Steve Price

Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers

Georgia Hatzivassiliou, Jacob R. Haling, Huifen Chen et al. · Nature · 2013 · 317 citations

Oncology, Medicine, Receptor Tyrosine Kinase +6

Discovery of 2-{3-[2-(1-Isopropyl-3-methyl-1<i>H</i>-1,2–4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-<i>d</i>][1,4]oxazepin-9-yl]-1<i>H</i>-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): A β-Sparing Phosphoinositide 3-Kinase Inhibitor with High Unbound Exposure and Robust in Vivo Antitumor Activity

Chudi Ndubaku, Timothy P. Heffron, Steven T. Staben et al. · Journal of Medicinal Chemistry · 2013 · 174 citations · Full text

Drug Target, Unbound Drug Exposure, Pharmacotherapy +21

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of ( <i>S</i> )-2-((2-(1-Isopropyl-1 <i>H</i> -1,2,4-triazol-5-yl)-5,6-dihydrobenzo[ <i>f</i> ]imidazo[1,2- <i>d</i> ][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326)

Timothy P. Heffron, Robert A. Heald, Chudi Ndubaku et al. · Journal of Medicinal Chemistry · 2016 · 102 citations · Full text

Discovery of Novel PI3-Kinase δ Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition

Brian S. Safina, Stewart Baker, Matt Baumgardner et al. · Journal of Medicinal Chemistry · 2012 · 66 citations · Full text

Drug Target, Immunology, Inflammatory Arthritis +25

Potent and selective inhibitors of PI3Kδ: Obtaining isoform selectivity from the affinity pocket and tryptophan shelf

Daniel P. Sutherlin, Stewart Baker, Angelina Bisconte et al. · Bioorganic & Medicinal Chemistry Letters · 2012 · 50 citations · Full text

Biochemistry, Functional Selectivity, Medicine +8