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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: murphy ea. 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
Identification and optimization of indolo[2,3-c]quinoline inhibitors of IRAK4.
Tumey LN, Boschelli DH, Bhagirath N, Shim J, Murphy EA, Goodwin D, Bennett EM, Wang M, Lin LL, Press B, Shen M, Frisbie RK, Morgan P, Mohan S, Shin J, Rao VR. Tumey LN, et al. Among authors: murphy ea. Bioorg Med Chem Lett. 2014 May 1;24(9):2066-72. doi: 10.1016/j.bmcl.2014.03.056. Epub 2014 Mar 29. Bioorg Med Chem Lett. 2014. PMID: 24726805
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD. McKew JC, et al. Among authors: murphy ea. J Med Chem. 2008 Jun 26;51(12):3388-413. doi: 10.1021/jm701467e. Epub 2008 May 23. J Med Chem. 2008. PMID: 18498150
Design of potent and selective GPR119 agonists for type II diabetes.
Szewczyk JW, Acton J, Adams AD, Chicchi G, Freeman S, Howard AD, Huang Y, Li C, Meinke PT, Mosely R, Murphy E, Samuel R, Santini C, Yang M, Zhang Y, Zhao K, Wood HB. Szewczyk JW, et al. Bioorg Med Chem Lett. 2011 May 1;21(9):2665-9. doi: 10.1016/j.bmcl.2010.12.086. Epub 2010 Dec 22. Bioorg Med Chem Lett. 2011. PMID: 21273063
Synovial fibroblast gene expression is associated with sensory nerve growth and pain in rheumatoid arthritis.
Bai Z, Bartelo N, Aslam M, Murphy EA, Hale CR, Blachere NE, Parveen S, Spolaore E, DiCarlo E, Gravallese EM, Smith MH; Accelerating Medicines Partnership RA/SLE Network; Frank MO, Jiang CS, Zhang H, Pyrgaki C, Lewis MJ, Sikandar S, Pitzalis C, Lesnak JB, Mazhar K, Price TJ, Malfait AM, Miller RE, Zhang F, Goodman S, Darnell RB, Wang F, Orange DE. Bai Z, et al. Among authors: murphy ea. Sci Transl Med. 2024 Apr 10;16(742):eadk3506. doi: 10.1126/scitranslmed.adk3506. Epub 2024 Apr 10. Sci Transl Med. 2024. PMID: 38598614
505 results