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Page 1
Discovery of the pan-genotypic hepatitis C virus NS3/4A protease inhibitor voxilaprevir (GS-9857): A component of Vosevi®.
Taylor JG, Zipfel S, Ramey K, Vivian R, Schrier A, Karki KK, Katana A, Kato D, Kobayashi T, Martinez R, Sangi M, Siegel D, Tran CV, Yang ZY, Zablocki J, Yang CY, Wang Y, Wang K, Chan K, Barauskas O, Cheng G, Jin D, Schultz BE, Appleby T, Villaseñor AG, Link JO. Taylor JG, et al. Among authors: zablocki j. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2428-2436. doi: 10.1016/j.bmcl.2019.03.037. Epub 2019 Mar 26. Bioorg Med Chem Lett. 2019. PMID: 31133531
Structure-guided discovery of a novel, potent, and orally bioavailable 3,5-dimethylisoxazole aryl-benzimidazole BET bromodomain inhibitor.
Sperandio D, Aktoudianakis V, Babaoglu K, Chen X, Elbel K, Chin G, Corkey B, Du J, Jiang B, Kobayashi T, Mackman R, Martinez R, Yang H, Zablocki J, Kusam S, Jordan K, Webb H, Bates JG, Lad L, Mish M, Niedziela-Majka A, Metobo S, Sapre A, Hung M, Jin D, Fung W, Kan E, Eisenberg G, Larson N, Newby ZER, Lansdon E, Tay C, Neve RM, Shevick SL, Breckenridge DG. Sperandio D, et al. Among authors: zablocki j. Bioorg Med Chem. 2019 Feb 1;27(3):457-469. doi: 10.1016/j.bmc.2018.11.020. Epub 2018 Nov 15. Bioorg Med Chem. 2019. PMID: 30606676
Discovery of GS-9688 (Selgantolimod) as a Potent and Selective Oral Toll-Like Receptor 8 Agonist for the Treatment of Chronic Hepatitis B.
Mackman RL, Mish M, Chin G, Perry JK, Appleby T, Aktoudianakis V, Metobo S, Pyun P, Niu C, Daffis S, Yu H, Zheng J, Villasenor AG, Zablocki J, Chamberlain J, Jin H, Lee G, Suekawa-Pirrone K, Santos R, Delaney WE 4th, Fletcher SP. Mackman RL, et al. Among authors: zablocki j. J Med Chem. 2020 Sep 24;63(18):10188-10203. doi: 10.1021/acs.jmedchem.0c00100. Epub 2020 Jun 3. J Med Chem. 2020. PMID: 32407112
Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Notte GT, Kalla R, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Smith-Maxwell C, Dhalla AK, Rajamani S, Stafford B, Tang J, Mollova N, Belardinelli L, Zablocki JA. Koltun DO, et al. Among authors: zablocki ja. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3202-3206. doi: 10.1016/j.bmcl.2016.03.101. Epub 2016 Mar 30. Bioorg Med Chem Lett. 2016. PMID: 27080178
Discovery of potent and selective inhibitors of calmodulin-dependent kinase II (CaMKII).
Koltun DO, Parkhill EQ, Kalla R, Perry TD, Elzein E, Li X, Simonovich SP, Ziebenhaus C, Hansen TR, Marchand B, Hung WK, Lagpacan L, Hung M, Aoyama RG, Murray BP, Perry JK, Somoza JR, Villaseñor AG, Pagratis N, Zablocki JA. Koltun DO, et al. Among authors: zablocki ja. Bioorg Med Chem Lett. 2018 Feb 1;28(3):541-546. doi: 10.1016/j.bmcl.2017.10.040. Epub 2017 Oct 20. Bioorg Med Chem Lett. 2018. PMID: 29254643
Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine.
Koltun DO, Parkhill EQ, Elzein E, Kobayashi T, Jiang RH, Li X, Perry TD, Avila B, Wang WQ, Hirakawa R, Smith-Maxwell C, Wu L, Dhalla AK, Rajamani S, Mollova N, Stafford B, Tang J, Belardinelli L, Zablocki JA. Koltun DO, et al. Among authors: zablocki ja. Bioorg Med Chem Lett. 2016 Jul 1;26(13):3207-3211. doi: 10.1016/j.bmcl.2016.03.096. Epub 2016 Mar 26. Bioorg Med Chem Lett. 2016. PMID: 27038498
Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties.
Zablocki JA, Elzein E, Li X, Koltun DO, Parkhill EQ, Kobayashi T, Martinez R, Corkey B, Jiang H, Perry T, Kalla R, Notte GT, Saunders O, Graupe M, Lu Y, Venkataramani C, Guerrero J, Perry J, Osier M, Strickley R, Liu G, Wang WQ, Hu L, Li XJ, El-Bizri N, Hirakawa R, Kahlig K, Xie C, Li CH, Dhalla AK, Rajamani S, Mollova N, Soohoo D, Lepist EI, Murray B, Rhodes G, Belardinelli L, Desai MC. Zablocki JA, et al. J Med Chem. 2016 Oct 13;59(19):9005-9017. doi: 10.1021/acs.jmedchem.6b00939. Epub 2016 Oct 3. J Med Chem. 2016. PMID: 27690427
Selectivity switch between FAK and Pyk2: Macrocyclization of FAK inhibitors improves Pyk2 potency.
Farand J, Mai N, Chandrasekhar J, Newby ZE, Van Veldhuizen J, Loyer-Drew J, Venkataramani C, Guerrero J, Kwok A, Li N, Zherebina Y, Wilbert S, Zablocki J, Phillips G, Watkins WJ, Mourey R, Notte GT. Farand J, et al. Among authors: zablocki j. Bioorg Med Chem Lett. 2016 Dec 15;26(24):5926-5930. doi: 10.1016/j.bmcl.2016.10.092. Epub 2016 Nov 2. Bioorg Med Chem Lett. 2016. PMID: 27876318
Potent, orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors.
Koltun DO, Zilbershtein TM, Migulin VA, Vasilevich NI, Parkhill EQ, Glushkov AI, McGregor MJ, Brunn SA, Chu N, Hao J, Mollova N, Leung K, Chisholm JW, Zablocki J. Koltun DO, et al. Among authors: zablocki j. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4070-4. doi: 10.1016/j.bmcl.2009.06.017. Epub 2009 Jun 13. Bioorg Med Chem Lett. 2009. PMID: 19577469
170 results