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Page 1
Optimization of a Novel DEL Hit That Binds in the Cbl-b SH2 Domain and Blocks Substrate Binding.
Liang J, Lambrecht MJ, Arenzana TL, Aubert-Nicol S, Bao L, Broccatelli F, Cai J, Eidenschenk C, Everett C, Garner T, Gruber F, Haghshenas P, Huestis MP, Hsu PL, Kou P, Jakalian A, Larouche-Gauthier R, Leclerc JP, Leung DH, Martin A, Murray J, Prangley M, Rutz S, Kakiuchi-Kiyota S, Satz AL, Skelton NJ, Steffek M, Stoffler D, Sudhamsu J, Tan S, Wang J, Wang S, Wang Q, Wendorff TJ, Wichert M, Yadav A, Yu C, Wang X. Liang J, et al. Among authors: murray j. ACS Med Chem Lett. 2024 May 29;15(6):864-872. doi: 10.1021/acsmedchemlett.4c00068. eCollection 2024 Jun 13. ACS Med Chem Lett. 2024. PMID: 38894924
Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma.
Bronner SM, Merrick KA, Murray J, Salphati L, Moffat JG, Pang J, Sneeringer CJ, Dompe N, Cyr P, Purkey H, Boenig GL, Li J, Kolesnikov A, Larouche-Gauthier R, Lai KW, Shen X, Aubert-Nicol S, Chen YC, Cheong J, Crawford JJ, Hafner M, Haghshenas P, Jakalian A, Leclerc JP, Lim NK, O'Brien T, Plise EG, Shalan H, Sturino C, Wai J, Xiao Y, Yin J, Zhao L, Gould S, Olivero A, Heffron TP. Bronner SM, et al. Among authors: murray j. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2294-2301. doi: 10.1016/j.bmcl.2019.06.021. Epub 2019 Jun 26. Bioorg Med Chem Lett. 2019. PMID: 31307887
Discovery of Selective Tertiary Amide Inhibitors of Cyclin-Dependent Kinase 2 (CDK2).
Zeng M, Grandner JM, Bryan MC, Verma V, Larouche-Gauthier R, Leclerc JP, Zhao L, Haghshenas P, Aubert-Nicol S, Yadav A, Ashley M, Chen JZ, Durk M, Samy KE, Nespi M, Levy E, Merrick K, Moffat JG, Murray J, Oh A, Orr C, Segal E, Sims J, Sneeringer C, Prangley M, Vartanian S, Magnuson S, Parr BT. Zeng M, et al. Among authors: murray j. ACS Med Chem Lett. 2023 Aug 24;14(9):1179-1187. doi: 10.1021/acsmedchemlett.3c00142. eCollection 2023 Sep 14. ACS Med Chem Lett. 2023. PMID: 37736184 Free PMC article.
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.
Zak M, Mendonca R, Balazs M, Barrett K, Bergeron P, Blair WS, Chang C, Deshmukh G, Devoss J, Dragovich PS, Eigenbrot C, Ghilardi N, Gibbons P, Gradl S, Hamman C, Hanan EJ, Harstad E, Hewitt PR, Hurley CA, Jin T, Johnson A, Johnson T, Kenny JR, Koehler MF, Bir Kohli P, Kulagowski JJ, Labadie S, Liao J, Liimatta M, Lin Z, Lupardus PJ, Maxey RJ, Murray JM, Pulk R, Rodriguez M, Savage S, Shia S, Steffek M, Ubhayakar S, Ultsch M, van Abbema A, Ward SI, Xiao L, Xiao Y. Zak M, et al. Among authors: murray jm. J Med Chem. 2012 Jul 12;55(13):6176-93. doi: 10.1021/jm300628c. Epub 2012 Jun 28. J Med Chem. 2012. PMID: 22698084
Lead optimization of a 4-aminopyridine benzamide scaffold to identify potent, selective, and orally bioavailable TYK2 inhibitors.
