Steven Do

A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo.

James G. Christensen, Randall Schreck, Jon Burrows et al. · PubMed · 2003 · 497 citations

Cancer Biology, Tumor Biology, C-met Kinase +20

Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors

James F. Blake, Rui Xu, Josef R. Bencsik et al. · Journal of Medicinal Chemistry · 2012 · 184 citations · Full text

Human Tumors, Tumor Biology, Medicinal Chemistry +15

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

Rational Design of Phosphoinositide 3-Kinase α Inhibitors That Exhibit Selectivity over the Phosphoinositide 3-Kinase β Isoform

Timothy P. Heffron, BinQing Wei, Alan G. Olivero et al. · Journal of Medicinal Chemistry · 2011 · 70 citations · Full text

Peptide Science, Chemical Biology, Exhibit Selectivity +19