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TitlePhthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of aurora-a kinase.
Journal, issue, pagesJ. Med. Chem., Vol. 54, Page 312-319, Year 2011
Publish dateOct 17, 2010 (structure data deposition date)
AuthorsPrime, M.E. / Courtney, S.M. / Brookfield, F.A. / Marston, R.W. / Walker, V. / Warne, J. / Boyd, A.E. / Kairies, N.A. / von der Saal, W. / Limberg, A. ...Prime, M.E. / Courtney, S.M. / Brookfield, F.A. / Marston, R.W. / Walker, V. / Warne, J. / Boyd, A.E. / Kairies, N.A. / von der Saal, W. / Limberg, A. / Georges, G. / Engh, R.A. / Goller, B. / Rueger, P. / Rueth, M.
External linksJ. Med. Chem. / PubMed:21128645
MethodsX-ray diffraction
Resolution2.8 Å
Structure data

PDB-3p9j:
Aurora A kinase domain with phthalazinone pyrazole inhibitor
Method: X-RAY DIFFRACTION / Resolution: 2.8 Å

Chemicals

ChemComp-P9J:
4-[(5-methyl-1H-pyrazol-3-yl)amino]-2-phenylphthalazin-1(2H)-one

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / Phosphotransferase / TRANSFERASE / TRANSFERASE-TRANSFERASE INHIBITOR complex

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