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31 results

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Page 1
Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases.
Gerstenberger BS, Ambler C, Arnold EP, Banker ME, Brown MF, Clark JD, Dermenci A, Dowty ME, Fensome A, Fish S, Hayward MM, Hegen M, Hollingshead BD, Knafels JD, Lin DW, Lin TH, Owen DR, Saiah E, Sharma R, Vajdos FF, Xing L, Yang X, Yang X, Wright SW. Gerstenberger BS, et al. Among authors: knafels jd. J Med Chem. 2020 Nov 25;63(22):13561-13577. doi: 10.1021/acs.jmedchem.0c00948. Epub 2020 Aug 25. J Med Chem. 2020. PMID: 32787094
Potent inhibitors of LpxC for the treatment of Gram-negative infections.
Brown MF, Reilly U, Abramite JA, Arcari JT, Oliver R, Barham RA, Che Y, Chen JM, Collantes EM, Chung SW, Desbonnet C, Doty J, Doroski M, Engtrakul JJ, Harris TM, Huband M, Knafels JD, Leach KL, Liu S, Marfat A, Marra A, McElroy E, Melnick M, Menard CA, Montgomery JI, Mullins L, Noe MC, O'Donnell J, Penzien J, Plummer MS, Price LM, Shanmugasundaram V, Thoma C, Uccello DP, Warmus JS, Wishka DG. Brown MF, et al. Among authors: knafels jd. J Med Chem. 2012 Jan 26;55(2):914-23. doi: 10.1021/jm2014748. Epub 2012 Jan 11. J Med Chem. 2012. PMID: 22175825
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.
Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen J, Minich ML, Filipski KJ, Jones CS, Tu M, Aspnes G, Risley H, Bian J, Stevens BD, Bourassa P, D'Aquila T, Baker L, Barucci N, Robertson AS, Bourbonais F, Derksen DR, Macdougall M, Cabrera O, Chen J, Lapworth AL, Landro JA, Zavadoski WJ, Atkinson K, Haddish-Berhane N, Tan B, Yao L, Kosa RE, Varma MV, Feng B, Duignan DB, El-Kattan A, Murdande S, Liu S, Ammirati M, Knafels J, Dasilva-Jardine P, Sweet L, Liras S, Rolph TP. Pfefferkorn JA, et al. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections.
Montgomery JI, Brown MF, Reilly U, Price LM, Abramite JA, Arcari J, Barham R, Che Y, Chen JM, Chung SW, Collantes EM, Desbonnet C, Doroski M, Doty J, Engtrakul JJ, Harris TM, Huband M, Knafels JD, Leach KL, Liu S, Marfat A, McAllister L, McElroy E, Menard CA, Mitton-Fry M, Mullins L, Noe MC, O'Donnell J, Oliver R, Penzien J, Plummer M, Shanmugasundaram V, Thoma C, Tomaras AP, Uccello DP, Vaz A, Wishka DG. Montgomery JI, et al. Among authors: knafels jd. J Med Chem. 2012 Feb 23;55(4):1662-70. doi: 10.1021/jm2014875. Epub 2012 Feb 8. J Med Chem. 2012. PMID: 22257165
Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring.
Boys ML, Bian F, Kramer JB, Chio CL, Ren XD, Chen H, Barrett SD, Sexton KE, Iula DM, Filzen GF, Nguyen MN, Angell P, Downs VL, Wang Z, Raheja N, Ellsworth EL, Fakhoury S, Bratton LD, Keller PR, Gowan R, Drummond EM, Maiti SN, Hena MA, Lu L, McConnell P, Knafels JD, Thanabal V, Sun F, Alessi D, McCarthy A, Zhang E, Finzel BC, Patel S, Ciotti SM, Eisma R, Payne NA, Gilbertsen RB, Kostlan CR, Pocalyko DJ, Lala DS. Boys ML, et al. Among authors: knafels jd. Bioorg Med Chem Lett. 2012 May 15;22(10):3392-7. doi: 10.1016/j.bmcl.2012.04.013. Epub 2012 Apr 10. Bioorg Med Chem Lett. 2012. PMID: 22542194
Ligand-protein interactions of selective casein kinase 1δ inhibitors.
Mente S, Arnold E, Butler T, Chakrapani S, Chandrasekaran R, Cherry K, DiRico K, Doran A, Fisher K, Galatsis P, Green M, Hayward M, Humphrey J, Knafels J, Li J, Liu S, Marconi M, McDonald S, Ohren J, Paradis V, Sneed B, Walton K, Wager T. Mente S, et al. J Med Chem. 2013 Sep 12;56(17):6819-28. doi: 10.1021/jm4006324. Epub 2013 Aug 28. J Med Chem. 2013. PMID: 23919824
Siderophore receptor-mediated uptake of lactivicin analogues in gram-negative bacteria.
Starr J, Brown MF, Aschenbrenner L, Caspers N, Che Y, Gerstenberger BS, Huband M, Knafels JD, Lemmon MM, Li C, McCurdy SP, McElroy E, Rauckhorst MR, Tomaras AP, Young JA, Zaniewski RP, Shanmugasundaram V, Han S. Starr J, et al. Among authors: knafels jd. J Med Chem. 2014 May 8;57(9):3845-55. doi: 10.1021/jm500219c. Epub 2014 Apr 21. J Med Chem. 2014. PMID: 24694215
Casein kinase 1δ/ε inhibitor PF-5006739 attenuates opioid drug-seeking behavior.
Wager TT, Chandrasekaran RY, Bradley J, Rubitski D, Berke H, Mente S, Butler T, Doran A, Chang C, Fisher K, Knafels J, Liu S, Ohren J, Marconi M, DeMarco G, Sneed B, Walton K, Horton D, Rosado A, Mead A. Wager TT, et al. ACS Chem Neurosci. 2014 Dec 17;5(12):1253-65. doi: 10.1021/cn500201x. Epub 2014 Oct 28. ACS Chem Neurosci. 2014. PMID: 25299732 Clinical Trial.
Discovery of Fragment-Derived Small Molecules for in Vivo Inhibition of Ketohexokinase (KHK).
Huard K, Ahn K, Amor P, Beebe DA, Borzilleri KA, Chrunyk BA, Coffey SB, Cong Y, Conn EL, Culp JS, Dowling MS, Gorgoglione MF, Gutierrez JA, Knafels JD, Lachapelle EA, Pandit J, Parris KD, Perez S, Pfefferkorn JA, Price DA, Raymer B, Ross TT, Shavnya A, Smith AC, Subashi TA, Tesz GJ, Thuma BA, Tu M, Weaver JD, Weng Y, Withka JM, Xing G, Magee TV. Huard K, et al. Among authors: knafels jd. J Med Chem. 2017 Sep 28;60(18):7835-7849. doi: 10.1021/acs.jmedchem.7b00947. Epub 2017 Sep 11. J Med Chem. 2017. PMID: 28853885
Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase.
Butler CR, Beck EM, Harris A, Huang Z, McAllister LA, Am Ende CW, Fennell K, Foley TL, Fonseca K, Hawrylik SJ, Johnson DS, Knafels JD, Mente S, Noell GS, Pandit J, Phillips TB, Piro JR, Rogers BN, Samad TA, Wang J, Wan S, Brodney MA. Butler CR, et al. Among authors: knafels jd. J Med Chem. 2017 Dec 14;60(23):9860-9873. doi: 10.1021/acs.jmedchem.7b01531. Epub 2017 Dec 5. J Med Chem. 2017. PMID: 29148769
31 results