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Structure paper

TitleRigidification Dramatically Improves Inhibitor Selectivity for RAF Kinases.
Journal, issue, pagesAcs Med. Chem. Lett., Vol. 10, Page 1074-1080, Year 2019
Publish dateJan 25, 2019 (structure data deposition date)
AuthorsAssadieskandar, A. / Yu, C. / Maisonneuve, P. / Kurinov, I. / Sicheri, F. / Zhang, C.
External linksAcs Med. Chem. Lett. / PubMed:31312411
MethodsX-ray diffraction
Resolution3.05 Å
Structure data

PDB-6nsq:
Crystal structure of BRAF kinase domain bound to the inhibitor 2l
Method: X-RAY DIFFRACTION / Resolution: 3.05 Å

Chemicals

ChemComp-KZP:
5-[(4-amino-1-ethyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl)ethynyl]-N-(4-chlorophenyl)-6-methylisoquinolin-1-amine

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / BRAF inhibitors / SIGNALING PROTEIN / TRANSFERASE-TRANSFERASE Inhibitor complex / TRANSFERASE

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