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TitleProteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors.
Journal, issue, pagesCell Chem Biol, Vol. 24, Page 1388-1400.e7, Year 2017
Publish dateFeb 21, 2017 (structure data deposition date)
AuthorsNiessen, S. / Dix, M.M. / Barbas, S. / Potter, Z.E. / Lu, S. / Brodsky, O. / Planken, S. / Behenna, D. / Almaden, C. / Gajiwala, K.S. ...Niessen, S. / Dix, M.M. / Barbas, S. / Potter, Z.E. / Lu, S. / Brodsky, O. / Planken, S. / Behenna, D. / Almaden, C. / Gajiwala, K.S. / Ryan, K. / Ferre, R. / Lazear, M.R. / Hayward, M.M. / Kath, J.C. / Cravatt, B.F.
External linksCell Chem Biol / PubMed:28965727
MethodsX-ray diffraction
Resolution3.06 Å
Structure data

PDB-5uwd:
Crystal structure of EGFR kinase domain (L858R, T790M, V948R) in complex with the covalent inhibitor CO-1686
Method: X-RAY DIFFRACTION / Resolution: 3.06 Å

Chemicals

ChemComp-8OV:
N-(3-{[2-{[4-(4-acetylpiperazin-1-yl)-2-methoxyphenyl]amino}-5-(trifluoromethyl)pyrimidin-4-yl]amino}phenyl)propanamide

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / EGFR / kinase / covalent inhibitor / TRANSFERASE-TRANSFERASE INHIBITOR complex

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