Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy A Hall, A Billinton, SH Brown, NM Clayton, A Chowdhury, GMP Giblin, ... Bioorganic & medicinal chemistry letters 18 (11), 3392-3399, 2008 | 98 | 2008 |
Discovery of a potent, cell penetrant, and selective p300/CBP-associated factor (PCAF)/general control nonderepressible 5 (GCN5) bromodomain chemical probe PG Humphreys, P Bamborough, C Chung, PD Craggs, L Gordon, ... Journal of medicinal chemistry 60 (2), 695-709, 2017 | 94 | 2017 |
Cell Penetrant Inhibitors of the KDM4 and KDM5 Families of Histone Lysine Demethylases. 2. Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives SM Westaway, AGS Preston, MD Barker, F Brown, JA Brown, M Campbell, ... Journal of medicinal chemistry 59 (4), 1370-1387, 2016 | 76 | 2016 |
Discovery of GSK143, a highly potent, selective and orally efficacious spleen tyrosine kinase inhibitor J Liddle, FL Atkinson, MD Barker, PS Carter, NR Curtis, RP Davis, ... Bioorganic & medicinal chemistry letters 21 (20), 6188-6194, 2011 | 68 | 2011 |
Cell penetrant inhibitors of the KDM4 and KDM5 families of histone lysine demethylases. 1. 3-Amino-4-pyridine carboxylate derivatives SM Westaway, AGS Preston, MD Barker, F Brown, JA Brown, M Campbell, ... Journal of Medicinal Chemistry 59 (4), 1357-1369, 2016 | 62 | 2016 |
The optimization of a novel, weak bromo and extra terminal domain (BET) bromodomain fragment ligand to a potent and selective second bromodomain (BD2) inhibitor JT Seal, SJ Atkinson, H Aylott, P Bamborough, C Chung, RCB Copley, ... Journal of Medicinal Chemistry 63 (17), 9093-9126, 2020 | 49 | 2020 |
Tetrahydroquinoline derivatives and their pharmaceutical use EH Demont, NS Garton, RLM Gosmini, TGC Hayhow, J Seal, DM Wilson, ... US Patent 8,697,725, 2014 | 34 | 2014 |
Discovery of GSK345931A: An EP1 receptor antagonist with efficacy in preclinical models of inflammatory pain A Hall, SH Brown, C Budd, NM Clayton, GMP Giblin, P Goldsmith, ... Bioorganic & medicinal chemistry letters 19 (2), 497-501, 2009 | 34 | 2009 |
A Buchwald–Hartwig Protocol to Enable Rapid Linker Exploration of Cereblon E3‐Ligase PROTACs TG Hayhow, REA Borrows, CR Diène, G Fairley, C Fallan, SM Fillery, ... Chemistry–A European Journal 26 (70), 16818-16823, 2020 | 23 | 2020 |
Orally active C-6 heteroaryl-and heterocyclyl-substituted imidazo [1, 2-a] pyridine acid pump antagonists (APAs) N Bailey, MJ Bamford, D Brissy, J Brookfield, E Demont, R Elliott, ... Bioorganic & medicinal chemistry letters 19 (13), 3602-3606, 2009 | 23 | 2009 |
Template-hopping approach leads to potent, selective, and highly soluble bromo and extraterminal domain (BET) second bromodomain (BD2) inhibitors HE Aylott, SJ Atkinson, P Bamborough, A Bassil, C Chung, L Gordon, ... Journal of Medicinal Chemistry 64 (6), 3249-3281, 2021 | 22 | 2021 |
Modulation of macrophage inflammatory function through selective inhibition of the epigenetic reader protein SP140 M Ghiboub, J Koster, PD Craggs, AYF Li Yim, A Shillings, S Hutchinson, ... BMC biology 20 (1), 182, 2022 | 18 | 2022 |
Discovery of brain penetrant, soluble, pyrazole amide EP1 receptor antagonists A Hall, A Billinton, AK Bristow, SH Brown, A Chowdhury, L Cutler, ... Bioorganic & medicinal chemistry letters 18 (14), 4027-4032, 2008 | 18 | 2008 |
Evaluation of basic, heterocyclic ring systems as templates for use as potassium competitive acid blockers (pCABs) T Panchal, N Bailey, M Bamford, E Demont, R Elliott, I Farre-Gutierrez, ... Bioorganic & medicinal chemistry letters 19 (23), 6813-6817, 2009 | 16 | 2009 |
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 | 14 | 2022 |
Pyridinone dicarboxamide for use as bromodomain inhibitors SJ Atkinson, EH Demont, LA Harrison, TGC Hayhow, D House, MJ Lindon, ... | 13 | 2017 |
Structural and physicochemical features of oral PROTACs M Schade, JS Scott, TG Hayhow, A Pike, I Terstiege, M Ahlqvist, ... Journal of Medicinal Chemistry 67 (15), 13106-13116, 2024 | 9 | 2024 |
Degradation by Design: New Cyclin K Degraders from Old CDK Inhibitors KL Thomas, H Bouguenina, DSJ Miller, FJ Sialana, TG Hayhow, ... ACS Chemical Biology 19 (1), 173-184, 2024 | 6 | 2024 |
Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTAC TG Hayhow, B Williamson, M Lawson, N Cureton, EL Braybrooke, ... Communications Biology 7 (1), 563, 2024 | 5 | 2024 |
Pyrazole compounds as prostaglandin receptors ligands EA Conway, GMP Giblin, M Gibson, A Hall, TGC Hayhow, MP Healy, ... US Patent App. 11/912,402, 2009 | 5 | 2009 |