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279 results

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Page 1
Identification and Optimization of a Ligand-Efficient Benzoazepinone Bromodomain and Extra Terminal (BET) Family Acetyl-Lysine Mimetic into the Oral Candidate Quality Molecule I-BET432.
Humphreys PG, Anderson NA, Bamborough P, Baxter A, Chung CW, Cookson R, Craggs PD, Dalton T, Fournier JCL, Gordon LJ, Gray HF, Gray MW, Gregory R, Hirst DJ, Jamieson C, Jones KL, Kessedjian H, Lugo D, McGonagle G, Patel VK, Patten C, Poole DL, Prinjha RK, Ramirez-Molina C, Rioja I, Seal G, Stafford KAJ, Shah RR, Tape D, Theodoulou NH, Tomlinson L, Ukuser S, Wall ID, Wellaway N, White G. Humphreys PG, et al. Among authors: shah rr. J Med Chem. 2022 Nov 24;65(22):15174-15207. doi: 10.1021/acs.jmedchem.2c01102. Epub 2022 Nov 15. J Med Chem. 2022. PMID: 36378954
Discovery of a Bromodomain and Extraterminal Inhibitor with a Low Predicted Human Dose through Synergistic Use of Encoded Library Technology and Fragment Screening.
Wellaway CR, Amans D, Bamborough P, Barnett H, Bit RA, Brown JA, Carlson NR, Chung CW, Cooper AWJ, Craggs PD, Davis RP, Dean TW, Evans JP, Gordon L, Harada IL, Hirst DJ, Humphreys PG, Jones KL, Lewis AJ, Lindon MJ, Lugo D, Mahmood M, McCleary S, Medeiros P, Mitchell DJ, O'Sullivan M, Le Gall A, Patel VK, Patten C, Poole DL, Shah RR, Smith JE, Stafford KAJ, Thomas PJ, Vimal M, Wall ID, Watson RJ, Wellaway N, Yao G, Prinjha RK. Wellaway CR, et al. Among authors: shah rr. J Med Chem. 2020 Jan 23;63(2):714-746. doi: 10.1021/acs.jmedchem.9b01670. Epub 2020 Jan 6. J Med Chem. 2020. PMID: 31904959
Investigation of Janus Kinase (JAK) Inhibitors for Lung Delivery and the Importance of Aldehyde Oxidase Metabolism.
Wellaway CR, Baldwin IR, Bamborough P, Barker D, Bartholomew MA, Chung CW, Dümpelfeld B, Evans JP, Fazakerley NJ, Homes P, Keeling SP, Lewell XQ, McNab FW, Morley J, Needham D, Neu M, van Oosterhout AJM, Pal A, Reinhard FBM, Rianjongdee F, Robertson CM, Rowland P, Shah RR, Sherriff EB, Sloan LA, Teague S, Thomas DA, Wellaway N, Wojno-Picon J, Woolven JM, Coe DM. Wellaway CR, et al. Among authors: shah rr. J Med Chem. 2022 Jan 13;65(1):633-664. doi: 10.1021/acs.jmedchem.1c01765. Epub 2021 Dec 20. J Med Chem. 2022. PMID: 34928601
Structure-Guided Design of a Domain-Selective Bromodomain and Extra Terminal N-Terminal Bromodomain Chemical Probe.
Bradley E, Fusani L, Chung CW, Craggs PD, Demont EH, Humphreys PG, Mitchell DJ, Phillipou A, Rioja I, Shah RR, Wellaway CR, Prinjha RK, Palmer DS, Kerr WJ, Reid M, Wall ID, Cookson R. Bradley E, et al. Among authors: shah rr. J Med Chem. 2023 Dec 14;66(23):15728-15749. doi: 10.1021/acs.jmedchem.3c00906. Epub 2023 Nov 15. J Med Chem. 2023. PMID: 37967462 Free PMC article.
Structure- and Property-Based Optimization of Efficient Pan-Bromodomain and Extra Terminal Inhibitors to Identify Oral and Intravenous Candidate I-BET787.
Hirst DJ, Bamborough P, Al-Mahdi N, Angell DC, Barnett HA, Baxter A, Bit RA, Brown JA, Chung CW, Craggs PD, Davis RP, Demont EH, Ferrie A, Gordon LJ, Harada I, Ho TCT, Holyer ID, Hooper-Greenhill E, Jones KL, Lindon MJ, Lovatt C, Lugo D, Maller C, McGonagle G, Messenger C, Mitchell DJ, Pascoe DD, Patel VK, Patten C, Poole DL, Shah RR, Rioja I, Stafford KAJ, Tape D, Taylor S, Theodoulou NH, Tomlinson L, Wall ID, Wellaway CR, White G, Prinjha RK, Humphreys PG. Hirst DJ, et al. Among authors: shah rr. J Med Chem. 2024 Jun 27;67(12):10464-10489. doi: 10.1021/acs.jmedchem.4c00959. Epub 2024 Jun 12. J Med Chem. 2024. PMID: 38866424
Unexpected response to a common pacing maneuver during tachycardia.
Pendyala VS, Shah RR, Kumar V, Doppalapudi H. Pendyala VS, et al. Among authors: shah rr. Heart Rhythm. 2024 Nov 28:S1547-5271(24)03629-4. doi: 10.1016/j.hrthm.2024.11.045. Online ahead of print. Heart Rhythm. 2024. PMID: 39613207 No abstract available.
279 results