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Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement.
Barlaam B, De Savi C, Dishington A, Drew L, Ferguson AD, Ferguson D, Gu C, Hande S, Hassall L, Hawkins J, Hird AW, Holmes J, Lamb ML, Lister AS, McGuire TM, Moore JE, O'Connell N, Patel A, Pike KG, Sarkar U, Shao W, Stead D, Varnes JG, Vasbinder MM, Wang L, Wu L, Xue L, Yang B, Yao T. Barlaam B, et al. Among authors: pike kg. J Med Chem. 2021 Oct 28;64(20):15189-15213. doi: 10.1021/acs.jmedchem.1c01249. Epub 2021 Oct 14. J Med Chem. 2021. PMID: 34647738
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
Pyrimidinone nicotinamide mimetics as selective tankyrase and wnt pathway inhibitors suitable for in vivo pharmacology.
Johannes JW, Almeida L, Barlaam B, Boriack-Sjodin PA, Casella R, Croft RA, Dishington AP, Gingipalli L, Gu C, Hawkins JL, Holmes JL, Howard T, Huang J, Ioannidis S, Kazmirski S, Lamb ML, McGuire TM, Moore JE, Ogg D, Patel A, Pike KG, Pontz T, Robb GR, Su N, Wang H, Wu X, Zhang HJ, Zhang Y, Zheng X, Wang T. Johannes JW, et al. Among authors: pike kg. ACS Med Chem Lett. 2015 Jan 13;6(3):254-9. doi: 10.1021/ml5003663. eCollection 2015 Mar 12. ACS Med Chem Lett. 2015. PMID: 25815142 Free PMC article.
Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.
Degorce SL, Barlaam B, Cadogan E, Dishington A, Ducray R, Glossop SC, Hassall LA, Lach F, Lau A, McGuire TM, Nowak T, Ouvry G, Pike KG, Thomason AG. Degorce SL, et al. Among authors: pike kg. J Med Chem. 2016 Jul 14;59(13):6281-92. doi: 10.1021/acs.jmedchem.6b00519. Epub 2016 Jun 16. J Med Chem. 2016. PMID: 27259031
29 results