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Page 1
Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors.
Lanman BA, Allen JR, Allen JG, Amegadzie AK, Ashton KS, Booker SK, Chen JJ, Chen N, Frohn MJ, Goodman G, Kopecky DJ, Liu L, Lopez P, Low JD, Ma V, Minatti AE, Nguyen TT, Nishimura N, Pickrell AJ, Reed AB, Shin Y, Siegmund AC, Tamayo NA, Tegley CM, Walton MC, Wang HL, Wurz RP, Xue M, Yang KC, Achanta P, Bartberger MD, Canon J, Hollis LS, McCarter JD, Mohr C, Rex K, Saiki AY, San Miguel T, Volak LP, Wang KH, Whittington DA, Zech SG, Lipford JR, Cee VJ. Lanman BA, et al. Among authors: pickrell aj. J Med Chem. 2020 Jan 9;63(1):52-65. doi: 10.1021/acs.jmedchem.9b01180. Epub 2019 Dec 24. J Med Chem. 2020. PMID: 31820981
Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.
Pennington LD, Croghan MD, Sham KK, Pickrell AJ, Harrington PE, Frohn MJ, Lanman BA, Reed AB, Lee MR, Xu H, McElvain M, Xu Y, Zhang X, Fiorino M, Horner M, Morrison HG, Arnett HA, Fotsch C, Tasker AS, Wong M, Cee VJ. Pennington LD, et al. Among authors: pickrell aj. Bioorg Med Chem Lett. 2012 Jan 1;22(1):527-31. doi: 10.1016/j.bmcl.2011.10.085. Epub 2011 Nov 4. Bioorg Med Chem Lett. 2012. PMID: 22104144
Synthesis and preliminary biological evaluation of potent and selective 2-(3-alkoxy-1-azetidinyl) quinolines as novel PDE10A inhibitors with improved solubility.
Rzasa RM, Frohn MJ, Andrews KL, Chmait S, Chen N, Clarine JG, Davis C, Eastwood HA, Horne DB, Hu E, Jones AD, Kaller MR, Kunz RK, Miller S, Monenschein H, Nguyen T, Pickrell AJ, Porter A, Reichelt A, Zhao X, Treanor JJS, Allen JR. Rzasa RM, et al. Among authors: pickrell aj. Bioorg Med Chem. 2014 Dec 1;22(23):6570-6585. doi: 10.1016/j.bmc.2014.10.013. Bioorg Med Chem. 2014. PMID: 25456383
Isoform-selective thiazolo[5,4-b]pyridine S1P1 agonists possessing acyclic amino carboxylate head-groups.
Reed AB, Lanman BA, Neira S, Harrington PE, Sham KK, Frohn M, Pickrell AJ, Tasker AS, Gore A, Fiorino M, Itano A, McElvain M, Middleton S, Morrison H, Xu H, Xu Y, Wong M, Cee VJ. Reed AB, et al. Among authors: pickrell aj. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1779-83. doi: 10.1016/j.bmcl.2011.12.073. Epub 2011 Dec 21. Bioorg Med Chem Lett. 2012. PMID: 22257889
The optimization of aminooxadiazoles as orally active inhibitors of Cdc7.
Harrington PE, Bourbeau MP, Fotsch C, Frohn M, Pickrell AJ, Reichelt A, Sham K, Siegmund AC, Bailis JM, Bush T, Escobar S, Hickman D, Heller S, Hsieh F, Orf JN, Rong M, San Miguel T, Tan H, Zalameda L, Allen JG. Harrington PE, et al. Among authors: pickrell aj. Bioorg Med Chem Lett. 2013 Dec 1;23(23):6396-400. doi: 10.1016/j.bmcl.2013.09.055. Epub 2013 Sep 25. Bioorg Med Chem Lett. 2013. PMID: 24120542
Discovery of AMG 369, a Thiazolo[5,4-b]pyridine Agonist of S1P1 and S1P5.
Cee VJ, Frohn M, Lanman BA, Golden J, Muller K, Neira S, Pickrell A, Arnett H, Buys J, Gore A, Fiorino M, Horner M, Itano A, Lee MR, McElvain M, Middleton S, Schrag M, Rivenzon-Segal D, Vargas HM, Xu H, Xu Y, Zhang X, Siu J, Wong M, Bürli RW. Cee VJ, et al. ACS Med Chem Lett. 2010 Dec 29;2(2):107-12. doi: 10.1021/ml100306h. eCollection 2011 Feb 10. ACS Med Chem Lett. 2010. PMID: 24900288 Free PMC article.
4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1.
Pennington LD, Sham KK, Pickrell AJ, Harrington PE, Frohn MJ, Lanman BA, Reed AB, Croghan MD, Lee MR, Xu H, McElvain M, Xu Y, Zhang X, Fiorino M, Horner M, Morrison HG, Arnett HA, Fotsch C, Wong M, Cee VJ. Pennington LD, et al. Among authors: pickrell aj. ACS Med Chem Lett. 2011 Jul 29;2(10):752-7. doi: 10.1021/ml2001399. eCollection 2011 Oct 13. ACS Med Chem Lett. 2011. PMID: 24900263 Free PMC article.
Optimization of a Potent, Orally Active S1P1 Agonist Containing a Quinolinone Core.
Harrington PE, Croghan MD, Fotsch C, Frohn M, Lanman BA, Pennington LD, Pickrell AJ, Reed AB, Sham KK, Tasker A, Arnett HA, Fiorino M, Lee MR, McElvain M, Morrison HG, Xu H, Xu Y, Zhang X, Wong M, Cee VJ. Harrington PE, et al. Among authors: pickrell aj. ACS Med Chem Lett. 2011 Nov 23;3(1):74-8. doi: 10.1021/ml200252b. eCollection 2012 Jan 12. ACS Med Chem Lett. 2011. PMID: 24900374 Free PMC article.
Novel 5- and 6-subtituted benzothiazoles with improved physicochemical properties: potent S1P₁ agonists with in vivo lymphocyte-depleting activity.
Frohn M, Cee VJ, Lanman BA, Pickrell AJ, Golden J, Rivenzon-Segal D, Middleton S, Fiorino M, Xu H, Schrag M, Xu Y, McElvain M, Muller K, Siu J, Bürli R. Frohn M, et al. Among authors: pickrell aj. Bioorg Med Chem Lett. 2012 Jan 1;22(1):628-33. doi: 10.1016/j.bmcl.2011.10.069. Epub 2011 Oct 28. Bioorg Med Chem Lett. 2012. PMID: 22100314
12 results