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Page 1
An improved model for fragment-based lead generation at AstraZeneca.
Fuller N, Spadola L, Cowen S, Patel J, Schönherr H, Cao Q, McKenzie A, Edfeldt F, Rabow A, Goodnow R. Fuller N, et al. Among authors: patel j. Drug Discov Today. 2016 Aug;21(8):1272-83. doi: 10.1016/j.drudis.2016.04.023. Epub 2016 May 11. Drug Discov Today. 2016. PMID: 27179986 Review.
Fragment-based Differential Targeting of PPI Stabilizer Interfaces.
Guillory X, Wolter M, Leysen S, Neves JF, Kuusk A, Genet S, Somsen B, Morrow JK, Rivers E, van Beek L, Patel J, Goodnow R, Schoenherr H, Fuller N, Cao Q, Doveston RG, Brunsveld L, Arkin MR, Castaldi P, Boyd H, Landrieu I, Chen H, Ottmann C. Guillory X, et al. Among authors: patel j. J Med Chem. 2020 Jul 9;63(13):6694-6707. doi: 10.1021/acs.jmedchem.9b01942. Epub 2020 Jun 23. J Med Chem. 2020. PMID: 32501690 Free PMC article.
Potent and selective bivalent inhibitors of BET bromodomains.
Waring MJ, Chen H, Rabow AA, Walker G, Bobby R, Boiko S, Bradbury RH, Callis R, Clark E, Dale I, Daniels DL, Dulak A, Flavell L, Holdgate G, Jowitt TA, Kikhney A, McAlister M, Méndez J, Ogg D, Patel J, Petteruti P, Robb GR, Robers MB, Saif S, Stratton N, Svergun DI, Wang W, Whittaker D, Wilson DM, Yao Y. Waring MJ, et al. Among authors: patel j. Nat Chem Biol. 2016 Dec;12(12):1097-1104. doi: 10.1038/nchembio.2210. Epub 2016 Oct 24. Nat Chem Biol. 2016. PMID: 27775716
Discovery of a Potent and Selective ATAD2 Bromodomain Inhibitor with Antiproliferative Activity in Breast Cancer Models.
Winter-Holt JJ, Bardelle C, Chiarparin E, Dale IL, Davey PRJ, Davies NL, Denz C, Fillery SM, Guérot CM, Han F, Hughes SJ, Kulkarni M, Liu Z, Milbradt A, Moss TA, Niu H, Patel J, Rabow AA, Schimpl M, Shi J, Sun D, Yang D, Guichard S. Winter-Holt JJ, et al. Among authors: patel j. J Med Chem. 2022 Feb 24;65(4):3306-3331. doi: 10.1021/acs.jmedchem.1c01871. Epub 2022 Feb 8. J Med Chem. 2022. PMID: 35133824
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
Discovery and optimization of covalent Bcl-xL antagonists.
Mukherjee H, Su N, Belmonte MA, Hargreaves D, Patel J, Tentarelli S, Aquila B, Grimster NP. Mukherjee H, et al. Among authors: patel j. Bioorg Med Chem Lett. 2019 Dec 1;29(23):126682. doi: 10.1016/j.bmcl.2019.126682. Epub 2019 Sep 13. Bioorg Med Chem Lett. 2019. PMID: 31606346
Identification of a novel series of azabenzimidazole-derived inhibitors of spleen tyrosine kinase.
Kawatkar SP, Barlaam B, Kemmitt P, Simpson I, Watson D, Wang P, Lamont S, Su Q, Boiko S, Ikeda T, Patel J, Pike A, Pollard H, Read J, Sarkar U, Wang H, Wen Q, Yan Z, Dowling JE, Dry H, Edmondson SD. Kawatkar SP, et al. Among authors: patel j. Bioorg Med Chem Lett. 2020 Sep 15;30(18):127393. doi: 10.1016/j.bmcl.2020.127393. Epub 2020 Jul 10. Bioorg Med Chem Lett. 2020. PMID: 32721854
Optimization of a series of novel, potent and selective Macrocyclic SYK inhibitors.
Grimster NP, Gingipalli L, Balazs A, Barlaam B, Boiko S, Boyd S, Dry H, Goldberg FW, Ikeda T, Johnson T, Kawatkar S, Kemmitt P, Lamont S, Lorthioir O, Mfuh A, Patel J, Pike A, Read J, Romero R, Sarkar U, Sha L, Simpson I, Song K, Su Q, Wang H, Watson D, Wu A, Zehnder TE, Zheng X, Li S, Dong Z, Yang D, Song Y, Wang P, Liu X, Dowling JE, Edmondson SD. Grimster NP, et al. Among authors: patel j. Bioorg Med Chem Lett. 2023 Jul 15;91:129352. doi: 10.1016/j.bmcl.2023.129352. Epub 2023 Jun 2. Bioorg Med Chem Lett. 2023. PMID: 37270074
Optimization of a series of potent, selective and orally bioavailable SYK inhibitors.
Grimster NP, Gingipalli L, Barlaam B, Su Q, Zheng X, Watson D, Wang H, Simpson I, Pike A, Balazs A, Boiko S, Ikeda TP, Impastato AC, Jones NH, Kawatkar S, Kemmitt P, Lamont S, Patel J, Read J, Sarkar U, Sha L, Tomlinson RC, Wang H, Wilson DM, Zehnder TE, Wang L, Wang P, Goldberg FW, Shao W, Fawell S, Dry H, Dowling JE, Edmondson SD. Grimster NP, et al. Among authors: patel j. Bioorg Med Chem Lett. 2020 Oct 1;30(19):127433. doi: 10.1016/j.bmcl.2020.127433. Epub 2020 Jul 24. Bioorg Med Chem Lett. 2020. PMID: 32717371
6,328 results