGTPYDLAIDMWSLG
CILVEMHTGEPLFSGSNEVDQMNRIVEVLGIPPAAMLDQAPKARKYFERLPGGGWTLRRT
KELRKDYQGPGTRRLQEVLGVQTGGPGGRRAGEPGHSPADYLRFQDLVLRMLEYEPAARI
SPLGALQHGFFRRTADEATNTGPAGSSASTSPAPLDTCPSSSTASSISSSGGSSGSSSDN
RTYRYSNRYCGGPGPPITDCEMNSPQVPPSQPLRPWAGGDVPHKTHQAPASASSLPGTGA
QLPPQPRYLGRPPSPTSPPPPELMDVSLVGGPADCSPPHPAPAPQHPAASALRTRMTGGR
PPLPPPDDPATLGPHLGLRGVPQSTAASS
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BDBM50081182 |
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n/a |
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Name | BDBM50081182 |
Synonyms: | CHEMBL3421966 |
Type | Small organic molecule |
Emp. Form. | C24H25N7O2 |
Mol. Mass. | 443.501 |
SMILES | COc1cc(ccc1Nc1nccc(n1)-c1c[nH]c2cnccc12)N1CCN(CC1)C(C)=O |
Structure |
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