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Page 1
Potent and Selective Inhibitors of the Epidermal Growth Factor Receptor to Overcome C797S-Mediated Resistance.
Finlay MRV, Barton P, Bickerton S, Bista M, Colclough N, Cross DAE, Evans L, Floc'h N, Gregson C, Guérot CM, Hargreaves D, Kang X, Lenz EM, Li X, Liu Y, Lorthioir O, Martin MJ, McKerrecher D, McWhirter C, O'Neill D, Orme JP, Mosallanejad A, Rahi A, Smith PD, Talbot V, Ward RA, Wrigley G, Wylot M, Xue L, Yao T, Ye Y, Zhao X. Finlay MRV, et al. Among authors: barton p. J Med Chem. 2021 Sep 23;64(18):13704-13718. doi: 10.1021/acs.jmedchem.1c01055. Epub 2021 Sep 7. J Med Chem. 2021. PMID: 34491761
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: barton p. 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
Preclinical Comparison of the Blood-brain barrier Permeability of Osimertinib with Other EGFR TKIs.
Colclough N, Chen K, Johnström P, Strittmatter N, Yan Y, Wrigley GL, Schou M, Goodwin R, Varnäs K, Adua SJ, Zhao M, Nguyen DX, Maglennon G, Barton P, Atkinson J, Zhang L, Janefeldt A, Wilson J, Smith A, Takano A, Arakawa R, Kondrashov M, Malmquist J, Revunov E, Vazquez-Romero A, Moein MM, Windhorst AD, Karp NA, Finlay MRV, Ward RA, Yates JWT, Smith PD, Farde L, Cheng Z, Cross DAE. Colclough N, et al. Among authors: barton p. Clin Cancer Res. 2021 Jan 1;27(1):189-201. doi: 10.1158/1078-0432.CCR-19-1871. Epub 2020 Oct 7. Clin Cancer Res. 2021. PMID: 33028591
Diverse, Potent, and Efficacious Inhibitors That Target the EED Subunit of the Polycomb Repressive Complex 2 Methyltransferase.
Bagal SK, Gregson C, O' Donovan DH, Pike KG, Bloecher A, Barton P, Borodovsky A, Code E, Fillery SM, Hsu JH, Kawatkar SP, Li C, Longmire D, Nai Y, Nash SC, Pike A, Robinson J, Read JA, Rawlins PB, Shen M, Tang J, Wang P, Woods H, Williamson B. Bagal SK, et al. Among authors: barton p. J Med Chem. 2021 Dec 9;64(23):17146-17183. doi: 10.1021/acs.jmedchem.1c01161. Epub 2021 Nov 22. J Med Chem. 2021. PMID: 34807608
Free energy perturbation in the design of EED ligands as inhibitors of polycomb repressive complex 2 (PRC2) methyltransferase.
O' Donovan DH, Gregson C, Packer MJ, Greenwood R, Pike KG, Kawatkar S, Bloecher A, Robinson J, Read J, Code E, Hsu JH, Shen M, Woods H, Barton P, Fillery S, Williamson B, Rawlins PB, Bagal SK. O' Donovan DH, et al. Among authors: barton p. Bioorg Med Chem Lett. 2021 May 1;39:127904. doi: 10.1016/j.bmcl.2021.127904. Epub 2021 Mar 6. Bioorg Med Chem Lett. 2021. PMID: 33684441
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: barton p. 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.
Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy.
McCoull W, Bailey A, Barton P, Birch AM, Brown AJ, Butler HS, Boyd S, Butlin RJ, Chappell B, Clarkson P, Collins S, Davies RM, Ertan A, Hammond CD, Holmes JL, Lenaghan C, Midha A, Morentin-Gutierrez P, Moore JE, Raubo P, Robb G. McCoull W, et al. Among authors: barton p. J Med Chem. 2017 Apr 13;60(7):3187-3197. doi: 10.1021/acs.jmedchem.7b00210. Epub 2017 Apr 4. J Med Chem. 2017. PMID: 28374589
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: barton p. 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
Pharmacological inhibition of MERTK induces in vivo retinal degeneration: a multimodal imaging ocular safety assessment.
Hamm G, Maglennon G, Williamson B, Macdonald R, Doherty A, Jones S, Harris J, Blades J, Harmer AR, Barton P, Rawlins PB, Smith P, Winter-Holt J, McMurray L, Johansson J, Fitzpatrick P, McCoull W, Coen M. Hamm G, et al. Among authors: barton p. Arch Toxicol. 2022 Feb;96(2):613-624. doi: 10.1007/s00204-021-03197-8. Epub 2022 Jan 1. Arch Toxicol. 2022. PMID: 34973110 Free PMC article.
Identification, optimization, and pharmacology of acylurea GHS-R1a inverse agonists.
McCoull W, Barton P, Brown AJ, Bowker SS, Cameron J, Clarke DS, Davies RD, Dossetter AG, Ertan A, Fenwick M, Green C, Holmes JL, Martin N, Masters D, Moore JE, Newcombe NJ, Newton C, Pointon H, Robb GR, Sheldon C, Stokes S, Morgan D. McCoull W, et al. Among authors: barton p. J Med Chem. 2014 Jul 24;57(14):6128-40. doi: 10.1021/jm500610n. Epub 2014 Jul 8. J Med Chem. 2014. PMID: 24967667
642 results