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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: patel a. 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
Discovery of a Series of 3-Cinnoline Carboxamides as Orally Bioavailable, Highly Potent, and Selective ATM Inhibitors.
Barlaam B, Cadogan E, Campbell A, Colclough N, Dishington A, Durant S, Goldberg K, Hassall LA, Hughes GD, MacFaul PA, McGuire TM, Pass M, Patel A, Pearson S, Petersen J, Pike KG, Robb G, Stratton N, Xin G, Zhai B. Barlaam B, et al. Among authors: patel a. ACS Med Chem Lett. 2018 Jul 13;9(8):809-814. doi: 10.1021/acsmedchemlett.8b00200. eCollection 2018 Aug 9. ACS Med Chem Lett. 2018. PMID: 30128072 Free PMC article.
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: patel a. 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.
Switching between agonists and antagonists at CRTh2 in a series of highly potent and selective biaryl phenoxyacetic acids.
Luker T, Bonnert R, Schmidt J, Sargent C, Paine SW, Thom S, Pairaudeau G, Patel A, Mohammed R, Akam E, Dougall I, Davis AM, Abbott P, Brough S, Millichip I, McInally T. Luker T, et al. Among authors: patel a. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3616-21. doi: 10.1016/j.bmcl.2011.04.101. Epub 2011 Apr 28. Bioorg Med Chem Lett. 2011. PMID: 21592791
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)-4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153).
Bradbury RH, Callis R, Carr GR, Chen H, Clark E, Feron L, Glossop S, Graham MA, Hattersley M, Jones C, Lamont SG, Ouvry G, Patel A, Patel J, Rabow AA, Roberts CA, Stokes S, Stratton N, Walker GE, Ward L, Whalley D, Whittaker D, Wrigley G, Waring MJ. Bradbury RH, et al. Among authors: patel j, patel a. J Med Chem. 2016 Sep 8;59(17):7801-17. doi: 10.1021/acs.jmedchem.6b00070. Epub 2016 Aug 24. J Med Chem. 2016. PMID: 27528113
Zwitterionic CRTh2 antagonists.
Luker T, Bonnert R, Paine SW, Schmidt J, Sargent C, Cook AR, Cook A, Gardiner P, Hill S, Weyman-Jones C, Patel A, Thom S, Thorne P. Luker T, et al. Among authors: patel a. J Med Chem. 2011 Mar 24;54(6):1779-88. doi: 10.1021/jm1014549. Epub 2011 Feb 28. J Med Chem. 2011. PMID: 21355602
Discovery of potent CRTh2 (DP2) receptor antagonists.
Birkinshaw TN, Teague SJ, Beech C, Bonnert RV, Hill S, Patel A, Reakes S, Sanganee H, Dougall IG, Phillips TT, Salter S, Schmidt J, Arrowsmith EC, Carrillo JJ, Bell FM, Paine SW, Weaver R. Birkinshaw TN, et al. Among authors: patel a. Bioorg Med Chem Lett. 2006 Aug 15;16(16):4287-90. doi: 10.1016/j.bmcl.2006.05.062. Epub 2006 Jun 5. Bioorg Med Chem Lett. 2006. PMID: 16753296
From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis.
Springthorpe B, Bailey A, Barton P, Birkinshaw TN, Bonnert RV, Brown RC, Chapman D, Dixon J, Guile SD, Humphries RG, Hunt SF, Ince F, Ingall AH, Kirk IP, Leeson PD, Leff P, Lewis RJ, Martin BP, McGinnity DF, Mortimore MP, Paine SW, Pairaudeau G, Patel A, Rigby AJ, Riley RJ, Teobald BJ, Tomlinson W, Webborn PJ, Willis PA. Springthorpe B, et al. Among authors: patel a. Bioorg Med Chem Lett. 2007 Nov 1;17(21):6013-8. doi: 10.1016/j.bmcl.2007.07.057. Epub 2007 Aug 19. Bioorg Med Chem Lett. 2007. PMID: 17827008
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