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Page 1
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: read ja. 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
Discovery of a novel class of triazolones as checkpoint kinase inhibitors--hit to lead exploration.
Oza V, Ashwell S, Brassil P, Breed J, Deng C, Ezhuthachan J, Haye H, Horn C, Janetka J, Lyne P, Newcombe N, Otterbien L, Pass M, Read J, Roswell S, Su M, Toader D, Yu D, Yu Y, Valentine A, Webborn P, White A, Zabludoff S, Zheng X. Oza V, et al. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5133-8. doi: 10.1016/j.bmcl.2010.07.015. Epub 2010 Jul 29. Bioorg Med Chem Lett. 2010. PMID: 20673630
Discovery of 5-chloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methyl-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (AZD1480) as a novel inhibitor of the Jak/Stat pathway.
Ioannidis S, Lamb ML, Wang T, Almeida L, Block MH, Davies AM, Peng B, Su M, Zhang HJ, Hoffmann E, Rivard C, Green I, Howard T, Pollard H, Read J, Alimzhanov M, Bebernitz G, Bell K, Ye M, Huszar D, Zinda M. Ioannidis S, et al. J Med Chem. 2011 Jan 13;54(1):262-76. doi: 10.1021/jm1011319. Epub 2010 Dec 7. J Med Chem. 2011. PMID: 21138246
Pyrrolamide DNA gyrase inhibitors: optimization of antibacterial activity and efficacy.
Sherer BA, Hull K, Green O, Basarab G, Hauck S, Hill P, Loch JT 3rd, Mullen G, Bist S, Bryant J, Boriack-Sjodin A, Read J, DeGrace N, Uria-Nickelsen M, Illingworth RN, Eakin AE. Sherer BA, et al. Bioorg Med Chem Lett. 2011 Dec 15;21(24):7416-20. doi: 10.1016/j.bmcl.2011.10.010. Epub 2011 Oct 12. Bioorg Med Chem Lett. 2011. PMID: 22041057
Synthesis and evaluation of triazolones as checkpoint kinase 1 inhibitors.
Oza V, Ashwell S, Brassil P, Breed J, Ezhuthachan J, Deng C, Grondine M, Horn C, Liu D, Lyne P, Newcombe N, Pass M, Read J, Su M, Toader D, Yu D, Yu Y, Zabludoff S. Oza V, et al. Bioorg Med Chem Lett. 2012 Mar 15;22(6):2330-7. doi: 10.1016/j.bmcl.2012.01.043. Epub 2012 Feb 1. Bioorg Med Chem Lett. 2012. PMID: 22342147
Discovery of checkpoint kinase inhibitor (S)-5-(3-fluorophenyl)-N-(piperidin-3-yl)-3-ureidothiophene-2-carboxamide (AZD7762) by structure-based design and optimization of thiophenecarboxamide ureas.
Oza V, Ashwell S, Almeida L, Brassil P, Breed J, Deng C, Gero T, Grondine M, Horn C, Ioannidis S, Liu D, Lyne P, Newcombe N, Pass M, Read J, Ready S, Rowsell S, Su M, Toader D, Vasbinder M, Yu D, Yu Y, Xue Y, Zabludoff S, Janetka J. Oza V, et al. J Med Chem. 2012 Jun 14;55(11):5130-42. doi: 10.1021/jm300025r. Epub 2012 Jun 4. J Med Chem. 2012. PMID: 22551018
Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.
Dakin LA, Block MH, Chen H, Code E, Dowling JE, Feng X, Ferguson AD, Green I, Hird AW, Howard T, Keeton EK, Lamb ML, Lyne PD, Pollard H, Read J, Wu AJ, Zhang T, Zheng X. Dakin LA, et al. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4599-604. doi: 10.1016/j.bmcl.2012.05.098. Epub 2012 Jun 6. Bioorg Med Chem Lett. 2012. PMID: 22727640
Discovery of selective and potent inhibitors of gram-positive bacterial thymidylate kinase (TMK).
Martínez-Botella G, Breen JN, Duffy JE, Dumas J, Geng B, Gowers IK, Green OM, Guler S, Hentemann MF, Hernandez-Juan FA, Joseph-McCarthy D, Kawatkar S, Larsen NA, Lazari O, Loch JT, Macritchie JA, McKenzie AR, Newman JV, Olivier NB, Otterson LG, Owens AP, Read J, Sheppard DW, Keating TA. Martínez-Botella G, et al. Among authors: read j. J Med Chem. 2012 Nov 26;55(22):10010-21. doi: 10.1021/jm3011806. Epub 2012 Oct 24. J Med Chem. 2012. PMID: 23043329
Discovery and optimization of a novel series of potent mutant B-Raf(V600E) selective kinase inhibitors.
Vasbinder MM, Aquila B, Augustin M, Chen H, Cheung T, Cook D, Drew L, Fauber BP, Glossop S, Grondine M, Hennessy E, Johannes J, Lee S, Lyne P, Mörtl M, Omer C, Palakurthi S, Pontz T, Read J, Sha L, Shen M, Steinbacher S, Wang H, Wu A, Ye M. Vasbinder MM, et al. J Med Chem. 2013 Mar 14;56(5):1996-2015. doi: 10.1021/jm301658d. Epub 2013 Feb 27. J Med Chem. 2013. PMID: 23398453
127 results