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Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide).
Johnson HWB, Lowe E, Anderl JL, Fan A, Muchamuel T, Bowers S, Moebius DC, Kirk C, McMinn DL. Johnson HWB, et al. J Med Chem. 2018 Dec 27;61(24):11127-11143. doi: 10.1021/acs.jmedchem.8b01201. Epub 2018 Dec 11. J Med Chem. 2018. PMID: 30380863
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors.
Leahy JW, Buhr CA, Johnson HW, Kim BG, Baik T, Cannoy J, Forsyth TP, Jeong JW, Lee MS, Ma S, Noson K, Wang L, Williams M, Nuss JM, Brooks E, Foster P, Goon L, Heald N, Holst C, Jaeger C, Lam S, Lougheed J, Nguyen L, Plonowski A, Song J, Stout T, Wu X, Yakes MF, Yu P, Zhang W, Lamb P, Raeber O. Leahy JW, et al. J Med Chem. 2012 Jun 14;55(11):5467-82. doi: 10.1021/jm300403a. Epub 2012 May 17. J Med Chem. 2012. PMID: 22548342
SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors.
Forsyth T, Kearney PC, Kim BG, Johnson HW, Aay N, Arcalas A, Brown DS, Chan V, Chen J, Du H, Epshteyn S, Galan AA, Huynh TP, Ibrahim MA, Kane B, Koltun ES, Mann G, Meyr LE, Lee MS, Lewis GL, Noguchi RT, Pack M, Ridgway BH, Shi X, Takeuchi CS, Zu P, Leahy JW, Nuss JM, Aoyama R, Engst S, Gendreau SB, Kassees R, Li J, Lin SH, Martini JF, Stout T, Tong P, Woolfrey J, Zhang W, Yu P. Forsyth T, et al. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8. doi: 10.1016/j.bmcl.2012.10.007. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2012. PMID: 23127890
Discovery of a novel class of potent and orally bioavailable sphingosine 1-phosphate receptor 1 antagonists.
Ibrahim MA, Johnson HW, Jeong JW, Lewis GL, Shi X, Noguchi RT, Williams M, Leahy JW, Nuss JM, Woolfrey J, Banica M, Bentzien F, Chou YC, Gibson A, Heald N, Lamb P, Mattheakis L, Matthews D, Shipway A, Wu X, Zhang W, Zhou S, Shankar G. Ibrahim MA, et al. J Med Chem. 2012 Feb 9;55(3):1368-81. doi: 10.1021/jm201533b. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22214363
Discovery of a novel class of highly potent, selective, ATP-competitive, and orally bioavailable inhibitors of the mammalian target of rapamycin (mTOR).
Takeuchi CS, Kim BG, Blazey CM, Ma S, Johnson HW, Anand NK, Arcalas A, Baik TG, Buhr CA, Cannoy J, Epshteyn S, Joshi A, Lara K, Lee MS, Wang L, Leahy JW, Nuss JM, Aay N, Aoyama R, Foster P, Lee J, Lehoux I, Munagala N, Plonowski A, Rajan S, Woolfrey J, Yamaguchi K, Lamb P, Miller N. Takeuchi CS, et al. J Med Chem. 2013 Mar 28;56(6):2218-34. doi: 10.1021/jm3007933. Epub 2013 Mar 7. J Med Chem. 2013. PMID: 23394126
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