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TitleSelective DYRK1A Inhibitor for the Treatment of Type 1 Diabetes: Discovery of 6-Azaindole Derivative GNF2133.
Journal, issue, pagesJ. Med. Chem., Vol. 63, Page 2958-2973, Year 2020
Publish dateOct 1, 2019 (structure data deposition date)
AuthorsLiu, Y.A. / Jin, Q. / Zou, Y. / Ding, Q. / Yan, S. / Wang, Z. / Hao, X. / Nguyen, B. / Zhang, X. / Pan, J. ...Liu, Y.A. / Jin, Q. / Zou, Y. / Ding, Q. / Yan, S. / Wang, Z. / Hao, X. / Nguyen, B. / Zhang, X. / Pan, J. / Mo, T. / Jacobsen, K. / Lam, T. / Wu, T.Y. / Petrassi, H.M. / Bursulaya, B. / DiDonato, M. / Gordon, W.P. / Liu, B. / Baaten, J. / Hill, R. / Nguyen-Tran, V. / Qiu, M. / Zhang, Y.Q. / Kamireddy, A. / Espinola, S. / Deaton, L. / Ha, S. / Harb, G. / Jia, Y. / Li, J. / Shen, W. / Schumacher, A.M. / Colman, K. / Glynne, R. / Pan, S. / McNamara, P. / Laffitte, B. / Meeusen, S. / Molteni, V. / Loren, J.
External linksJ. Med. Chem. / PubMed:32077280
MethodsX-ray diffraction
Resolution3.7 Å
Structure data

PDB-6uip:
DYRK1A Kinase Domain in Complex with a 6-azaindole Derivative, GNF2133.
Method: X-RAY DIFFRACTION / Resolution: 3.7 Å

Chemicals

ChemComp-Q8J:
4-ethyl-N-{4-[1-(oxan-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]pyridin-2-yl}piperazine-1-carboxamide

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / Kinase / Inhibitor

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