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Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.
Vasbinder MM, Aquila B, Augustin M, Chen H, Cheung T, Cook D, Drew L, Fauber BP, Glossop S, Grondine M, Hennessy E, Johannes J, Lee S, Lyne P, Mörtl M, Omer C, Palakurthi S, Pontz T, Read J, Sha L, Shen M, Steinbacher S, Wang H, Wu A, Ye M. Vasbinder MM, et al. Among authors: sha l. J Med Chem. 2013 Mar 14;56(5):1996-2015. doi: 10.1021/jm301658d. Epub 2013 Feb 27. J Med Chem. 2013. PMID: 23398453
Discovery of aminopiperidine-based Smac mimetics as IAP antagonists.
Hennessy EJ, Saeh JC, Sha L, MacIntyre T, Wang H, Larsen NA, Aquila BM, Ferguson AD, Laing NM, Omer CA. Hennessy EJ, et al. Among authors: sha l. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1690-4. doi: 10.1016/j.bmcl.2011.12.109. Epub 2011 Dec 31. Bioorg Med Chem Lett. 2012. PMID: 22264476
Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582).
Hennessy EJ, Adam A, Aquila BM, Castriotta LM, Cook D, Hattersley M, Hird AW, Huntington C, Kamhi VM, Laing NM, Li D, MacIntyre T, Omer CA, Oza V, Patterson T, Repik G, Rooney MT, Saeh JC, Sha L, Vasbinder MM, Wang H, Whitston D. Hennessy EJ, et al. Among authors: sha l. J Med Chem. 2013 Dec 27;56(24):9897-919. doi: 10.1021/jm401075x. Epub 2013 Dec 13. J Med Chem. 2013. PMID: 24320998
Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.
Hennessy EJ, Oza V, Adam A, Byth K, Castriotta L, Grewal G, Hamilton GA, Kamhi VM, Lewis P, Li D, Lyne P, Öster L, Rooney MT, Saeh JC, Sha L, Su Q, Wen S, Xue Y, Yang B. Hennessy EJ, et al. Among authors: sha l. J Med Chem. 2015 Sep 10;58(17):7057-75. doi: 10.1021/acs.jmedchem.5b01078. Epub 2015 Aug 26. J Med Chem. 2015. PMID: 26291341
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
Grimster NP, Gingipalli L, Barlaam B, Su Q, Zheng X, Watson D, Wang H, Simpson I, Pike A, Balazs A, Boiko S, Ikeda TP, Impastato AC, Jones NH, Kawatkar S, Kemmitt P, Lamont S, Patel J, Read J, Sarkar U, Sha L, Tomlinson RC, Wang H, Wilson DM, Zehnder TE, Wang L, Wang P, Goldberg FW, Shao W, Fawell S, Dry H, Dowling JE, Edmondson SD. Grimster NP, et al. Among authors: sha l. Bioorg Med Chem Lett. 2020 Oct 1;30(19):127433. doi: 10.1016/j.bmcl.2020.127433. Epub 2020 Jul 24. Bioorg Med Chem Lett. 2020. PMID: 32717371
Utilization of Structure-Based Design to Identify Novel, Irreversible Inhibitors of EGFR Harboring the T790M Mutation.
Hennessy EJ, Chuaqui C, Ashton S, Colclough N, Cross DA, Debreczeni JÉ, Eberlein C, Gingipalli L, Klinowska TC, Orme JP, Sha L, Wu X. Hennessy EJ, et al. Among authors: sha l. ACS Med Chem Lett. 2016 Mar 21;7(5):514-9. doi: 10.1021/acsmedchemlett.6b00058. eCollection 2016 May 12. ACS Med Chem Lett. 2016. PMID: 27190603 Free PMC article.
Discovery of efficacious Pseudomonas aeruginosa-targeted siderophore-conjugated monocarbams by application of a semi-mechanistic pharmacokinetic/pharmacodynamic model.
Murphy-Benenato KE, Bhagunde PR, Chen A, Davis HE, Durand-Réville TF, Ehmann DE, Galullo V, Harris JJ, Hatoum-Mokdad H, Jahić H, Kim A, Manjunatha MR, Manyak EL, Mueller J, Patey S, Quiroga O, Rooney M, Sha L, Shapiro AB, Sylvester M, Tan B, Tsai AS, Uria-Nickelsen M, Wu Y, Zambrowski M, Zhao SX. Murphy-Benenato KE, et al. Among authors: sha l. J Med Chem. 2015 Mar 12;58(5):2195-205. doi: 10.1021/jm501506f. Epub 2015 Mar 3. J Med Chem. 2015. PMID: 25658376
594 results