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11,209 results

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Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265P Mutant Diffuse Large B Cell Lymphoma.
Degorce SL, Anjum R, Bloecher A, Carbajo RJ, Dillman KS, Drew L, Halsall CT, Lenz EM, Lindsay NA, Mayo MF, Pink JH, Robb GR, Rosen A, Scott JS, Xue Y. Degorce SL, et al. Among authors: xue y. J Med Chem. 2019 Nov 14;62(21):9918-9930. doi: 10.1021/acs.jmedchem.9b01346. Epub 2019 Nov 1. J Med Chem. 2019. PMID: 31622099
Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4.
Degorce SL, Anjum R, Dillman KS, Drew L, Groombridge SD, Halsall CT, Lenz EM, Lindsay NA, Mayo MF, Pink JH, Robb GR, Scott JS, Stokes S, Xue Y. Degorce SL, et al. Among authors: xue y. Bioorg Med Chem. 2018 Feb 15;26(4):913-924. doi: 10.1016/j.bmc.2018.01.008. Epub 2018 Jan 17. Bioorg Med Chem. 2018. PMID: 29398441
Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors.
Degorce SL, Aagaard A, Anjum R, Cumming IA, Diène CR, Fallan C, Johnson T, Leuchowius KJ, Orton AL, Pearson S, Robb GR, Rosen A, Scarfe GB, Scott JS, Smith JM, Steward OR, Terstiege I, Tucker MJ, Turner P, Wilkinson SD, Wrigley GL, Xue Y. Degorce SL, et al. Among authors: xue y. Bioorg Med Chem. 2020 Dec 1;28(23):115815. doi: 10.1016/j.bmc.2020.115815. Epub 2020 Oct 15. Bioorg Med Chem. 2020. PMID: 33091850
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: xue y. 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 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. Among authors: xue y. J Med Chem. 2012 Jun 14;55(11):5130-42. doi: 10.1021/jm300025r. Epub 2012 Jun 4. J Med Chem. 2012. PMID: 22551018
Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.
Hennessy EJ, Oza V, Adam A, Byth K, Castriotta L, Grewal G, Hamilton GA, Kamhi VM, Lewis P, Li D, Lyne P, Öster L, Rooney MT, Saeh JC, Sha L, Su Q, Wen S, Xue Y, Yang B. Hennessy EJ, et al. Among authors: xue y. J Med Chem. 2015 Sep 10;58(17):7057-75. doi: 10.1021/acs.jmedchem.5b01078. Epub 2015 Aug 26. J Med Chem. 2015. PMID: 26291341
Potent and Orally Bioavailable Inverse Agonists of RORγt Resulting from Structure-Based Design.
Narjes F, Xue Y, von Berg S, Malmberg J, Llinas A, Olsson RI, Jirholt J, Grindebacke H, Leffler A, Hossain N, Lepistö M, Thunberg L, Leek H, Aagaard A, McPheat J, Hansson EL, Bäck E, Tångefjord S, Chen R, Xiong Y, Hongbin G, Hansson TG. Narjes F, et al. Among authors: xue y. J Med Chem. 2018 Sep 13;61(17):7796-7813. doi: 10.1021/acs.jmedchem.8b00783. Epub 2018 Aug 27. J Med Chem. 2018. PMID: 30095900
Discovery of novel potent and highly selective glycogen synthase kinase-3β (GSK3β) inhibitors for Alzheimer's disease: design, synthesis, and characterization of pyrazines.
Berg S, Bergh M, Hellberg S, Högdin K, Lo-Alfredsson Y, Söderman P, von Berg S, Weigelt T, Ormö M, Xue Y, Tucker J, Neelissen J, Jerning E, Nilsson Y, Bhat R. Berg S, et al. Among authors: xue y. J Med Chem. 2012 Nov 8;55(21):9107-19. doi: 10.1021/jm201724m. Epub 2012 Apr 27. J Med Chem. 2012. PMID: 22489897
Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors.
Malmström J, Viklund J, Slivo C, Costa A, Maudet M, Sandelin C, Hiller G, Olsson LL, Aagaard A, Geschwindner S, Xue Y, Vasänge M. Malmström J, et al. Among authors: xue y. Bioorg Med Chem Lett. 2012 Sep 15;22(18):5919-23. doi: 10.1016/j.bmcl.2012.07.068. Epub 2012 Jul 25. Bioorg Med Chem Lett. 2012. PMID: 22889803
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