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Page 1
Assessing inhibitors of mutant isocitrate dehydrogenase using a suite of pre-clinical discovery assays.
Urban DJ, Martinez NJ, Davis MI, Brimacombe KR, Cheff DM, Lee TD, Henderson MJ, Titus SA, Pragani R, Rohde JM, Liu L, Fang Y, Karavadhi S, Shah P, Lee OW, Wang A, McIver A, Zheng H, Wang X, Xu X, Jadhav A, Simeonov A, Shen M, Boxer MB, Hall MD. Urban DJ, et al. Among authors: brimacombe kr. Sci Rep. 2017 Oct 6;7(1):12758. doi: 10.1038/s41598-017-12630-x. Sci Rep. 2017. PMID: 28986582 Free PMC article.
Collateral sensitivity of multidrug-resistant cells to the orphan drug tiopronin.
Goldsborough AS, Handley MD, Dulcey AE, Pluchino KM, Kannan P, Brimacombe KR, Hall MD, Griffiths G, Gottesman MM. Goldsborough AS, et al. Among authors: brimacombe kr. J Med Chem. 2011 Jul 28;54(14):4987-97. doi: 10.1021/jm2001663. Epub 2011 Jun 24. J Med Chem. 2011. Retraction in: J Med Chem. 2020 Feb 13;63(3):1443. doi: 10.1021/acs.jmedchem.9b01794 PMID: 21657271 Free PMC article. Retracted.
Synthesis and structure-activity evaluation of isatin-β-thiosemicarbazones with improved selective activity toward multidrug-resistant cells expressing P-glycoprotein.
Hall MD, Brimacombe KR, Varonka MS, Pluchino KM, Monda JK, Li J, Walsh MJ, Boxer MB, Warren TH, Fales HM, Gottesman MM. Hall MD, et al. Among authors: brimacombe kr. J Med Chem. 2011 Aug 25;54(16):5878-89. doi: 10.1021/jm2006047. Epub 2011 Aug 1. J Med Chem. 2011. PMID: 21721528 Free PMC article.
2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase.
Walsh MJ, Brimacombe KR, Veith H, Bougie JM, Daniel T, Leister W, Cantley LC, Israelsen WJ, Vander Heiden MG, Shen M, Auld DS, Thomas CJ, Boxer MB. Walsh MJ, et al. Among authors: brimacombe kr. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6322-7. doi: 10.1016/j.bmcl.2011.08.114. Epub 2011 Sep 14. Bioorg Med Chem Lett. 2011. PMID: 21958545 Free PMC article.
HTS Assay Validation.
Iversen PW, Beck B, Chen YF, Dere W, Devanarayan V, Eastwood BJ, Farmen MW, Iturria SJ, Montrose C, Moore RA, Weidner JR, Sittampalam GS. Iversen PW, et al. 2012 May 1 [updated 2012 Oct 1]. In: Markossian S, Grossman A, Arkin M, Auld D, Austin C, Baell J, Brimacombe K, Chung TDY, Coussens NP, Dahlin JL, Devanarayan V, Foley TL, Glicksman M, Gorshkov K, Haas JV, Hall MD, Hoare S, Inglese J, Iversen PW, Lal-Nag M, Li Z, Manro JR, McGee J, McManus O, Pearson M, Riss T, Saradjian P, Sittampalam GS, Tarselli M, Trask OJ Jr, Weidner JR, Wildey MJ, Wilson K, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004–. 2012 May 1 [updated 2012 Oct 1]. In: Markossian S, Grossman A, Arkin M, Auld D, Austin C, Baell J, Brimacombe K, Chung TDY, Coussens NP, Dahlin JL, Devanarayan V, Foley TL, Glicksman M, Gorshkov K, Haas JV, Hall MD, Hoare S, Inglese J, Iversen PW, Lal-Nag M, Li Z, Manro JR, McGee J, McManus O, Pearson M, Riss T, Saradjian P, Sittampalam GS, Tarselli M, Trask OJ Jr, Weidner JR, Wildey MJ, Wilson K, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004–. PMID: 22553862 Free Books & Documents. Review.
Assay Development for Protein Kinase Enzymes.
Glickman JF. Glickman JF. 2012 May 1 [updated 2012 Oct 1]. In: Markossian S, Grossman A, Arkin M, Auld D, Austin C, Baell J, Brimacombe K, Chung TDY, Coussens NP, Dahlin JL, Devanarayan V, Foley TL, Glicksman M, Gorshkov K, Haas JV, Hall MD, Hoare S, Inglese J, Iversen PW, Lal-Nag M, Li Z, Manro JR, McGee J, McManus O, Pearson M, Riss T, Saradjian P, Sittampalam GS, Tarselli M, Trask OJ Jr, Weidner JR, Wildey MJ, Wilson K, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004–. 2012 May 1 [updated 2012 Oct 1]. In: Markossian S, Grossman A, Arkin M, Auld D, Austin C, Baell J, Brimacombe K, Chung TDY, Coussens NP, Dahlin JL, Devanarayan V, Foley TL, Glicksman M, Gorshkov K, Haas JV, Hall MD, Hoare S, Inglese J, Iversen PW, Lal-Nag M, Li Z, Manro JR, McGee J, McManus O, Pearson M, Riss T, Saradjian P, Sittampalam GS, Tarselli M, Trask OJ Jr, Weidner JR, Wildey MJ, Wilson K, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004–. PMID: 22553863 Free Books & Documents. Review.
Receptor Binding Assays for HTS and Drug Discovery.
Auld DS, Farmen MW, Kahl SD, Kriauciunas A, McKnight KL, Montrose C, Weidner JR. Auld DS, et al. 2012 May 1 [updated 2018 Jul 1]. In: Markossian S, Grossman A, Arkin M, Auld D, Austin C, Baell J, Brimacombe K, Chung TDY, Coussens NP, Dahlin JL, Devanarayan V, Foley TL, Glicksman M, Gorshkov K, Haas JV, Hall MD, Hoare S, Inglese J, Iversen PW, Lal-Nag M, Li Z, Manro JR, McGee J, McManus O, Pearson M, Riss T, Saradjian P, Sittampalam GS, Tarselli M, Trask OJ Jr, Weidner JR, Wildey MJ, Wilson K, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004–. 2012 May 1 [updated 2018 Jul 1]. In: Markossian S, Grossman A, Arkin M, Auld D, Austin C, Baell J, Brimacombe K, Chung TDY, Coussens NP, Dahlin JL, Devanarayan V, Foley TL, Glicksman M, Gorshkov K, Haas JV, Hall MD, Hoare S, Inglese J, Iversen PW, Lal-Nag M, Li Z, Manro JR, McGee J, McManus O, Pearson M, Riss T, Saradjian P, Sittampalam GS, Tarselli M, Trask OJ Jr, Weidner JR, Wildey MJ, Wilson K, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004–. PMID: 22553864 Free Books & Documents. Review.
107 results