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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Lee KL, Ambler CM, Anderson DR, Boscoe BP, Bree AG, Brodfuehrer JI, Chang JS, Choi C, Chung S, Curran KJ, Day JE, Dehnhardt CM, Dower K, Drozda SE, Frisbie RK, Gavrin LK, Goldberg JA, Han S, Hegen M, Hepworth D, Hope HR, Kamtekar S, Kilty IC, Lee A, Lin LL, Lovering FE, Lowe MD, Mathias JP, Morgan HM, Murphy EA, Papaioannou N, Patny A, Pierce BS, Rao VR, Saiah E, Samardjiev IJ, Samas BM, Shen MWH, Shin JH, Soutter HH, Strohbach JW, Symanowicz PT, Thomason JR, Trzupek JD, Vargas R, Vincent F, Yan J, Zapf CW, Wright SW. Lee KL, et al. Among authors: yan j. J Med Chem. 2017 Jul 13;60(13):5521-5542. doi: 10.1021/acs.jmedchem.7b00231. Epub 2017 Jun 14. J Med Chem. 2017. PMID: 28498658
Discovery of Potent and Orally Bioavailable Macrocyclic Peptide-Peptoid Hybrid CXCR7 Modulators.
Boehm M, Beaumont K, Jones R, Kalgutkar AS, Zhang L, Atkinson K, Bai G, Brown JA, Eng H, Goetz GH, Holder BR, Khunte B, Lazzaro S, Limberakis C, Ryu S, Shapiro MJ, Tylaska L, Yan J, Turner R, Leung SSF, Ramaseshan M, Price DA, Liras S, Jacobson MP, Earp DJ, Lokey RS, Mathiowetz AM, Menhaji-Klotz E. Boehm M, et al. Among authors: yan j. J Med Chem. 2017 Dec 14;60(23):9653-9663. doi: 10.1021/acs.jmedchem.7b01028. Epub 2017 Oct 30. J Med Chem. 2017. PMID: 29045152 Free article.
Design and optimization of selective azaindole amide M1 positive allosteric modulators.
Davoren JE, O'Neil SV, Anderson DP, Brodney MA, Chenard L, Dlugolenski K, Edgerton JR, Green M, Garnsey M, Grimwood S, Harris AR, Kauffman GW, LaChapelle E, Lazzaro JT, Lee CW, Lotarski SM, Nason DM, Obach RS, Reinhart V, Salomon-Ferrer R, Steyn SJ, Webb D, Yan J, Zhang L. Davoren JE, et al. Among authors: yan j. Bioorg Med Chem Lett. 2016 Jan 15;26(2):650-655. doi: 10.1016/j.bmcl.2015.11.053. Epub 2015 Nov 17. Bioorg Med Chem Lett. 2016. PMID: 26631313
Intramolecular Ring-Opening Decomposition of Aryl Azetidines.
Bai G, O'Connell TN, Brodney MA, Butler CR, Czabaniuk LC, Gilbert AM, LaChapelle EA, Li C, McAllister LA, Ogilvie K, Philippe L, Salomon-Ferrer R, Shapiro MJ, Starr JT, Uccello DP, Withka JM, Yan J, Brown MF. Bai G, et al. Among authors: yan j. ACS Med Chem Lett. 2021 Sep 30;12(10):1585-1588. doi: 10.1021/acsmedchemlett.1c00402. eCollection 2021 Oct 14. ACS Med Chem Lett. 2021. PMID: 34676040 Free PMC article.
Discovery of a Selective Covalent Inhibitor of Lysophospholipase-like 1 (LYPLAL1) as a Tool to Evaluate the Role of this Serine Hydrolase in Metabolism.
Ahn K, Boehm M, Brown MF, Calloway J, Che Y, Chen J, Fennell KF, Geoghegan KF, Gilbert AM, Gutierrez JA, Kalgutkar AS, Lanba A, Limberakis C, Magee TV, O'Doherty I, Oliver R, Pabst B, Pandit J, Parris K, Pfefferkorn JA, Rolph TP, Patel R, Schuff B, Shanmugasundaram V, Starr JT, Varghese AH, Vera NB, Vernochet C, Yan J. Ahn K, et al. Among authors: yan j. ACS Chem Biol. 2016 Sep 16;11(9):2529-40. doi: 10.1021/acschembio.6b00266. Epub 2016 Jul 19. ACS Chem Biol. 2016. PMID: 27391855
The hepatoselective glucokinase activator PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats.
Erion DM, Lapworth A, Amor PA, Bai G, Vera NB, Clark RW, Yan Q, Zhu Y, Ross TT, Purkal J, Gorgoglione M, Zhang G, Bonato V, Baker L, Barucci N, D'Aquila T, Robertson A, Aiello RJ, Yan J, Trimmer J, Rolph TP, Pfefferkorn JA. Erion DM, et al. Among authors: yan q, yan j. PLoS One. 2014 May 23;9(5):e97139. doi: 10.1371/journal.pone.0097139. eCollection 2014. PLoS One. 2014. PMID: 24858947 Free PMC article.
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