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Page 1
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: pike kg. 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
Design of a potent, soluble glucokinase activator with excellent in vivo efficacy.
McKerrecher D, Allen JV, Caulkett PW, Donald CS, Fenwick ML, Grange E, Johnson KM, Johnstone C, Jones CD, Pike KG, Rayner JW, Walker RP. McKerrecher D, et al. Among authors: pike kg. Bioorg Med Chem Lett. 2006 May 15;16(10):2705-9. doi: 10.1016/j.bmcl.2006.02.022. Epub 2006 Feb 28. Bioorg Med Chem Lett. 2006. PMID: 16503142
Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR.
Menear KA, Gomez S, Malagu K, Bailey C, Blackburn K, Cockcroft XL, Ewen S, Fundo A, Le Gall A, Hermann G, Sebastian L, Sunose M, Presnot T, Torode E, Hickson I, Martin NM, Smith GC, Pike KG. Menear KA, et al. Among authors: pike kg. Bioorg Med Chem Lett. 2009 Oct 15;19(20):5898-901. doi: 10.1016/j.bmcl.2009.08.069. Epub 2009 Aug 21. Bioorg Med Chem Lett. 2009. PMID: 19733066
The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38α MAP kinase inhibitor for the treatment of inflammatory diseases.
Brown DS, Cumming JG, Bethel P, Finlayson J, Gerhardt S, Nash I, Pauptit RA, Pike KG, Reid A, Snelson W, Swallow S, Thompson C. Brown DS, et al. Among authors: pike kg. Bioorg Med Chem Lett. 2012 Jun 15;22(12):3879-83. doi: 10.1016/j.bmcl.2012.04.116. Epub 2012 May 2. Bioorg Med Chem Lett. 2012. PMID: 22608965
Discovery of AZD3147: a potent, selective dual inhibitor of mTORC1 and mTORC2.
Pike KG, Morris J, Ruston L, Pass SL, Greenwood R, Williams EJ, Demeritt J, Culshaw JD, Gill K, Pass M, Finlay MR, Good CJ, Roberts CA, Currie GS, Blades K, Eden JM, Pearson SE. Pike KG, et al. J Med Chem. 2015 Mar 12;58(5):2326-49. doi: 10.1021/jm501778s. Epub 2015 Feb 18. J Med Chem. 2015. PMID: 25643210
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. 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
Discovery of AZD4573, a Potent and Selective Inhibitor of CDK9 That Enables Short Duration of Target Engagement for the Treatment of Hematological Malignancies.
Barlaam B, Casella R, Cidado J, Cook C, De Savi C, Dishington A, Donald CS, Drew L, Ferguson AD, Ferguson D, Glossop S, Grebe T, Gu C, Hande S, Hawkins J, Hird AW, Holmes J, Horstick J, Jiang Y, Lamb ML, McGuire TM, Moore JE, O'Connell N, Pike A, Pike KG, Proia T, Roberts B, San Martin M, Sarkar U, Shao W, Stead D, Sumner N, Thakur K, Vasbinder MM, Varnes JG, Wang J, Wang L, Wu D, Wu L, Yang B, Yao T. Barlaam B, et al. Among authors: pike kg. J Med Chem. 2020 Dec 24;63(24):15564-15590. doi: 10.1021/acs.jmedchem.0c01754. Epub 2020 Dec 11. J Med Chem. 2020. PMID: 33306391
29 results