Publications by authors named "Kirk Robarge"

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Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.
BinQing Wei, Kirk Robarge, Sharada S Labadie, Jinhua Chen, Laura B Corson

Bioorg Med Chem Lett· March 2022

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Metabolic plasticity underpins innate and acquired resistance to LDHA inhibition.
Aaron Boudreau, Hans E Purkey, Anna Hitz, Kirk Robarge, David Peterson

Nat Chem Biol· October 2016

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Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in Mice.
Hans E Purkey, Kirk Robarge, Jinhua Chen, Zhongguo Chen, Laura B Corson

ACS Med Chem Lett· October 2016

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Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development.
James F Blake, Michael Burkard, Jocelyn Chan, Huifen Chen, Kang-Jye Chou, Kirk Robarge

J Med Chem· June 2016

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Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.
Benjamin P Fauber, Alberto Gobbi, Kirk Robarge, Aihe Zhou, Adrian Barnard

Bioorg Med Chem Lett· August 2015

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Optimization of 5-(2,6-dichlorophenyl)-3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
Sharada Labadie, Peter S Dragovich, Jinhua Chen, Benjamin P Fauber, Jason Boggs, Kirk Robarge

Bioorg Med Chem Lett· January 2015

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Identification of 3,6-disubstituted dihydropyrones as inhibitors of human lactate dehydrogenase.
Benjamin P Fauber, Peter S Dragovich, Jinhua Chen, Laura B Corson, Charles Z Ding, Kirk Robarge

Bioorg Med Chem Lett· December 2014

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Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479.
Kirk D Robarge, Wendy Lee, Charles Eigenbrot, Mark Ultsch, Christian Wiesmann

Bioorg Med Chem Lett· October 2014

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Discovery and preclinical development of vismodegib.
Stephen E Gould, Jennifer A Low, James C Marsters, Kirk Robarge, Lee L Rubin

Expert Opin Drug Discov· August 2014

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Identification of substituted 3-hydroxy-2-mercaptocyclohex-2-enones as potent inhibitors of human lactate dehydrogenase.
Peter S Dragovich, Benjamin P Fauber, Jason Boggs, Jinhua Chen, Laura B Corson, Kirk Robarge

Bioorg Med Chem Lett· August 2014

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A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors.
Wendy Lee, Daniel F Ortwine, Philippe Bergeron, Kevin Lau, Lichuan Lin, Kirk D Robarge

Bioorg Med Chem Lett· September 2013

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Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions.
Edna F Choo, Marcia Belvin, Jason Boggs, Yuzhong Deng, Klaus P Hoeflich, Kirk Robarge

Drug Metab Dispos· May 2012

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Potent, selective, and orally bioavailable inhibitors of mammalian target of rapamycin (mTOR) kinase based on a quaternary substituted dihydrofuropyrimidine.
Frederick Cohen, Philippe Bergeron, Elizabeth Blackwood, Krista K Bowman, Huifen Chen, Kirk D Robarge

J Med Chem· May 2011

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Small molecule inhibition of GDC-0449 refractory smoothened mutants and downstream mechanisms of drug resistance.
Gerrit J P Dijkgraaf, Bruno Alicke, Lasse Weinmann, Thomas Januario, Kristina West, Kirk Robarge

Cancer Res· January 2011

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Preclinical disposition and pharmacokinetics-pharmacodynamic modeling of biomarker response and tumour growth inhibition in xenograft mouse models of G-573, a MEK inhibitor.
Edna F Choo, Marcia Belvin, Jocelyn Chan, Klaus Hoeflich, Christine Orr, Kirk Robarge

Xenobiotica· November 2010

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Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway.
Georgette M Castanedo, Shumei Wang, Kirk D Robarge, Elizabeth Blackwood, Daniel Burdick

Bioorg Med Chem Lett· November 2010

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GDC-0449-a potent inhibitor of the hedgehog pathway.
Kirk D Robarge, Shirley A Brunton, Georgette M Castanedo, Yong Cui, Michael S Dina

Bioorg Med Chem Lett· October 2009

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A selective, slow binding inhibitor of factor VIIa binds to a nonstandard active site conformation and attenuates thrombus formation in vivo.
Alan G Olivero, Charles Eigenbrot, Richard Goldsmith, Kirk Robarge, Dean R Artis

J Biol Chem· March 2005

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