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846 results

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Page 1
Discovery of GSK251: A Highly Potent, Highly Selective, Orally Bioavailable Inhibitor of PI3Kδ with a Novel Binding Mode.
Down K, Amour A, Anderson NA, Barton N, Campos S, Cannons EP, Clissold C, Convery MA, Coward JJ, Doyle K, Duempelfeld B, Edwards CD, Goldsmith MD, Krause J, Mallett DN, McGonagle GA, Patel VK, Rowedder J, Rowland P, Sharpe A, Sriskantharajah S, Thomas DA, Thomson DW, Uddin S, Hamblin JN, Hessel EM. Down K, et al. Among authors: sharpe a. J Med Chem. 2021 Sep 23;64(18):13780-13792. doi: 10.1021/acs.jmedchem.1c01102. Epub 2021 Sep 11. J Med Chem. 2021. PMID: 34510892
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma.
Wang X, Blackaby W, Allen V, Chan GKY, Chang JH, Chiang PC, Diène C, Drummond J, Do S, Fan E, Harstad EB, Hodges A, Hu H, Jia W, Kofie W, Kolesnikov A, Lyssikatos JP, Ly J, Matteucci M, Moffat JG, Munugalavadla V, Murray J, Nash D, Noland CL, Del Rosario G, Ross L, Rouse C, Sharpe A, Slaga D, Sun M, Tsui V, Wallweber H, Yu SF, Ebens AJ. Wang X, et al. Among authors: sharpe a. J Med Chem. 2019 Feb 28;62(4):2140-2153. doi: 10.1021/acs.jmedchem.8b01857. Epub 2019 Feb 20. J Med Chem. 2019. PMID: 30715878
Discovery of a Novel Class of d-Amino Acid Oxidase Inhibitors Using the Schrödinger Computational Platform.
Tang H, Jensen K, Houang E, McRobb FM, Bhat S, Svensson M, Bochevarov A, Day T, Dahlgren MK, Bell JA, Frye L, Skene RJ, Lewis JH, Osborne JD, Tierney JP, Gordon JA, Palomero MA, Gallati C, Chapman RSL, Jones DR, Hirst KL, Sephton M, Chauhan A, Sharpe A, Tardia P, Dechaux EA, Taylor A, Waddell RD, Valentine A, Janssens HB, Aziz O, Bloomfield DE, Ladha S, Fraser IJ, Ellard JM. Tang H, et al. Among authors: sharpe a. J Med Chem. 2022 May 12;65(9):6775-6802. doi: 10.1021/acs.jmedchem.2c00118. Epub 2022 Apr 28. J Med Chem. 2022. PMID: 35482677
Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
Alam M, Beevers RE, Ceska T, Davenport RJ, Dickson KM, Fortunato M, Gowers L, Haughan AF, James LA, Jones MW, Kinsella N, Lowe C, Meissner JW, Nicolas AL, Perry BG, Phillips DJ, Pitt WR, Platt A, Ratcliffe AJ, Sharpe A, Tait LJ. Alam M, et al. Among authors: sharpe a. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3463-7. doi: 10.1016/j.bmcl.2007.03.078. Epub 2007 Mar 30. Bioorg Med Chem Lett. 2007. PMID: 17459703
7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
Buckley GM, Cooper N, Davenport RJ, Dyke HJ, Galleway FP, Gowers L, Haughan AF, Kendall HJ, Lowe C, Montana JG, Oxford J, Peake JC, Picken CL, Richard MD, Sabin V, Sharpe A, Warneck JB. Buckley GM, et al. Among authors: sharpe a. Bioorg Med Chem Lett. 2002 Feb 11;12(3):509-12. doi: 10.1016/s0960-894x(01)00786-7. Bioorg Med Chem Lett. 2002. PMID: 11814830
Novel 7-methoxy-6-oxazol-5-yl-2,3-dihydro-1H-quinazolin-4-ones as IMPDH inhibitors.
Birch HL, Buckley GM, Davies N, Dyke HJ, Frost EJ, Gilbert PJ, Hannah DR, Haughan AF, Madigan MJ, Morgan T, Pitt WR, Ratcliffe AJ, Ray NC, Richard MD, Sharpe A, Taylor AJ, Whitworth JM, Williams SC. Birch HL, et al. Among authors: sharpe a. Bioorg Med Chem Lett. 2005 Dec 1;15(23):5335-9. doi: 10.1016/j.bmcl.2005.06.108. Epub 2005 Oct 3. Bioorg Med Chem Lett. 2005. PMID: 16202581
Quinazolinethiones and quinazolinediones, novel inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.
Buckley GM, Davies N, Dyke HJ, Gilbert PJ, Hannah DR, Haughan AF, Hunt CA, Pitt WR, Profit RH, Ray NC, Richard MD, Sharpe A, Taylor AJ, Whitworth JM, Williams SC. Buckley GM, et al. Among authors: sharpe a. Bioorg Med Chem Lett. 2005 Feb 1;15(3):751-4. doi: 10.1016/j.bmcl.2004.11.015. Bioorg Med Chem Lett. 2005. PMID: 15664851
Low molecular weight indole fragments as IMPDH inhibitors.
Beevers RE, Buckley GM, Davies N, Fraser JL, Galvin FC, Hannah DR, Haughan AF, Jenkins K, Mack SR, Pitt WR, Ratcliffe AJ, Richard MD, Sabin V, Sharpe A, Williams SC. Beevers RE, et al. Among authors: sharpe a. Bioorg Med Chem Lett. 2006 May 1;16(9):2535-8. doi: 10.1016/j.bmcl.2006.01.089. Epub 2006 Feb 17. Bioorg Med Chem Lett. 2006. PMID: 16483769
Synthesis and profile of SCH351591, a novel PDE4 inhibitor.
Billah M, Cooper N, Cuss F, Davenport RJ, Dyke HJ, Egan R, Ganguly A, Gowers L, Hannah DR, Haughan AF, Kendall HJ, Lowe C, Minnicozzi M, Montana JG, Naylor R, Oxford J, Peake JC, Piwinski JJ, Runcie KA, Sabin V, Sharpe A, Shih NY, Warneck JB. Billah M, et al. Among authors: sharpe a. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1621-3. doi: 10.1016/s0960-894x(02)00225-1. Bioorg Med Chem Lett. 2002. PMID: 12039576
846 results