4UXL

Structure of Human ROS1 Kinase Domain in Complex with PF-06463922

Summary for 4UXL

• Entry DOI: 10.2210/pdb4uxl/pdb
• Descriptor: PROTO-ONCOGENE TYROSINE-PROTEIN KINASE ROS, (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]benzoxadiazacyclotetradecine-3-carbonitrile (3 entities in total)
• Functional Keywords: transferase, inhibitor, ros
• Biological source: HOMO SAPIENS (HUMAN)
• Total number of polymer chains: 1
• Total formula weight: 37420.90

Authors

McTigue, M.,Deng, Y.,Liu, W.,Brooun, A.,Stewart, A. (deposition date: 2014-08-25, release date: 2015-03-11, Last modification date: 2024-01-10)

• Primary citation: Zou, H.Y.,Li, Q.,Engstrom, L.D.,West, M.,Appleman, V.,Wong, K.A.,Mctigue, M.,Deng, Y.,Liu, W.,Brooun, A.,Timofeevski, S.,Mcdonnell, S.R.P.,Jiang, P.,Falk, M.D.,Lappin, P.B.,Affolter, T.,Nichols, T.,Hu, W.,Lam, J.,Johnson, T.W.,Smeal, T.,Charest, A.,Fantin, V.R.; Pf-06463922 is a Potent and Selective Next-Generation Ros1/Alk Inhibitor Capable of Blocking Crizotinib-Resistant Ros1 Mutations.; Proc.Natl.Acad.Sci.USA, 112:3493-, 2015; PubMed: 25733882; DOI: 10.1073/PNAS.1420785112

Experimental method

X-RAY DIFFRACTION (2.4 Å)