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TitleDiscovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.
Journal, issue, pagesJ. Med. Chem., Vol. 54, Page 7334-7349, Year 2011
Publish dateMay 6, 2011 (structure data deposition date)
AuthorsLim, J. / Taoka, B. / Otte, R.D. / Spencer, K. / Dinsmore, C.J. / Altman, M.D. / Chan, G. / Rosenstein, C. / Sharma, S. / Su, H.P. ...Lim, J. / Taoka, B. / Otte, R.D. / Spencer, K. / Dinsmore, C.J. / Altman, M.D. / Chan, G. / Rosenstein, C. / Sharma, S. / Su, H.P. / Szewczak, A.A. / Xu, L. / Yin, H. / Zugay-Murphy, J. / Marshall, C.G. / Young, J.R.
External linksJ. Med. Chem. / PubMed:21942426
MethodsX-ray diffraction
Resolution2.498 Å
Structure data

PDB-3rvg:
Crystals structure of Jak2 with a 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitor
Method: X-RAY DIFFRACTION / Resolution: 2.498 Å

Chemicals

ChemComp-17P:
1-(cyclohexylamino)-7-(1-methyl-1H-pyrazol-4-yl)-5H-pyrido[4,3-b]indole-4-carboxamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / Tyrosine Kinase / Janus Kinase 2 / Enzyme Inhibitors / TRANSFERASE-TRANSFERASE INHIBITOR complex

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