An improved procedure for the preparation of the Garner aldehyde and its use for the synthesis of N-protected 1-halo-2-(R)-amino-3-butenes A McKillop, RJK Taylor, RJ Watson, N Lewis SYNTHESIS-STUTTGART, 31-33, 1994 | 161 | 1994 |
CXCR3 antagonist NBI-74330 attenuates atherosclerotic plaque formation in LDL receptor–deficient mice EJA Van Wanrooij, SCA de Jager, T van Es, P de Vos, HL Birch, DA Owen, ... Arteriosclerosis, thrombosis, and vascular biology 28 (2), 251-257, 2008 | 134 | 2008 |
1, 3-Dimethyl benzimidazolones are potent, selective inhibitors of the BRPF1 bromodomain EH Demont, P Bamborough, C Chung, PD Craggs, D Fallon, LJ Gordon, ... ACS medicinal chemistry letters 5 (11), 1190-1195, 2014 | 99 | 2014 |
Structure-based optimization of naphthyridones into potent ATAD2 bromodomain inhibitors P Bamborough, C Chung, RC Furze, P Grandi, AM Michon, RJ Sheppard, ... Journal of Medicinal Chemistry 58 (15), 6151-6178, 2015 | 98 | 2015 |
Fragment-based discovery of low-micromolar ATAD2 bromodomain inhibitors EH Demont, C Chung, RC Furze, P Grandi, AM Michon, C Wellaway, ... Journal of medicinal chemistry 58 (14), 5649-5673, 2015 | 96 | 2015 |
An enantioselective synthesis of sulphonamide hydroxamic acids as matrix metalloproteinase inhibitors RJ Watson, D Batty, AD Baxter, DR Hannah, DA Owen, JG Montana Tetrahedron Letters 43 (4), 683-685, 2002 | 92 | 2002 |
A chemical probe for the ATAD2 bromodomain P Bamborough, C Chung, EH Demont, RC Furze, AJ Bannister, KH Che, ... Angewandte Chemie 128 (38), 11554-11558, 2016 | 83 | 2016 |
A simple and efficient procedure for the preparation of p-quinols by hypervalent iodine oxidation of phenols and phenol tripropylsilyl ethers A McKillop, L McLaren, RJK Taylor Journal of the Chemical Society, Perkin Transactions 1, 2047-2048, 1994 | 79 | 1994 |
Copper-catalyzed rearrangement of oximes into primary amides SK Sharma, SD Bishopp, CL Allen, R Lawrence, MJ Bamford, AA Lapkin, ... Tetrahedron letters 52 (33), 4252-4255, 2011 | 78 | 2011 |
Iridium-catalyzed formylation of amines with paraformaldehyde O Saidi, MJ Bamford, AJ Blacker, J Lynch, SP Marsden, P Plucinski, ... Tetrahedron Letters 51 (44), 5804-5806, 2010 | 78 | 2010 |
A simple and efficient procedure for the preparation of chiral 2-oxazolidinones from α-amino acids N Lewis, A McKillop, RJK Taylor, RJ Watson Synthetic communications 25 (4), 561-568, 1995 | 76 | 1995 |
GSK789: a selective inhibitor of the first bromodomains (BD1) of the bromo and extra terminal domain (BET) proteins RJ Watson, P Bamborough, H Barnett, C Chung, R Davis, L Gordon, ... Journal of Medicinal Chemistry 63 (17), 9045-9069, 2020 | 68 | 2020 |
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 | 65 | 2011 |
GSK6853, a chemical probe for inhibition of the BRPF1 bromodomain P Bamborough, HA Barnett, I Becher, MJ Bird, C Chung, PD Craggs, ... ACS medicinal chemistry letters 7 (6), 552-557, 2016 | 62 | 2016 |
Synthesis and structure–activity relationships of guanine analogues as phosphodiesterase 7 (PDE7) inhibitors MJ Barnes, N Cooper, RJ Davenport, HJ Dyke, FP Galleway, FCA Galvin, ... Bioorganic & medicinal chemistry letters 11 (8), 1081-1083, 2001 | 60 | 2001 |
Pt/C catalysed direct reductive amination of nitriles with primary amines in a continuous flow multichannel microreactor SK Sharma, J Lynch, AM Sobolewska, P Plucinski, RJ Watson, ... Catalysis Science & Technology 3 (1), 85-88, 2013 | 57* | 2013 |
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 | 52 | 2020 |
Identification and structure–activity relationships of 1-aryl-3-piperidin-4-yl-urea derivatives as CXCR3 receptor antagonists DR Allen, A Bolt, GA Chapman, RL Knight, JWG Meissner, DA Owen, ... Bioorganic & medicinal chemistry letters 17 (3), 697-701, 2007 | 47 | 2007 |
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 | 44 | 2020 |
Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3 ME Hayes, GA Wallace, P Grongsaard, A Bischoff, DM George, W Miao, ... Bioorganic & medicinal chemistry letters 18 (5), 1573-1576, 2008 | 44 | 2008 |