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TitleHighly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.
Journal, issue, pagesBioorg. Med. Chem. Lett., Vol. 24, Page 1923-1927, Year 2014
Publish dateFeb 26, 2014 (structure data deposition date)
AuthorsWenglowsky, S. / Ren, L. / Grina, J. / Hansen, J.D. / Laird, E.R. / Moreno, D. / Dinkel, V. / Gloor, S.L. / Hastings, G. / Rana, S. ...Wenglowsky, S. / Ren, L. / Grina, J. / Hansen, J.D. / Laird, E.R. / Moreno, D. / Dinkel, V. / Gloor, S.L. / Hastings, G. / Rana, S. / Rasor, K. / Sturgis, H.L. / Voegtli, W.C. / Vigers, G. / Willis, B. / Mathieu, S. / Rudolph, J.
External linksBioorg. Med. Chem. Lett. / PubMed:24675381
MethodsX-ray diffraction
Resolution3.4 Å
Structure data

PDB-4pp7:
Highly Potent and Selective 3-N-methylquinazoline-4(3H)-one Based Inhibitors of B-RafV600E Kinase
Method: X-RAY DIFFRACTION / Resolution: 3.4 Å

Chemicals

ChemComp-2VX:
N-{2,4-difluoro-3-[methyl(3-methyl-4-oxo-3,4-dihydroquinazolin-6-yl)amino]phenyl}propane-1-sulfonamide

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / serine/threonine-protein kinase B-Raf / TRANSFERASE-TRANSFERASE INHIBITOR complex

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