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Page 1
Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors.
Grimster NP, Gingipalli L, Balazs A, Barlaam B, Boiko S, Boyd S, Dry H, Goldberg FW, Ikeda T, Johnson T, Kawatkar S, Kemmitt P, Lamont S, Lorthioir O, Mfuh A, Patel J, Pike A, Read J, Romero R, Sarkar U, Sha L, Simpson I, Song K, Su Q, Wang H, Watson D, Wu A, Zehnder TE, Zheng X, Li S, Dong Z, Yang D, Song Y, Wang P, Liu X, Dowling JE, Edmondson SD. Grimster NP, et al. Bioorg Med Chem Lett. 2023 Jul 15;91:129352. doi: 10.1016/j.bmcl.2023.129352. Epub 2023 Jun 2. Bioorg Med Chem Lett. 2023. PMID: 37270074
Identification, optimisation and in vivo evaluation of oxadiazole DGAT-1 inhibitors for the treatment of obesity and diabetes.
McCoull W, Addie MS, Birch AM, Birtles S, Buckett LK, Butlin RJ, Bowker SS, Boyd S, Chapman S, Davies RD, Donald CS, Green CP, Jenner C, Kemmitt PD, Leach AG, Moody GC, Gutierrez PM, Newcombe NJ, Nowak T, Packer MJ, Plowright AT, Revill J, Schofield P, Sheldon C, Stokes S, Turnbull AV, Wang SJ, Whalley DP, Wood JM. McCoull W, et al. Among authors: kemmitt pd. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3873-8. doi: 10.1016/j.bmcl.2012.04.117. Epub 2012 May 2. Bioorg Med Chem Lett. 2012. PMID: 22608962
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.
Finlay MR, Anderton M, Ashton S, Ballard P, Bethel PA, Box MR, Bradbury RH, Brown SJ, Butterworth S, Campbell A, Chorley C, Colclough N, Cross DA, Currie GS, Grist M, Hassall L, Hill GB, James D, James M, Kemmitt P, Klinowska T, Lamont G, Lamont SG, Martin N, McFarland HL, Mellor MJ, Orme JP, Perkins D, Perkins P, Richmond G, Smith P, Ward RA, Waring MJ, Whittaker D, Wells S, Wrigley GL. Finlay MR, et al. J Med Chem. 2014 Oct 23;57(20):8249-67. doi: 10.1021/jm500973a. Epub 2014 Oct 1. J Med Chem. 2014. PMID: 25271963
Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.
McCoull W, Hennessy EJ, Blades K, Chuaqui C, Dowling JE, Ferguson AD, Goldberg FW, Howe N, Jones CR, Kemmitt PD, Lamont G, Varnes JG, Ward RA, Yang B. McCoull W, et al. Among authors: kemmitt pd. ACS Med Chem Lett. 2016 Sep 14;7(12):1118-1123. doi: 10.1021/acsmedchemlett.6b00322. eCollection 2016 Dec 8. ACS Med Chem Lett. 2016. PMID: 27994749 Free PMC article.
Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, Fuller NO, Gangl E, Gao N, Grist M, Hargreaves D, Howard MR, Hu J, Kemmitt PD, Nelson JE, O'Connell N, Prince DB, Raubo P, Rawlins PB, Robb GR, Shi J, Waring MJ, Whittaker D, Wylot M, Zhu X. McCoull W, et al. Among authors: kemmitt pd. J Med Chem. 2017 May 25;60(10):4386-4402. doi: 10.1021/acs.jmedchem.7b00359. Epub 2017 May 9. J Med Chem. 2017. PMID: 28485934
Correction to Discovery of Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, Fuller NO, Gangl E, Gao N, Grist M, Hargreaves D, Howard MR, Hu J, Kemmitt PD, Nelson JE, O'Connell N, Prince DB, Raubo P, Rawlins PB, Robb GR, Shi J, Waring MJ, Whittaker D, Wylot M, Zhu X. McCoull W, et al. Among authors: kemmitt pd. J Med Chem. 2017 Jul 27;60(14):6459. doi: 10.1021/acs.jmedchem.7b00962. Epub 2017 Jul 17. J Med Chem. 2017. PMID: 28714680 No abstract available.
Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6.
McCoull W, Cheung T, Anderson E, Barton P, Burgess J, Byth K, Cao Q, Castaldi MP, Chen H, Chiarparin E, Carbajo RJ, Code E, Cowan S, Davey PR, Ferguson AD, Fillery S, Fuller NO, Gao N, Hargreaves D, Howard MR, Hu J, Kawatkar A, Kemmitt PD, Leo E, Molina DM, O'Connell N, Petteruti P, Rasmusson T, Raubo P, Rawlins PB, Ricchiuto P, Robb GR, Schenone M, Waring MJ, Zinda M, Fawell S, Wilson DM. McCoull W, et al. Among authors: kemmitt pd. ACS Chem Biol. 2018 Nov 16;13(11):3131-3141. doi: 10.1021/acschembio.8b00698. Epub 2018 Oct 17. ACS Chem Biol. 2018. PMID: 30335946
Design and optimisation of dendrimer-conjugated Bcl-2/xL inhibitor, AZD0466, with improved therapeutic index for cancer therapy.
Patterson CM, Balachander SB, Grant I, Pop-Damkov P, Kelly B, McCoull W, Parker J, Giannis M, Hill KJ, Gibbons FD, Hennessy EJ, Kemmitt P, Harmer AR, Gales S, Purbrick S, Redmond S, Skinner M, Graham L, Secrist JP, Schuller AG, Wen S, Adam A, Reimer C, Cidado J, Wild M, Gangl E, Fawell SE, Saeh J, Davies BR, Owen DJ, Ashford MB. Patterson CM, et al. Commun Biol. 2021 Jan 25;4(1):112. doi: 10.1038/s42003-020-01631-8. Commun Biol. 2021. PMID: 33495510 Free PMC article.
30 results