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Page 1
The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor.
Duffy JP, Harrington EM, Salituro FG, Cochran JE, Green J, Gao H, Bemis GW, Evindar G, Galullo VP, Ford PJ, Germann UA, Wilson KP, Bellon SF, Chen G, Taslimi P, Jones P, Huang C, Pazhanisamy S, Wang YM, Murcko MA, Su MS. Duffy JP, et al. Among authors: bellon sf. ACS Med Chem Lett. 2011 Jul 28;2(10):758-63. doi: 10.1021/ml2001455. eCollection 2011 Oct 13. ACS Med Chem Lett. 2011. PMID: 24900264 Free PMC article.
Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.
Gehling VS, Hewitt MC, Vaswani RG, Leblanc Y, Côté A, Nasveschuk CG, Taylor AM, Harmange JC, Audia JE, Pardo E, Joshi S, Sandy P, Mertz JA, Sims RJ 3rd, Bergeron L, Bryant BM, Bellon S, Poy F, Jayaram H, Sankaranarayanan R, Yellapantula S, Bangalore Srinivasamurthy N, Birudukota S, Albrecht BK. Gehling VS, et al. ACS Med Chem Lett. 2013 Jul 16;4(9):835-40. doi: 10.1021/ml4001485. eCollection 2013 Sep 12. ACS Med Chem Lett. 2013. PMID: 24900758 Free PMC article.
Discovery of potent and selective 8-fluorotriazolopyridine c-Met inhibitors.
Peterson EA, Teffera Y, Albrecht BK, Bauer D, Bellon SF, Boezio A, Boezio C, Broome MA, Choquette D, Copeland KW, Dussault I, Lewis R, Lin MH, Lohman J, Liu J, Potashman M, Rex K, Shimanovich R, Whittington DA, Vaida KR, Harmange JC. Peterson EA, et al. Among authors: bellon sf. J Med Chem. 2015 Mar 12;58(5):2417-30. doi: 10.1021/jm501913a. Epub 2015 Mar 3. J Med Chem. 2015. PMID: 25699405
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. 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.
Discovery of a potent, selective, and orally bioavailable pyridinyl-pyrimidine phthalazine aurora kinase inhibitor.
Cee VJ, Schenkel LB, Hodous BL, Deak HL, Nguyen HN, Olivieri PR, Romero K, Bak A, Be X, Bellon S, Bush TL, Cheng AC, Chung G, Coats S, Eden PM, Hanestad K, Gallant PL, Gu Y, Huang X, Kendall RL, Lin MH, Morrison MJ, Patel VF, Radinsky R, Rose PE, Ross S, Sun JR, Tang J, Zhao H, Payton M, Geuns-Meyer SD. Cee VJ, et al. J Med Chem. 2010 Sep 9;53(17):6368-77. doi: 10.1021/jm100394y. J Med Chem. 2010. PMID: 20684549
Discovery of Benzotriazolo[4,3-d][1,4]diazepines as Orally Active Inhibitors of BET Bromodomains.
Taylor AM, Vaswani RG, Gehling VS, Hewitt MC, Leblanc Y, Audia JE, Bellon S, Cummings RT, Côté A, Harmange JC, Jayaram H, Joshi S, Lora JM, Mertz JA, Neiss A, Pardo E, Nasveschuk CG, Poy F, Sandy P, Setser JW, Sims RJ 3rd, Tang Y, Albrecht BK. Taylor AM, et al. ACS Med Chem Lett. 2015 Mar 25;7(2):145-50. doi: 10.1021/ml500411h. eCollection 2016 Feb 11. ACS Med Chem Lett. 2015. PMID: 26985289 Free PMC article.
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. 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.
49 results