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Journal of Medicinal Chemistry|October 11, 2011
Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancerDaniel P Sutherlin, Linda Bao, Megan Berry, et al.Journal of Medicinal Chemistry|May 14, 2013
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activityChudi O Ndubaku, Timothy P Heffron, Steven T Staben, et al.Journal of Medicinal Chemistry|January 8, 2016
The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)Timothy P Heffron, Robert A Heald, Chudi Ndubaku, et al.Bioorganic & Medicinal Chemistry Letters|April 2, 2013
Discovery of thiazolobenzoxepin PI3-kinase inhibitors that spare the PI3-kinase β isoformSteven T Staben, Chudi Ndubaku, Nicole Blaquiere, et al.ACS Medicinal Chemistry Letters|June 6, 2014
Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349Zhonghua Pei, Elizabeth Blackwood, Lichuan Liu, et al.Bioorganic & Medicinal Chemistry Letters|April 15, 2019
Discovery of a class of highly potent Janus Kinase 1/2 (JAK1/2) inhibitors demonstrating effective cell-based blockade of IL-13 signalingMark Zak, Emily J Hanan, Patrick Lupardus, et al.Bioorganic & Medicinal Chemistry Letters|June 8, 2012
Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelfDaniel P Sutherlin, Stewart Baker, Angelina Bisconte, et al.Journal of Medicinal Chemistry|December 12, 2017
Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease SpecificityBinQing Wei, Janet Gunzner-Toste, Hui Yao, et al.Elife|July 14, 2016
The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancerJames D Joseph, Beatrice Darimont, Wei Zhou, et al.Journal of Medicinal Chemistry|May 26, 2012
Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibitionBrian S Safina, Stewart Baker, Matt Baumgardner, et al.Pageof 5