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Pyrrolamide DNA gyrase inhibitors: fragment-based nuclear magnetic resonance screening to identify antibacterial agents.
Eakin AE, Green O, Hales N, Walkup GK, Bist S, Singh A, Mullen G, Bryant J, Embrey K, Gao N, Breeze A, Timms D, Andrews B, Uria-Nickelsen M, Demeritt J, Loch JT 3rd, Hull K, Blodgett A, Illingworth RN, Prince B, Boriack-Sjodin PA, Hauck S, MacPherson LJ, Ni H, Sherer B. Eakin AE, et al. Among authors: sherer b. Antimicrob Agents Chemother. 2012 Mar;56(3):1240-6. doi: 10.1128/AAC.05485-11. Epub 2011 Dec 19. Antimicrob Agents Chemother. 2012. PMID: 22183167 Free PMC article.
Pyrrolamide DNA gyrase inhibitors: optimization of antibacterial activity and efficacy.
Sherer BA, Hull K, Green O, Basarab G, Hauck S, Hill P, Loch JT 3rd, Mullen G, Bist S, Bryant J, Boriack-Sjodin A, Read J, DeGrace N, Uria-Nickelsen M, Illingworth RN, Eakin AE. Sherer BA, et al. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7416-20. doi: 10.1016/j.bmcl.2011.10.010. Epub 2011 Oct 12. Bioorg Med Chem Lett. 2011. PMID: 22041057
Discovery of Evobrutinib: An Oral, Potent, and Highly Selective, Covalent Bruton's Tyrosine Kinase (BTK) Inhibitor for the Treatment of Immunological Diseases.
Caldwell RD, Qiu H, Askew BC, Bender AT, Brugger N, Camps M, Dhanabal M, Dutt V, Eichhorn T, Gardberg AS, Goutopoulos A, Grenningloh R, Head J, Healey B, Hodous BL, Huck BR, Johnson TL, Jones C, Jones RC, Mochalkin I, Morandi F, Nguyen N, Meyring M, Potnick JR, Santos DC, Schmidt R, Sherer B, Shutes A, Urbahns K, Follis AV, Wegener AA, Zimmerli SC, Liu-Bujalski L. Caldwell RD, et al. Among authors: sherer b. J Med Chem. 2019 Sep 12;62(17):7643-7655. doi: 10.1021/acs.jmedchem.9b00794. Epub 2019 Aug 15. J Med Chem. 2019. PMID: 31368705
Identification of Clinical Candidate M2698, a Dual p70S6K and Akt Inhibitor, for Treatment of PAM Pathway-Altered Cancers.
DeSelm L, Huck B, Lan R, Neagu C, Potnick J, Xiao Y, Chen X, Jones R, Richardson TE, Heasley BH, Haxell T, Moore J, Tian H, Georgi K, Rohdich F, Sutton A, Johnson T, Mochalkin I, Jackson J, Lin J, Crowley L, Machl A, Clark A, Wilker E, Sherer B, Goutopoulos A. DeSelm L, et al. Among authors: sherer b. J Med Chem. 2021 Oct 14;64(19):14603-14619. doi: 10.1021/acs.jmedchem.1c01087. Epub 2021 Oct 1. J Med Chem. 2021. PMID: 34596404
Discovery of potent and selective reversible Bruton's tyrosine kinase inhibitors.
Qiu H, Ali Z, Bender A, Caldwell R, Chen YY, Fang Z, Gardberg A, Glaser N, Goettsche A, Goutopoulos A, Grenningloh R, Hanschke B, Head J, Johnson T, Jones C, Jones R, Kulkarni S, Maurer C, Morandi F, Neagu C, Poetzsch S, Potnick J, Schmidt R, Roe K, Viacava Follis A, Wing C, Zhu X, Sherer B. Qiu H, et al. Among authors: sherer b. Bioorg Med Chem. 2021 Jun 15;40:116163. doi: 10.1016/j.bmc.2021.116163. Epub 2021 Apr 20. Bioorg Med Chem. 2021. PMID: 33932711
Optimization of the efflux ratio and permeability of covalent irreversible BTK inhibitors.
Qiu H, Liu-Bujalski L, Caldwell RD, Viacava Follis A, Gardberg A, Goutopoulos A, Grenningloh R, Head J, Johnson T, Jones CCV, Jones R, Mochalkin I, Morandi F, Neagu C, Potnick J, Sherer B. Qiu H, et al. Among authors: sherer b. Bioorg Med Chem Lett. 2018 Nov 1;28(20):3307-3311. doi: 10.1016/j.bmcl.2018.09.018. Epub 2018 Sep 15. Bioorg Med Chem Lett. 2018. PMID: 30243592
62 results