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Page 1
Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1).
Yang SM, Yasgar A, Miller B, Lal-Nag M, Brimacombe K, Hu X, Sun H, Wang A, Xu X, Nguyen K, Oppermann U, Ferrer M, Vasiliou V, Simeonov A, Jadhav A, Maloney DJ. Yang SM, et al. Among authors: brimacombe k. J Med Chem. 2015 Aug 13;58(15):5967-78. doi: 10.1021/acs.jmedchem.5b00577. Epub 2015 Jul 24. J Med Chem. 2015. PMID: 26207746 Free PMC article.
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.
Inhibition of Protein-Protein Interactions: Non-Cellular Assay Formats.
Arkin MR, Glicksman MA, Fu H, Havel JJ, Du Y. Arkin MR, et al. 2012 Mar 18 [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 Mar 18 [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: 22553871 Free Books & Documents. Review.
Identification of ML251, a Potent Inhibitor of T. brucei and T. cruzi Phosphofructokinase.
Brimacombe KR, Walsh MJ, Liu L, Vásquez-Valdivieso MG, Morgan HP, McNae I, Fothergill-Gilmore LA, Michels PA, Auld DS, Simeonov A, Walkinshaw MD, Shen M, Boxer MB. Brimacombe KR, et al. ACS Med Chem Lett. 2013 Oct 30;5(1):12-7. doi: 10.1021/ml400259d. eCollection 2014 Jan 9. ACS Med Chem Lett. 2013. PMID: 24900769 Free PMC article.
Structure activity relationships of human galactokinase inhibitors.
Liu L, Tang M, Walsh MJ, Brimacombe KR, Pragani R, Tanega C, Rohde JM, Baker HL, Fernandez E, Blackman B, Bougie JM, Leister WH, Auld DS, Shen M, Lai K, Boxer MB. Liu L, et al. Among authors: brimacombe kr. Bioorg Med Chem Lett. 2015 Feb 1;25(3):721-7. doi: 10.1016/j.bmcl.2014.11.061. Epub 2014 Dec 13. Bioorg Med Chem Lett. 2015. PMID: 25553891
Assay Interference by Chemical Reactivity.
Dahlin JL, Baell J, Walters MA. Dahlin JL, et al. 2015 Sep 18. 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–. 2015 Sep 18. 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: 26561694 Free Books & Documents. Review.
In Vitro and In Vivo Assessment of ADME and PK Properties During Lead Selection and Lead Optimization – Guidelines, Benchmarks and Rules of Thumb.
Chung TDY, Terry DB, Smith LH. Chung TDY, et al. 2015 Sep 9. 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–. 2015 Sep 9. 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: 26561695 Free Books & Documents. Review.
A PHGDH inhibitor reveals coordination of serine synthesis and one-carbon unit fate.
Pacold ME, Brimacombe KR, Chan SH, Rohde JM, Lewis CA, Swier LJ, Possemato R, Chen WW, Sullivan LB, Fiske BP, Cho S, Freinkman E, Birsoy K, Abu-Remaileh M, Shaul YD, Liu CM, Zhou M, Koh MJ, Chung H, Davidson SM, Luengo A, Wang AQ, Xu X, Yasgar A, Liu L, Rai G, Westover KD, Vander Heiden MG, Shen M, Gray NS, Boxer MB, Sabatini DM. Pacold ME, et al. Among authors: brimacombe kr. Nat Chem Biol. 2016 Jun;12(6):452-8. doi: 10.1038/nchembio.2070. Epub 2016 Apr 25. Nat Chem Biol. 2016. PMID: 27110680 Free PMC article.
106 results