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Journal of Medicinal Chemistry|June 16, 2026
Discovery of CNS Penetrant SOS1 Inhibitors for the Treatment of KRAS-Dependent CancersSharan K Bagal, Coura R N Diène, Sandra Stefanovic-Barrett, et al.Science Translational Medicine|May 1, 2020
Discovery and pharmacological characterization of AZD3229, a potent KIT/PDGFRα inhibitor for treatment of gastrointestinal stromal tumorsErica Banks, Michael Grondine, Deepa Bhavsar, et al.Journal of Medicinal Chemistry|June 25, 2024
Design of a Lead-Like Cysteine-Targeting Covalent Library and the Identification of Hits to Cys55 of Bfl-1Simon C C Lucas, Alexander G Milbradt, J Henry Blackwell, et al.Journal of Medicinal Chemistry|April 17, 2020
Discovery of (2<i>R</i>)-<i>N</i>-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1<i>H</i>-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 InhibitorQibin Su, Erica Banks, Geraldine Bebernitz, et al.Journal of Medicinal Chemistry|September 12, 2018
Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal TumorsJason G Kettle, Rana Anjum, Evan Barry, et al.Journal of Medicinal Chemistry|June 2, 2018
Discovery and Optimization of a Novel Series of Highly Selective JAK1 Kinase InhibitorsNeil P Grimster, Erica Anderson, Marat Alimzhanov, et al.Journal of Medicinal Chemistry|April 8, 2015
Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3Scott Boyd, Joanna L Brookfield, Susan E Critchlow, et al.Communications Biology|May 13, 2024
Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTACThomas G Hayhow, Beth Williamson, Mandy Lawson, et al.Journal of Medicinal Chemistry|February 6, 2020
Structure-Based Design and Pharmacokinetic Optimization of Covalent Allosteric Inhibitors of the Mutant GTPase KRAS<sup>G12C</sup>Jason G Kettle, Sharan K Bagal, Sue Bickerton, et al.Nature Communications|December 19, 2018
Discovery of Mcl-1-specific inhibitor AZD5991 and preclinical activity in multiple myeloma and acute myeloid leukemiaAdriana E Tron, Matthew A Belmonte, Ammar Adam, et al.Pageof 8