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TitleDiscovery and Optimization of a Novel Series of Dyrk1B Kinase Inhibitors to Explore a Mek Resistance Hypothesis.
Journal, issue, pagesJ. Med. Chem., Vol. 58, Page 2834-, Year 2015
Publish dateMay 12, 2014 (structure data deposition date)
AuthorsKettle, J.G. / Ballard, P. / Bardelle, C. / Cockerill, M. / Colclough, N. / Critchlow, S.E. / Debreczeni, J.E. / Fairley, G. / Fillery, S. / Graham, M.A. ...Kettle, J.G. / Ballard, P. / Bardelle, C. / Cockerill, M. / Colclough, N. / Critchlow, S.E. / Debreczeni, J.E. / Fairley, G. / Fillery, S. / Graham, M.A. / Goodwin, L. / Guichard, S. / Hudson, K. / Ward, R.A. / Whittaker, D.
External linksJ. Med. Chem. / PubMed:25738750
MethodsX-ray diffraction
Resolution2.1 - 2.5 Å
Structure data

PDB-4d2r:
Human IGF in complex with a Dyrk1B inhibitor
Method: X-RAY DIFFRACTION / Resolution: 2.1 Å

PDB-4d2s:
Human TTK in complex with a Dyrk1B inhibitor
Method: X-RAY DIFFRACTION / Resolution: 2.5 Å

Chemicals

ChemComp-CL:
Unknown entry

ChemComp-DYK:
N-{2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]phenyl}-4-(1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / KINASE / INHIBITOR / ONCOLOGY

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