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Page 1
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. Among authors: code e. 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 Pyrazolo[1,5-a]pyrimidine B-Cell Lymphoma 6 (BCL6) Binders and Optimization to High Affinity Macrocyclic Inhibitors.
McCoull W, Abrams RD, Anderson E, Blades K, Barton P, Box M, Burgess J, Byth K, Cao Q, Chuaqui C, Carbajo RJ, Cheung T, Code E, Ferguson AD, Fillery S, Fuller NO, Gangl E, Gao N, Grist M, Hargreaves D, Howard MR, Hu J, Kemmitt PD, Nelson JE, O'Connell N, Prince DB, Raubo P, Rawlins PB, Robb GR, Shi J, Waring MJ, Whittaker D, Wylot M, Zhu X. McCoull W, et al. Among authors: code e. J Med Chem. 2017 May 25;60(10):4386-4402. doi: 10.1021/acs.jmedchem.7b00359. Epub 2017 May 9. J Med Chem. 2017. PMID: 28485934
Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6.
McCoull W, Cheung T, Anderson E, Barton P, Burgess J, Byth K, Cao Q, Castaldi MP, Chen H, Chiarparin E, Carbajo RJ, Code E, Cowan S, Davey PR, Ferguson AD, Fillery S, Fuller NO, Gao N, Hargreaves D, Howard MR, Hu J, Kawatkar A, Kemmitt PD, Leo E, Molina DM, O'Connell N, Petteruti P, Rasmusson T, Raubo P, Rawlins PB, Ricchiuto P, Robb GR, Schenone M, Waring MJ, Zinda M, Fawell S, Wilson DM. McCoull W, et al. Among authors: code e. ACS Chem Biol. 2018 Nov 16;13(11):3131-3141. doi: 10.1021/acschembio.8b00698. Epub 2018 Oct 17. ACS Chem Biol. 2018. PMID: 30335946
Rapid Identification of Novel Allosteric PRC2 Inhibitors.
Read JA, Tart J, Rawlins PB, Gregson C, Jones K, Gao N, Zhu X, Tomlinson R, Code E, Cheung T, Chen H, Kawatkar SP, Bloecher A, Bagal S, O'Donovan DH, Robinson J. Read JA, et al. Among authors: code e. ACS Chem Biol. 2019 Oct 18;14(10):2134-2140. doi: 10.1021/acschembio.9b00468. Epub 2019 Sep 23. ACS Chem Biol. 2019. PMID: 31525019
EED-Targeted PROTACs Degrade EED, EZH2, and SUZ12 in the PRC2 Complex.
Hsu JH, Rasmusson T, Robinson J, Pachl F, Read J, Kawatkar S, O' Donovan DH, Bagal S, Code E, Rawlins P, Argyrou A, Tomlinson R, Gao N, Zhu X, Chiarparin E, Jacques K, Shen M, Woods H, Bednarski E, Wilson DM, Drew L, Castaldi MP, Fawell S, Bloecher A. Hsu JH, et al. Among authors: code e. Cell Chem Biol. 2020 Jan 16;27(1):41-46.e17. doi: 10.1016/j.chembiol.2019.11.004. Epub 2019 Nov 27. Cell Chem Biol. 2020. PMID: 31786184 Free article.
Discovery of a Novel Benzodiazepine Series of Cbl-b Inhibitors for the Enhancement of Antitumor Immunity.
Boerth JA, Chinn AJ, Schimpl M, Bommakanti G, Chan C, Code EL, Giblin KA, Gohlke A, Hansel CS, Jin M, Kavanagh SL, Lamb ML, Lane JS, Larner CJB, Mfuh AM, Moore RK, Puri T, Quinn TR, Ye M, Robbins KJ, Gancedo-Rodrigo M, Tang H, Walsh J, Ware J, Wrigley GL, Reddy IK, Zhang Y, Grimster NP. Boerth JA, et al. Among authors: code el. ACS Med Chem Lett. 2023 Nov 17;14(12):1848-1856. doi: 10.1021/acsmedchemlett.3c00439. eCollection 2023 Dec 14. ACS Med Chem Lett. 2023. PMID: 38116444 Free PMC article.
Discovery, Optimization, and Biological Evaluation of Arylpyridones as Cbl-b Inhibitors.
Mfuh AM, Boerth JA, Bommakanti G, Chan C, Chinn AJ, Code E, Fricke PJ, Giblin KA, Gohlke A, Hansel C, Hariparsad N, Hughes SJ, Jin M, Kantae V, Kavanagh SL, Lamb ML, Lane J, Moore R, Puri T, Quinn TR, Reddy I, Robb GR, Robbins KJ, Gancedo Rodrigo M, Schimpl M, Singh B, Singh M, Tang H, Thomson C, Walsh JJ, Ware J, Watson IDG, Ye MW, Wrigley GL, Zhang AX, Zhang Y, Grimster NP. Mfuh AM, et al. Among authors: code e. J Med Chem. 2024 Jan 25;67(2):1500-1512. doi: 10.1021/acs.jmedchem.3c02083. Epub 2024 Jan 16. J Med Chem. 2024. PMID: 38227216
Accelerated Discovery of Carbamate Cbl-b Inhibitors Using Generative AI Models and Structure-Based Drug Design.
Quinn TR, Giblin KA, Thomson C, Boerth JA, Bommakanti G, Braybrooke E, Chan C, Chinn AJ, Code E, Cui C, Fan Y, Grimster NP, Kohara K, Lamb ML, Ma L, Mfuh AM, Robb GR, Robbins KJ, Schimpl M, Tang H, Ware J, Wrigley GL, Xue L, Zhang Y, Zhu H, Hughes SJ. Quinn TR, et al. Among authors: code e. J Med Chem. 2024 Aug 22;67(16):14210-14233. doi: 10.1021/acs.jmedchem.4c01034. Epub 2024 Aug 12. J Med Chem. 2024. PMID: 39132828
17 results