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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.
J Med Chem. 2016 Jun 23;59(12):5650-60. doi: 10.1021/acs.jmedchem.6b00389. Epub 2016 Jun 7.
J Med Chem. 2016.
PMID: 27227380
Highly potent and selective 3-N-methylquinazoline-4(3H)-one based inhibitors of B-Raf(V600E) kinase.
Wenglowsky S, Ren L, Grina J, Hansen JD, Laird ER, Moreno D, Dinkel V, Gloor SL, Hastings G, Rana S, Rasor K, Sturgis HL, Voegtli WC, Vigers G, Willis B, Mathieu S, Rudolph J.
Wenglowsky S, et al. Among authors: rasor k.
Bioorg Med Chem Lett. 2014 Apr 15;24(8):1923-7. doi: 10.1016/j.bmcl.2014.03.007. Epub 2014 Mar 13.
Bioorg Med Chem Lett. 2014.
PMID: 24675381
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Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2.
Ren L, Grina J, Moreno D, Blake JF, Gaudino JJ, Garrey R, Metcalf AT, Burkard M, Martinson M, Rasor K, Chen H, Dean B, Gould SE, Pacheco P, Shahidi-Latham S, Yin J, West K, Wang W, Moffat JG, Schwarz JB.
Ren L, et al. Among authors: rasor k.
J Med Chem. 2015 Feb 26;58(4):1976-91. doi: 10.1021/jm501921k. Epub 2015 Feb 11.
J Med Chem. 2015.
PMID: 25603482
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Potent and selective pyrazolo[1,5-a]pyrimidine based inhibitors of B-Raf(V600E) kinase with favorable physicochemical and pharmacokinetic properties.
Ren L, Laird ER, Buckmelter AJ, Dinkel V, Gloor SL, Grina J, Newhouse B, Rasor K, Hastings G, Gradl SN, Rudolph J.
Ren L, et al. Among authors: rasor k.
Bioorg Med Chem Lett. 2012 Jan 15;22(2):1165-8. doi: 10.1016/j.bmcl.2011.11.092. Epub 2011 Nov 30.
Bioorg Med Chem Lett. 2012.
PMID: 22196124
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The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase.
Ren L, Ahrendt KA, Grina J, Laird ER, Buckmelter AJ, Hansen JD, Newhouse B, Moreno D, Wenglowsky S, Dinkel V, Gloor SL, Hastings G, Rana S, Rasor K, Risom T, Sturgis HL, Voegtli WC, Mathieu S.
Ren L, et al. Among authors: rasor k.
Bioorg Med Chem Lett. 2012 May 15;22(10):3387-91. doi: 10.1016/j.bmcl.2012.04.015. Epub 2012 Apr 10.
Bioorg Med Chem Lett. 2012.
PMID: 22534450
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