Liang J, van Abbema A, Balazs M, Barrett K, Berezhkovsky L, Blair W, Chang C, Delarosa D, DeVoss J, Driscoll J, Eigenbrot C, Ghilardi N, Gibbons P, Halladay J, Johnson A, Kohli PB, Lai Y, Liu Y, Lyssikatos J, Mantik P, Menghrajani K, Murray J, Peng I, Sambrone A, Shia S, Shin Y, Smith J, Sohn S, Tsui V, Ultsch M, Wu LC, Xiao Y, Yang W, Young J, Zhang B, Zhu BY, Magnuson S. Liang J, et al. Among authors: murray j. J Med Chem. 2013 Jun 13;56(11):4521-36. doi: 10.1021/jm400266t. Epub 2013 May 29. J Med Chem. 2013. PMID: 23668484
GNE-886: A Potent and Selective Inhibitor of the Cat Eye Syndrome Chromosome Region Candidate 2 Bromodomain (CECR2).
Crawford TD, Audia JE, Bellon S, Burdick DJ, Bommi-Reddy A, Côté A, Cummings RT, Duplessis M, Flynn EM, Hewitt M, Huang HR, Jayaram H, Jiang Y, Joshi S, Kiefer JR, Murray J, Nasveschuk CG, Neiss A, Pardo E, Romero FA, Sandy P, Sims RJ 3rd, Tang Y, Taylor AM, Tsui V, Wang J, Wang S, Wang Y, Xu Z, Zawadzke L, Zhu X, Albrecht BK, Magnuson SR, Cochran AG. Crawford TD, et al. Among authors: murray j. ACS Med Chem Lett. 2017 Jun 1;8(7):737-741. doi: 10.1021/acsmedchemlett.7b00132. eCollection 2017 Jul 13. ACS Med Chem Lett. 2017. PMID: 28740608 Free PMC article.
Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance.
Crawford TD, Vartanian S, Côté A, Bellon S, Duplessis M, Flynn EM, Hewitt M, Huang HR, Kiefer JR, Murray J, Nasveschuk CG, Pardo E, Romero FA, Sandy P, Tang Y, Taylor AM, Tsui V, Wang J, Wang S, Zawadzke L, Albrecht BK, Magnuson SR, Cochran AG, Stokoe D. Crawford TD, et al. Among authors: murray j. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3534-3541. doi: 10.1016/j.bmcl.2017.05.063. Epub 2017 Jun 3. Bioorg Med Chem Lett. 2017. PMID: 28606761
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637).
Taylor AM, Côté A, Hewitt MC, Pastor R, Leblanc Y, Nasveschuk CG, Romero FA, Crawford TD, Cantone N, Jayaram H, Setser J, Murray J, Beresini MH, de Leon Boenig G, Chen Z, Conery AR, Cummings RT, Dakin LA, Flynn EM, Huang OW, Kaufman S, Keller PJ, Kiefer JR, Lai T, Li Y, Liao J, Liu W, Lu H, Pardo E, Tsui V, Wang J, Wang Y, Xu Z, Yan F, Yu D, Zawadzke L, Zhu X, Zhu X, Sims RJ 3rd, Cochran AG, Bellon S, Audia JE, Magnuson S, Albrecht BK. Taylor AM, et al. Among authors: murray j. ACS Med Chem Lett. 2016 Mar 15;7(5):531-6. doi: 10.1021/acsmedchemlett.6b00075. eCollection 2016 May 12. ACS Med Chem Lett. 2016. PMID: 27190605 Free PMC article.
GNE-371, a Potent and Selective Chemical Probe for the Second Bromodomains of Human Transcription-Initiation-Factor TFIID Subunit 1 and Transcription-Initiation-Factor TFIID Subunit 1-like.
Wang S, Tsui V, Crawford TD, Audia JE, Burdick DJ, Beresini MH, Côté A, Cummings R, Duplessis M, Flynn EM, Hewitt MC, Huang HR, Jayaram H, Jiang Y, Joshi S, Murray J, Nasveschuk CG, Pardo E, Poy F, Romero FA, Tang Y, Taylor AM, Wang J, Xu Z, Zawadzke LE, Zhu X, Albrecht BK, Magnuson SR, Bellon S, Cochran AG. Wang S, et al. Among authors: murray j. J Med Chem. 2018 Oct 25;61(20):9301-9315. doi: 10.1021/acs.jmedchem.8b01225. Epub 2018 Oct 5. J Med Chem. 2018. PMID: 30289257
7,208 results