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TitleEvolution of a Highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor
Journal, issue, pagesJ. Med. Chem., Vol. 50, Page 611-626, Year 2007
Publish dateMar 7, 2007 (structure data deposition date)
AuthorsHodous, B.L. / Geuns-Meyer, S.D. / Hughes, P.E. / Albrecht, B.K. / Bellon, S. / Bready, J. / Caenepeel, S. / Cee, V.J. / Chaffee, S.C. / Coxon, A. ...Hodous, B.L. / Geuns-Meyer, S.D. / Hughes, P.E. / Albrecht, B.K. / Bellon, S. / Bready, J. / Caenepeel, S. / Cee, V.J. / Chaffee, S.C. / Coxon, A. / Emery, M. / Fretland, J. / Gallant, P. / Gu, Y. / Hoffman, D. / Johnson, R.E. / Kendall, R. / Kim, J.L. / Long, A.M. / Morrison, M. / Olivieri, P.R. / Patel, V.F. / Polverino, A. / Rose, P. / Tempest, P. / Wang, L. / Whittington, D.A. / Zhao, H.
External linksJ. Med. Chem. / PubMed:17253678
MethodsX-ray diffraction
Resolution1.95 - 2.5 Å
Structure data

PDB-2p2h:
Crystal structure of the VEGFR2 kinase domain in complex with a pyridinyl-triazine inhibitor
Method: X-RAY DIFFRACTION / Resolution: 1.95 Å

PDB-2p2i:
Crystal structure of the VEGFR2 kinase domain in complex with a nicotinamide inhibitor
Method: X-RAY DIFFRACTION / Resolution: 2.4 Å

PDB-2p4i:
Evolution of a highly Selective and Potent 2-(Pyridin-2-yl)-1,3,5-triazine Tie-2 Kinase Inhibitor
Method: X-RAY DIFFRACTION / Resolution: 2.5 Å

Chemicals

ChemComp-994:
4-(2-anilinopyridin-3-yl)-N-(3,4,5-trimethoxyphenyl)-1,3,5-triazin-2-amine

ChemComp-HOH:
WATER

ChemComp-608:
N-(4-phenoxyphenyl)-2-[(pyridin-4-ylmethyl)amino]nicotinamide

ChemComp-MR9:
4-METHYL-3-({3-[2-(METHYLAMINO)PYRIMIDIN-4-YL]PYRIDIN-2-YL}OXY)-N-[2-MORPHOLIN-4-YL-5-(TRIFLUOROMETHYL)PHENYL]BENZAMIDE

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / receptor tyrosine kinase / KDR / Tie-2 Kinase Inhibitor triazine

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