Discovery of (2, 4-Dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1, 3-dihydroisoindol-2-yl] methanone (AT13387), a Novel Inhibitor of the Molecular Chaperone … AJ Woodhead, H Angove, MG Carr, G Chessari, M Congreve, JE Coyle, ... Journal of medicinal chemistry 53 (16), 5956-5969, 2010 | 302 | 2010 |
Application of fragment-based lead generation to the discovery of novel, cyclic amidine β-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency PD Edwards, JS Albert, M Sylvester, D Aharony, D Andisik, O Callaghan, ... Journal of medicinal chemistry 50 (24), 5912-5925, 2007 | 254 | 2007 |
Fragment-based drug discovery applied to Hsp90. Discovery of two lead series with high ligand efficiency CW Murray, MG Carr, O Callaghan, G Chessari, M Congreve, S Cowan, ... Journal of medicinal chemistry 53 (16), 5942-5955, 2010 | 222 | 2010 |
Apo and inhibitor complex structures of BACE (β-secretase) S Patel, L Vuillard, A Cleasby, CW Murray, J Yon Journal of molecular biology 343 (2), 407-416, 2004 | 221 | 2004 |
Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of β-secretase M Congreve, D Aharony, J Albert, O Callaghan, J Campbell, RAE Carr, ... Journal of medicinal chemistry 50 (6), 1124-1132, 2007 | 177 | 2007 |
Application of fragment screening by X-ray crystallography to β-secretase CW Murray, O Callaghan, G Chessari, A Cleasby, M Congreve, ... Journal of medicinal chemistry 50 (6), 1116-1123, 2007 | 165 | 2007 |
High-throughput X-ray crystallography for drug discovery TL Blundell, S Patel Current opinion in pharmacology 4 (5), 490-496, 2004 | 161 | 2004 |
Potent and selective bivalent inhibitors of BET bromodomains MJ Waring, H Chen, AA Rabow, G Walker, R Bobby, S Boiko, ... Nature chemical biology 12 (12), 1097-1104, 2016 | 137 | 2016 |
Small molecule binding sites on the Ras: SOS complex can be exploited for inhibition of Ras activation JJG Winter, M Anderson, K Blades, C Brassington, AL Breeze, C Chresta, ... Journal of medicinal chemistry 58 (5), 2265-2274, 2015 | 133 | 2015 |
X-ray structure of yeast Hal2p, a major target of lithium and sodium toxicity, and identification of framework interactions determining cation sensitivity A Albert, L Yenush, MR Gil-Mascarell, PL Rodriguez, S Patel, ... Journal of molecular biology 295 (4), 927-938, 2000 | 91 | 2000 |
Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3 R)-4-[2-[4-[1-(3-Methoxy-[1, 2, 4] triazolo [4, 3-b … RH Bradbury, R Callis, GR Carr, H Chen, E Clark, L Feron, S Glossop, ... Journal of medicinal chemistry 59 (17), 7801-7817, 2016 | 78 | 2016 |
An improved model for fragment-based lead generation at AstraZeneca N Fuller, L Spadola, S Cowen, J Patel, H Schönherr, Q Cao, A McKenzie, ... Drug Discovery Today 21 (8), 1272-1283, 2016 | 77 | 2016 |
Fragment-based discovery of potent and selective DDR1/2 inhibitors CW Murray, V Berdini, IM Buck, ME Carr, A Cleasby, JE Coyle, JE Curry, ... ACS medicinal chemistry letters 6 (7), 798-803, 2015 | 64 | 2015 |
Crystal structure of an enzyme displaying both inositol-polyphosphate-1-phosphatase and 3′-phosphoadenosine-5′-phosphate phosphatase activities: a novel target of lithium therapy S Patel, L Yenush, PL Rodrıguez, R Serrano, TL Blundell Journal of molecular biology 315 (4), 677-685, 2002 | 55 | 2002 |
Structural enzymology of Li+-sensitive/Mg2+-dependent phosphatases S Patel, M Martınez-Ripoll, TL Blundell, A Albert Journal of molecular biology 320 (5), 1087-1094, 2002 | 45 | 2002 |
Purification and biochemical properties of soluble recombinant human Bax S Lewis, SS Bethell, S Patel, JC Martinou, B Antonsson Protein expression and purification 13 (1), 120-126, 1998 | 42 | 1998 |
Substituted pyrrolo [3, 4-b] pyridinamines and pharmaceutical compositions G Chessari, MS Congreve, J Holenz, C Murray, S Patel, L Rakos, ... US Patent 7,629,356, 2009 | 40 | 2009 |
Fragment-based differential targeting of PPI stabilizer interfaces X Guillory, M Wolter, S Leysen, JF Neves, A Kuusk, S Genet, B Somsen, ... Journal of medicinal chemistry 63 (13), 6694-6707, 2020 | 38 | 2020 |
Structural characterization of degrader-induced ternary complexes using hydrogen–deuterium exchange mass spectrometry and computational modeling: implications for structure … SJ Eron, H Huang, RV Agafonov, ME Fitzgerald, J Patel, RE Michael, ... ACS Chemical Biology 16 (11), 2228-2243, 2021 | 36 | 2021 |
Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase CN Johnson, V Berdini, L Beke, P Bonnet, D Brehmer, JE Coyle, PJ Day, ... ACS medicinal chemistry letters 6 (1), 25-30, 2015 | 34 | 2015 |