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Page 1
Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma.
Scott JS, Degorce SL, Anjum R, Culshaw J, Davies RDM, Davies NL, Dillman KS, Dowling JE, Drew L, Ferguson AD, Groombridge SD, Halsall CT, Hudson JA, Lamont S, Lindsay NA, Marden SK, Mayo MF, Pease JE, Perkins DR, Pink JH, Robb GR, Rosen A, Shen M, McWhirter C, Wu D. Scott JS, et al. Among authors: davies rdm, davies nl. J Med Chem. 2017 Dec 28;60(24):10071-10091. doi: 10.1021/acs.jmedchem.7b01290. Epub 2017 Dec 11. J Med Chem. 2017. PMID: 29172502
Potent and Selective Inhibitors of MTH1 Probe Its Role in Cancer Cell Survival.
Kettle JG, Alwan H, Bista M, Breed J, Davies NL, Eckersley K, Fillery S, Foote KM, Goodwin L, Jones DR, Käck H, Lau A, Nissink JW, Read J, Scott JS, Taylor B, Walker G, Wissler L, Wylot M. Kettle JG, et al. Among authors: davies nl. J Med Chem. 2016 Mar 24;59(6):2346-61. doi: 10.1021/acs.jmedchem.5b01760. Epub 2016 Feb 16. J Med Chem. 2016. PMID: 26878898
The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2 H-pyran-4-yl)-1,3-dihydro-2 H-imidazo[4,5- c]quinolin-2-one).
Pike KG, Barlaam B, Cadogan E, Campbell A, Chen Y, Colclough N, Davies NL, de-Almeida C, Degorce SL, Didelot M, Dishington A, Ducray R, Durant ST, Hassall LA, Holmes J, Hughes GD, MacFaul PA, Mulholland KR, McGuire TM, Ouvry G, Pass M, Robb G, Stratton N, Wang Z, Wilson J, Zhai B, Zhao K, Al-Huniti N. Pike KG, et al. Among authors: davies nl. J Med Chem. 2018 May 10;61(9):3823-3841. doi: 10.1021/acs.jmedchem.7b01896. Epub 2018 May 2. J Med Chem. 2018. PMID: 29683659
Correction to "Free Ligand 1D NMR Conformational Signatures To Enhance Structure Based Drug Design of a Mcl-1 Inhibitor (AZD5991) and Other Synthetic Macrocycles".
Balazs AYS, Carbajo RJ, Davies NL, Dong Y, Hird AW, Johannes JW, Lamb ML, McCoull W, Raubo P, Robb GR, Packer MJ, Chiarparin E. Balazs AYS, et al. Among authors: davies nl. J Med Chem. 2021 Mar 11;64(5):2849. doi: 10.1021/acs.jmedchem.1c00273. Epub 2021 Mar 1. J Med Chem. 2021. PMID: 33646774 Free article. No abstract available.
Optimization of an Imidazo[1,2-a]pyridine Series to Afford Highly Selective Type I1/2 Dual Mer/Axl Kinase Inhibitors with In Vivo Efficacy.
McCoull W, Boyd S, Brown MR, Coen M, Collingwood O, Davies NL, Doherty A, Fairley G, Goldberg K, Hardaker E, He G, Hennessy EJ, Hopcroft P, Hodgson G, Jackson A, Jiang X, Karmokar A, Lainé AL, Lindsay N, Mao Y, Markandu R, McMurray L, McLean N, Mooney L, Musgrove H, Nissink JWM, Pflug A, Reddy VP, Rawlins PB, Rivers E, Schimpl M, Smith GF, Tentarelli S, Travers J, Troup RI, Walton J, Wang C, Wilkinson S, Williamson B, Winter-Holt J, Yang D, Zheng Y, Zhu Q, Smith PD. McCoull W, et al. Among authors: davies nl. J Med Chem. 2021 Sep 23;64(18):13524-13539. doi: 10.1021/acs.jmedchem.1c00920. Epub 2021 Sep 3. J Med Chem. 2021. PMID: 34478292
Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.
Winter-Holt JJ, Bardelle C, Chiarparin E, Dale IL, Davey PRJ, Davies NL, Denz C, Fillery SM, Guérot CM, Han F, Hughes SJ, Kulkarni M, Liu Z, Milbradt A, Moss TA, Niu H, Patel J, Rabow AA, Schimpl M, Shi J, Sun D, Yang D, Guichard S. Winter-Holt JJ, et al. Among authors: davies nl. J Med Chem. 2022 Feb 24;65(4):3306-3331. doi: 10.1021/acs.jmedchem.1c01871. Epub 2022 Feb 8. J Med Chem. 2022. PMID: 35133824
Identification and optimisation of a pyrimidopyridone series of IRAK4 inhibitors.
Cumming IA, Degorce SL, Aagaard A, Braybrooke EL, Davies NL, Diène CR, Eatherton AJ, Felstead HR, Groombridge SD, Lenz EM, Li Y, Nai Y, Pearson S, Robb GR, Scott JS, Steward OR, Wu C, Xue Y, Zhang L, Zhang Y. Cumming IA, et al. Among authors: davies nl. Bioorg Med Chem. 2022 Jun 1;63:116729. doi: 10.1016/j.bmc.2022.116729. Epub 2022 Apr 2. Bioorg Med Chem. 2022. PMID: 35439688
Discovery of AZD4625, a Covalent Allosteric Inhibitor of the Mutant GTPase KRASG12C.
Kettle JG, Bagal SK, Bickerton S, Bodnarchuk MS, Boyd S, Breed J, Carbajo RJ, Cassar DJ, Chakraborty A, Cosulich S, Cumming I, Davies M, Davies NL, Eatherton A, Evans L, Feron L, Fillery S, Gleave ES, Goldberg FW, Hanson L, Harlfinger S, Howard M, Howells R, Jackson A, Kemmitt P, Lamont G, Lamont S, Lewis HJ, Liu L, Niedbala MJ, Phillips C, Polanski R, Raubo P, Robb G, Robinson DM, Ross S, Sanders MG, Tonge M, Whiteley R, Wilkinson S, Yang J, Zhang W. Kettle JG, et al. Among authors: davies nl. J Med Chem. 2022 May 12;65(9):6940-6952. doi: 10.1021/acs.jmedchem.2c00369. Epub 2022 Apr 26. J Med Chem. 2022. PMID: 35471939
Discovery of AZD4747, a Potent and Selective Inhibitor of Mutant GTPase KRASG12C with Demonstrable CNS Penetration.
Kettle JG, Bagal SK, Barratt D, Bodnarchuk MS, Boyd S, Braybrooke E, Breed J, Cassar DJ, Cosulich S, Davies M, Davies NL, Deng C, Eatherton A, Evans L, Feron LJ, Fillery S, Gleave ES, Goldberg FW, Cortés González MA, Guerot C, Haider A, Harlfinger S, Howells R, Jackson A, Johnström P, Kemmitt PD, Koers A, Kondrashov M, Lamont GM, Lamont S, Lewis HJ, Liu L, Mylrea M, Nash S, Niedbala MJ, Peter A, Phillips C, Pike K, Raubo P, Robb GR, Ross S, Sanders MG, Schou M, Simpson I, Steward O. Kettle JG, et al. Among authors: davies nl. J Med Chem. 2023 Jul 13;66(13):9147-9160. doi: 10.1021/acs.jmedchem.3c00746. Epub 2023 Jul 3. J Med Chem. 2023. PMID: 37395055
31 results