Michael Burkard

The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients

Jill Hallin, Lars D. Engstrom, Lauren Hargis et al. · Cancer Discovery · 2019 · 1.2K citations · Full text

Identification of the Clinical Development Candidate <b>MRTX849</b>, a Covalent KRAS^G12C Inhibitor for the Treatment of Cancer

Jay B. Fell, John P. Fischer, Brian R. Baer et al. · Journal of Medicinal Chemistry · 2020 · 559 citations · Full text

Discovery of (<i>S</i>)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1<i>H</i>-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1<i>H</i>)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development

James F. Blake, Michael Burkard, Jocelyn Chan et al. · Journal of Medicinal Chemistry · 2016 · 156 citations · Full text

Erk Kinase Activity, Cellular Pharmacology, Tumor Biology +20

Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity

Jay B. Fell, John P. Fischer, Brian R. Baer et al. · ACS Medicinal Chemistry Letters · 2018 · 104 citations · Full text

Spirocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: From Hit to Lowering of Cerebrospinal Fluid (CSF) Amyloid β in a Higher Species

Kevin W. Hunt, Adam W. Cook, Ryan J. Watts et al. · Journal of Medicinal Chemistry · 2013 · 58 citations · Full text