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TitleOptimization of Selectivity and Pharmacokinetic Properties of Salt-Inducible Kinase Inhibitors that Led to the Discovery of Pan-SIK Inhibitor GLPG3312.
Journal, issue, pagesJ. Med. Chem., Vol. 67, Page 380-401, Year 2024
Publish dateMar 29, 2023 (structure data deposition date)
AuthorsTemal-Laib, T. / Peixoto, C. / Desroy, N. / De Lemos, E. / Bonnaterre, F. / Bienvenu, N. / Picolet, O. / Sartori, E. / Bucher, D. / Lopez-Ramos, M. ...Temal-Laib, T. / Peixoto, C. / Desroy, N. / De Lemos, E. / Bonnaterre, F. / Bienvenu, N. / Picolet, O. / Sartori, E. / Bucher, D. / Lopez-Ramos, M. / Roca Magadan, C. / Laenen, W. / Flower, T. / Mollat, P. / Bugaud, O. / Touitou, R. / Pereira Fernandes, A. / Lavazais, S. / Monjardet, A. / Borgonovi, M. / Gosmini, R. / Brys, R. / Amantini, D. / De Vos, S. / Andrews, M.
External linksJ. Med. Chem. / PubMed:38147525
MethodsX-ray diffraction
Resolution3.1 Å
Structure data

PDB-8oku:
Salt-Inducible Kinase 3 in complex with an inhibitor
Method: X-RAY DIFFRACTION / Resolution: 3.1 Å

Chemicals

ChemComp-VRU:
~{N}-ethyl-4-[5-[1-(2-hydroxyethyl)pyrazol-4-yl]benzimidazol-1-yl]-2,6-dimethoxy-benzamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsSIGNALING PROTEIN / Kinase UBA Inhibitor

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