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TitleThe discovery of 2-substituted phenol quinazolines as potent RET kinase inhibitors with improved KDR selectivity.
Journal, issue, pagesEur J Med Chem, Vol. 112, Page 20-32, Year 2016
Publish dateMar 11, 2015 (structure data deposition date)
AuthorsNewton, R. / Bowler, K.A. / Burns, E.M. / Chapman, P.J. / Fairweather, E.E. / Fritzl, S.J.R. / Goldberg, K.M. / Hamilton, N.M. / Holt, S.V. / Hopkins, G.V. ...Newton, R. / Bowler, K.A. / Burns, E.M. / Chapman, P.J. / Fairweather, E.E. / Fritzl, S.J.R. / Goldberg, K.M. / Hamilton, N.M. / Holt, S.V. / Hopkins, G.V. / Jones, S.D. / Jordan, A.M. / Lyons, A.J. / Nikki March, H. / McDonald, N.Q. / Maguire, L.A. / Mould, D.P. / Purkiss, A.G. / Small, H.F. / Stowell, A.I.J. / Thomson, G.J. / Waddell, I.D. / Waszkowycz, B. / Watson, A.J. / Ogilvie, D.J.
External linksEur J Med Chem / PubMed:26874741
MethodsX-ray diffraction
Resolution2.57 Å
Structure data

PDB-5amn:
The Discovery of 2-Substituted Phenol Quinazolines as Potent and Selective RET Kinase Inhibitors
Method: X-RAY DIFFRACTION / Resolution: 2.57 Å

Chemicals

ChemComp-DTQ:
4-[3-HYDROXYANILINO]-6,7-DIMETHOXYQUINAZOLINE

ChemComp-FMT:
FORMIC ACID

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / RET / ONCOGENE / RECEPTOR TYROSINE KINASE / CHEMICAL INHIBITOR / CANCER

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