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Identification of imidazo[1,2-b]pyridazine TYK2 pseudokinase ligands as potent and selective allosteric inhibitors of TYK2 signalling.
Moslin R, Gardner D, Santella J, Zhang Y, Duncia JV, Liu C, Lin J, Tokarski JS, Strnad J, Pedicord D, Chen J, Blat Y, Zupa-Fernandez A, Cheng L, Sun H, Chaudhry C, Huang C, D'Arienzo C, Sack JS, Muckelbauer JK, Chang C, Tredup J, Xie D, Aranibar N, Burke JR, Carter PH, Weinstein DS. Moslin R, et al. Among authors: sack js. Medchemcomm. 2016 Dec 15;8(4):700-712. doi: 10.1039/c6md00560h. eCollection 2017 Apr 1. Medchemcomm. 2016. PMID: 30108788 Free PMC article.
Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities.
Kim KS, Zhang L, Schmidt R, Cai ZW, Wei D, Williams DK, Lombardo LJ, Trainor GL, Xie D, Zhang Y, An Y, Sack JS, Tokarski JS, Darienzo C, Kamath A, Marathe P, Zhang Y, Lippy J, Jeyaseelan R Sr, Wautlet B, Henley B, Gullo-Brown J, Manne V, Hunt JT, Fargnoli J, Borzilleri RM. Kim KS, et al. Among authors: sack js. J Med Chem. 2008 Sep 11;51(17):5330-41. doi: 10.1021/jm800476q. Epub 2008 Aug 9. J Med Chem. 2008. PMID: 18690676
Pyrazole and pyrimidine phenylacylsulfonamides as dual Bcl-2/Bcl-xL antagonists.
Schroeder GM, Wei D, Banfi P, Cai ZW, Lippy J, Menichincheri M, Modugno M, Naglich J, Penhallow B, Perez HL, Sack J, Schmidt RJ, Tebben A, Yan C, Zhang L, Galvani A, Lombardo LJ, Borzilleri RM. Schroeder GM, et al. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3951-6. doi: 10.1016/j.bmcl.2012.04.106. Epub 2012 Apr 30. Bioorg Med Chem Lett. 2012. PMID: 22608393
Discovery of 7-(3-(piperazin-1-yl)phenyl)pyrrolo[2,1-f][1,2,4]triazin-4-amine derivatives as highly potent and selective PI3Kδ inhibitors.
Qin LY, Ruan Z, Cherney RJ, Dhar TGM, Neels J, Weigelt CA, Sack JS, Srivastava AS, Cornelius LAM, Tino JA, Stefanski K, Gu X, Xie J, Susulic V, Yang X, Yarde-Chinn M, Skala S, Bosnius R, Goldstein C, Davies P, Ruepp S, Salter-Cid L, Bhide RS, Poss MA. Qin LY, et al. Among authors: sack js. Bioorg Med Chem Lett. 2017 Feb 15;27(4):855-861. doi: 10.1016/j.bmcl.2017.01.016. Epub 2017 Jan 10. Bioorg Med Chem Lett. 2017. PMID: 28108251
116 results