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Page 1
Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927.
Labadie SS, Li J, Blake RA, Chang JH, Goodacre S, Hartman SJ, Liang W, Kiefer JR, Kleinheinz T, Lai T, Liao J, Ortwine DF, Mody V, Ray NC, Roussel F, Vinogradova M, Yeap SK, Zhang B, Zheng X, Zbieg JR, Liang J, Wang X. Labadie SS, et al. Among authors: liang w, liang j. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2090-2093. doi: 10.1016/j.bmcl.2019.07.013. Epub 2019 Jul 6. Bioorg Med Chem Lett. 2019. PMID: 31311734
A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability.
Rawson TE, Rüth M, Blackwood E, Burdick D, Corson L, Dotson J, Drummond J, Fields C, Georges GJ, Goller B, Halladay J, Hunsaker T, Kleinheinz T, Krell HW, Li J, Liang J, Limberg A, McNutt A, Moffat J, Phillips G, Ran Y, Safina B, Ultsch M, Walker L, Wiesmann C, Zhang B, Zhou A, Zhu BY, Rüger P, Cochran AG. Rawson TE, et al. Among authors: liang j. J Med Chem. 2008 Aug 14;51(15):4465-75. doi: 10.1021/jm800052b. Epub 2008 Jul 17. J Med Chem. 2008. PMID: 18630890
A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B.
Aliagas-Martin I, Burdick D, Corson L, Dotson J, Drummond J, Fields C, Huang OW, Hunsaker T, Kleinheinz T, Krueger E, Liang J, Moffat J, Phillips G, Pulk R, Rawson TE, Ultsch M, Walker L, Wiesmann C, Zhang B, Zhu BY, Cochran AG. Aliagas-Martin I, et al. Among authors: liang j. J Med Chem. 2009 May 28;52(10):3300-7. doi: 10.1021/jm9000314. J Med Chem. 2009. PMID: 19402633
Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.
Blake JF, Xu R, Bencsik JR, Xiao D, Kallan NC, Schlachter S, Mitchell IS, Spencer KL, Banka AL, Wallace EM, Gloor SL, Martinson M, Woessner RD, Vigers GP, Brandhuber BJ, Liang J, Safina BS, Li J, Zhang B, Chabot C, Do S, Lee L, Oeh J, Sampath D, Lee BB, Lin K, Liederer BM, Skelton NJ. Blake JF, et al. Among authors: liang j. J Med Chem. 2012 Sep 27;55(18):8110-27. doi: 10.1021/jm301024w. Epub 2012 Sep 18. J Med Chem. 2012. PMID: 22934575
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. J Med Chem. 2013 Jun 13;56(11):4521-36. doi: 10.1021/jm400266t. Epub 2013 May 29. J Med Chem. 2013. PMID: 23668484
Lead identification of novel and selective TYK2 inhibitors.
Liang J, Tsui V, Van Abbema A, Bao L, Barrett K, Beresini M, Berezhkovskiy L, Blair WS, Chang C, Driscoll J, Eigenbrot C, Ghilardi N, Gibbons P, Halladay J, Johnson A, Kohli PB, Lai Y, Liimatta M, Mantik P, Menghrajani K, Murray J, Sambrone A, Xiao Y, Shia S, Shin Y, Smith J, Sohn S, Stanley M, Ultsch M, Zhang B, Wu LC, Magnuson S. Liang J, et al. Eur J Med Chem. 2013 Sep;67:175-87. doi: 10.1016/j.ejmech.2013.03.070. Epub 2013 May 14. Eur J Med Chem. 2013. PMID: 23867602
Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies.
Liang J, Zhang B, Labadie S, Ortwine DF, Vinogradova M, Kiefer JR, Gehling VS, Harmange JC, Cummings R, Lai T, Liao J, Zheng X, Liu Y, Gustafson A, Van der Porten E, Mao W, Liederer BM, Deshmukh G, Classon M, Trojer P, Dragovich PS, Murray L. Liang J, et al. Bioorg Med Chem Lett. 2016 Aug 15;26(16):4036-41. doi: 10.1016/j.bmcl.2016.06.078. Epub 2016 Jun 29. Bioorg Med Chem Lett. 2016. PMID: 27406798
Design and evaluation of 1,7-naphthyridones as novel KDM5 inhibitors.
Labadie SS, Dragovich PS, Cummings RT, Deshmukh G, Gustafson A, Han N, Harmange JC, Kiefer JR, Li Y, Liang J, Liederer BM, Liu Y, Manieri W, Mao W, Murray L, Ortwine DF, Trojer P, VanderPorten E, Vinogradova M, Wen L. Labadie SS, et al. Among authors: liang j. Bioorg Med Chem Lett. 2016 Sep 15;26(18):4492-4496. doi: 10.1016/j.bmcl.2016.07.070. Epub 2016 Jul 29. Bioorg Med Chem Lett. 2016. PMID: 27499454
From a novel HTS hit to potent, selective, and orally bioavailable KDM5 inhibitors.
Liang J, Labadie S, Zhang B, Ortwine DF, Patel S, Vinogradova M, Kiefer JR, Mauer T, Gehling VS, Harmange JC, Cummings R, Lai T, Liao J, Zheng X, Liu Y, Gustafson A, Van der Porten E, Mao W, Liederer BM, Deshmukh G, An L, Ran Y, Classon M, Trojer P, Dragovich PS, Murray L. Liang J, et al. Bioorg Med Chem Lett. 2017 Jul 1;27(13):2974-2981. doi: 10.1016/j.bmcl.2017.05.016. Epub 2017 May 5. Bioorg Med Chem Lett. 2017. PMID: 28512031
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