Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation O Gilan, I Rioja, K Knezevic, MJ Bell, MM Yeung, NR Harker, EYN Lam, ... Science 368 (6489), 387-394, 2020 | 323 | 2020 |
Click chemistry enables preclinical evaluation of targeted epigenetic therapies DS Tyler, J Vappiani, T Cañeque, EYN Lam, A Ward, O Gilan, YC Chan, ... Science 356 (6345), 1397-1401, 2017 | 132 | 2017 |
Discovery of a bromodomain and extraterminal inhibitor with a low predicted human dose through synergistic use of encoded library technology and fragment screening CR Wellaway, D Amans, P Bamborough, H Barnett, RA Bit, JA Brown, ... Journal of Medicinal Chemistry 63 (2), 714-746, 2020 | 54 | 2020 |
Structure-based design of a bromodomain and extraterminal domain (BET) inhibitor selective for the N-terminal bromodomains that retains an anti-inflammatory and … CR Wellaway, P Bamborough, SG Bernard, C Chung, PD Craggs, ... Journal of Medicinal Chemistry 63 (17), 9020-9044, 2020 | 40 | 2020 |
Furopyridines as bromodomain inhibitors D Amans, P Bamborough, MD Barker, RA Bit, JA Brown, M Campbell, ... US Patent 9,670,221, 2017 | 31 | 2017 |
Conformationally rigid pyrazoloquinazoline α-amino acids: one-and two-photon induced fluorescence JD Bell, AH Harkiss, D Nobis, E Malcolm, A Knuhtsen, CR Wellaway, ... Chemical Communications 56 (12), 1887-1890, 2020 | 25 | 2020 |
Synthesis and photophysical properties of benzotriazole-derived unnatural α-amino acids JD Bell, TEF Morgan, N Buijs, AH Harkiss, CR Wellaway, A Sutherland The Journal of Organic Chemistry 84 (16), 10436-10448, 2019 | 20 | 2019 |
2, 3-disubstituted 1-acyl-4-amino-1, 2, 3, 4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors D Amans, SJ Atkinson, LA Harrison, DJ Hirst, RP Law, M Lindon, ... US Patent 9,637,456, 2017 | 20 | 2017 |
Design, synthesis, and characterization of I-BET567, a pan-bromodomain and extra terminal (BET) bromodomain oral candidate PG Humphreys, SJ Atkinson, P Bamborough, RA Bit, C Chung, ... Journal of Medicinal Chemistry 65 (3), 2262-2287, 2022 | 13 | 2022 |
2, 3-Disubstituted 1-acyl-4-amino-1, 2, 3, 4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors D Amans, SJ Atkinson, LA Harrison, DJ Hirst, RP Law, M Lindon, ... US Patent 10,583,139, 2020 | 11 | 2020 |
Investigation of Janus kinase (JAK) inhibitors for lung delivery and the importance of aldehyde oxidase metabolism CR Wellaway, IR Baldwin, P Bamborough, D Barker, MA Bartholomew, ... Journal of Medicinal Chemistry 65 (1), 633-664, 2021 | 9 | 2021 |
Furopyridines as bromodomain inhibitors D AMANS, P Bamborough, MD Barker, RA Bit, JA Brown, M Campbell, ... | 8 | 2014 |
2, 3-disubstituted 1-acyl-4-amino-1, 2, 3, 4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors D Amans, SJ Atkinson, LA Harrison, DJ Hirst, RP Law, M Lindon, ... US Patent 10,034,881, 2018 | 6 | 2018 |
Tetrahydroquinoline derivatives as bromodomain inhibitors SJ Atkinson, DJ Hirst, PG Humphreys, MJ Lindon, AG Preston, JT Seal, ... US Patent 10,059,699, 2018 | 5 | 2018 |
Stereoselective synthesis of 2, 6-trans-4-oxopiperidines using an acid-mediated 6-endo-trig cyclisation JD Bell, AH Harkiss, CR Wellaway, A Sutherland Organic & Biomolecular Chemistry 16 (35), 6410-6422, 2018 | 5 | 2018 |
Structure-guided design of a domain-selective bromodomain and extra terminal N-terminal bromodomain chemical probe E Bradley, L Fusani, C Chung, PD Craggs, EH Demont, PG Humphreys, ... Journal of Medicinal Chemistry 66 (23), 15728-15749, 2023 | 3 | 2023 |
2-(azaindol-2-yl) benzimidazoles as Pad4 Inhibitors SJ Atkinson, MD Barker, M Campbell, H Diallo, C Douault, NS Garton, ... US Patent 9,127,003, 2015 | 3 | 2015 |
Chemical compounds FL Atkinson, JM Axten, M Cichy-Knight, ML Moore, VK Patel, X Tian, ... US Patent 8,383,635, 2013 | 3 | 2013 |
2, 3-disubstituted 1-acyl-4-amino-1, 2, 3, 4-tetrahydroquinoline derivatives and their use as bromodomain inhibitors D Amans, SJ Atkinson, LA Harrison, DJ Hirst, RP Law, M Lindon, ... US Patent 11,478,478, 2022 | 2 | 2022 |
Thieno [3, 2-C] pyridin-4 (5H)-ones as BET inhibitors D Amans, P Bamborough, RA Bit, JA Brown, M Campbell, MJ Lindon, ... US Patent 9,663,533, 2017 | 2 | 2017 |