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A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors.
Tucker TJ, Embrey MW, Alleyne C, Amin RP, Bass A, Bhatt B, Bianchi E, Branca D, Bueters T, Buist N, Ha SN, Hafey M, He H, Higgins J, Johns DG, Kerekes AD, Koeplinger KA, Kuethe JT, Li N, Murphy B, Orth P, Salowe S, Shahripour A, Tracy R, Wang W, Wu C, Xiong Y, Zokian HJ, Wood HB, Walji A. Tucker TJ, et al. Among authors: murphy b. J Med Chem. 2021 Nov 25;64(22):16770-16800. doi: 10.1021/acs.jmedchem.1c01599. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34704436
Series of Novel and Highly Potent Cyclic Peptide PCSK9 Inhibitors Derived from an mRNA Display Screen and Optimized via Structure-Based Design.
Alleyne C, Amin RP, Bhatt B, Bianchi E, Blain JC, Boyer N, Branca D, Embrey MW, Ha SN, Jette K, Johns DG, Kerekes AD, Koeplinger KA, LaPlaca D, Li N, Murphy B, Orth P, Ricardo A, Salowe S, Seyb K, Shahripour A, Stringer JR, Sun Y, Tracy R, Wu C, Xiong Y, Youm H, Zokian HJ, Tucker TJ. Alleyne C, et al. Among authors: murphy b. J Med Chem. 2020 Nov 25;63(22):13796-13824. doi: 10.1021/acs.jmedchem.0c01084. Epub 2020 Nov 10. J Med Chem. 2020. PMID: 33170686
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
Vachal P, Duffy JL, Campeau LC, Amin RP, Mitra K, Murphy BA, Shao PP, Sinclair PJ, Ye F, Katipally R, Lu Z, Ondeyka D, Chen YH, Zhao K, Sun W, Tyagarajan S, Bao J, Wang SP, Cote J, Lipardi C, Metzger D, Leung D, Hartmann G, Wollenberg GK, Liu J, Tan L, Xu Y, Chen Q, Liu G, Blaustein RO, Johns DG. Vachal P, et al. J Med Chem. 2021 Sep 23;64(18):13215-13258. doi: 10.1021/acs.jmedchem.1c00959. Epub 2021 Aug 10. J Med Chem. 2021. PMID: 34375108
Discovery of Novel Indoline Cholesterol Ester Transfer Protein Inhibitors (CETP) through a Structure-Guided Approach.
Wilson JE, Kurukulasuriya R, Reibarkh M, Reiter M, Zwicker A, Zhao K, Zhang F, Anand R, Colandrea VJ, Cumiskey AM, Crespo A, Duffy RA, Murphy BA, Mitra K, Johns DG, Duffy JL, Vachal P. Wilson JE, et al. ACS Med Chem Lett. 2016 Jan 4;7(3):261-5. doi: 10.1021/acsmedchemlett.5b00404. eCollection 2016 Mar 10. ACS Med Chem Lett. 2016. PMID: 26985312 Free PMC article.
Optimization of Preclinical Metabolism for Somatostatin Receptor Subtype 5-Selective Antagonists.
Liu W, Hussain Z, Zang Y, Sweis RF, Romero FA, Finke PE, Moningka R, Bao J, Plotkin MA, Shang J, Dingley KH, Salituro G, Murphy BA, Howard AD, Ujjainwalla F, Wood HB, Duffy JL. Liu W, et al. Among authors: murphy ba. ACS Med Chem Lett. 2018 Oct 5;9(11):1088-1093. doi: 10.1021/acsmedchemlett.8b00306. eCollection 2018 Nov 8. ACS Med Chem Lett. 2018. PMID: 30429950 Free PMC article.
Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety.
He S, Hong Q, Lai Z, Wu Z, Yu Y, Kim DW, Ting PC, Kuethe JT, Yang GX, Jian T, Liu J, Guiadeen D, Krikorian AD, Sperbeck DM, Sonatore LM, Wiltsie J, Chung CC, Gibson JT, Lisnock J, Murphy BA, Gorski JN, Liu J, Chen D, Chen X, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ. He S, et al. ACS Med Chem Lett. 2013 Jun 6;4(8):773-8. doi: 10.1021/ml400168h. eCollection 2013 Aug 8. ACS Med Chem Lett. 2013. PMID: 24900745 Free PMC article.
Discovery and Pharmacology of a Novel Class of Diacylglycerol Acyltransferase 2 Inhibitors.
Imbriglio JE, Shen DM, Liang R, Marby K, You M, Youm HW, Feng Z, London C, Xiong Y, Tata J, Verras A, Garcia-Calvo M, Song X, Addona GH, McLaren DG, He T, Murphy B, Metzger DE, Salituro G, Deckman D, Chen Q, Jin X, Stout SJ, Wang SP, Wilsie L, Palyha O, Han S, Hubbard BK, Previs SF, Pinto S, Taggart A. Imbriglio JE, et al. Among authors: murphy b. J Med Chem. 2015 Dec 10;58(23):9345-53. doi: 10.1021/acs.jmedchem.5b01345. Epub 2015 Nov 20. J Med Chem. 2015. PMID: 26561979
Benzimidazole-based DGAT1 inhibitors with a [3.1.0] bicyclohexane carboxylic acid moiety.
He S, Lai Z, Hong Q, Shang J, Reibarkh M, Kuethe JT, Liu J, Guiadeen D, Krikorian AD, Cernak TA, Dykstra KD, Sperbeck DM, Wu Z, Yu Y, Yang GX, Jian T, Verras A, Sonatore LM, Wiltsie J, Chung CC, Murphy BA, Gorski JN, Liu J, Xiao J, Wolff M, Tong SX, Madeira M, Karanam BV, Shen DM, Balkovec JM, Pinto S, Nargund RP, DeVita RJ. He S, et al. Bioorg Med Chem Lett. 2019 May 15;29(10):1182-1186. doi: 10.1016/j.bmcl.2019.03.025. Epub 2019 Mar 21. Bioorg Med Chem Lett. 2019. PMID: 30926247
Microscale High-Throughput Experimentation as an Enabling Technology in Drug Discovery: Application in the Discovery of (Piperidinyl)pyridinyl-1H-benzimidazole Diacylglycerol Acyltransferase 1 Inhibitors.
Cernak T, Gesmundo NJ, Dykstra K, Yu Y, Wu Z, Shi ZC, Vachal P, Sperbeck D, He S, Murphy BA, Sonatore L, Williams S, Madeira M, Verras A, Reiter M, Lee CH, Cuff J, Sherer EC, Kuethe J, Goble S, Perrotto N, Pinto S, Shen DM, Nargund R, Balkovec J, DeVita RJ, Dreher SD. Cernak T, et al. J Med Chem. 2017 May 11;60(9):3594-3605. doi: 10.1021/acs.jmedchem.6b01543. Epub 2017 Mar 2. J Med Chem. 2017. PMID: 28252959
3,135 results