The promise and peril of chemical probes CH Arrowsmith, JE Audia, C Austin, J Baell, J Bennett, J Blagg, C Bountra, ... Nature chemical biology 11 (8), 536-541, 2015 | 863 | 2015 |
Phosphatidylinositol 3-kinase couples the interleukin-2 receptor to the cell cycle regulator E2F P Brennan, JW Babbage, BMT Burgering, B Groner, K Reif, DA Cantrell Immunity 7 (5), 679-689, 1997 | 527 | 1997 |
RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain S Picaud, C Wells, I Felletar, D Brotherton, S Martin, P Savitsky, ... Proceedings of the National Academy of Sciences 110 (49), 19754-19759, 2013 | 496 | 2013 |
Discovery and optimization of small-molecule ligands for the CBP/p300 bromodomains DA Hay, O Fedorov, S Martin, DC Singleton, C Tallant, C Wells, S Picaud, ... Journal of the American Chemical Society 136 (26), 9308-9319, 2014 | 344 | 2014 |
K2P channel gating mechanisms revealed by structures of TREK-2 and a complex with Prozac YY Dong, ACW Pike, A Mackenzie, C McClenaghan, P Aryal, L Dong, ... Science 347 (6227), 1256-1259, 2015 | 333 | 2015 |
PFI-1, a highly selective protein interaction inhibitor, targeting BET Bromodomains S Picaud, D Da Costa, A Thanasopoulou, P Filippakopoulos, PV Fish, ... Cancer research 73 (11), 3336-3346, 2013 | 298 | 2013 |
Differential cognitive effects of colloid cysts in the third ventricle that spare or compromise the fornix JP Aggleton, D McMackin, K Carpenter, J Hornak, N Kapur, S Halpin, ... Brain 123 (4), 800-815, 2000 | 278 | 2000 |
Rapid covalent-probe discovery by electrophile-fragment screening E Resnick, A Bradley, J Gan, A Douangamath, T Krojer, R Sethi, ... Journal of the American Chemical Society 141 (22), 8951-8968, 2019 | 276 | 2019 |
CBP30, a selective CBP/p300 bromodomain inhibitor, suppresses human Th17 responses A Hammitzsch, C Tallant, O Fedorov, A O’Mahony, PE Brennan, DA Hay, ... Proceedings of the National Academy of Sciences 112 (34), 10768-10773, 2015 | 265 | 2015 |
Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit PV Fish, P Filippakopoulos, G Bish, PE Brennan, ME Bunnage, AS Cook, ... Journal of medicinal chemistry 55 (22), 9831-9837, 2012 | 258 | 2012 |
Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy S Picaud, O Fedorov, A Thanasopoulou, K Leonards, K Jones, J Meier, ... Cancer research 75 (23), 5106-5119, 2015 | 253 | 2015 |
Regulation of an activated S6 kinase 1 variant reveals a novel mammalian target of rapamycin phosphorylation site M Saitoh, N Pullen, P Brennan, D Cantrell, PB Dennis, G Thomas Journal of Biological Chemistry 277 (22), 20104-20112, 2002 | 228 | 2002 |
Progress in the development and application of small molecule inhibitors of bromodomain–acetyl-lysine interactions DS Hewings, TPC Rooney, LE Jennings, DA Hay, CJ Schofield, ... Journal of medicinal chemistry 55 (22), 9393-9413, 2012 | 219 | 2012 |
LP99: discovery and synthesis of the first selective BRD7/9 bromodomain inhibitor PGK Clark, LCC Vieira, C Tallant, O Fedorov, DC Singleton, CM Rogers, ... Angewandte Chemie 127 (21), 6315-6319, 2015 | 214 | 2015 |
Recent progress in histone demethylase inhibitors TE McAllister, KS England, RJ Hopkinson, PE Brennan, A Kawamura, ... Journal of medicinal chemistry 59 (4), 1308-1329, 2016 | 196 | 2016 |
Fragment-based hit identification: thinking in 3D AD Morley, A Pugliese, K Birchall, J Bower, P Brennan, N Brown, ... Drug Discovery Today 18 (23-24), 1221-1227, 2013 | 187 | 2013 |
Structural analysis of human KDM5B guides histone demethylase inhibitor development C Johansson, S Velupillai, A Tumber, A Szykowska, ES Hookway, ... Nature chemical biology 12 (7), 539-545, 2016 | 186 | 2016 |
A genetics-led approach defines the drug target landscape of 30 immune-related traits H Fang, H De Wolf, B Knezevic, KL Burnham, J Osgood, A Sanniti, ... Nature genetics 51 (7), 1082-1091, 2019 | 184 | 2019 |
p70s6k Integrates Phosphatidylinositol 3-Kinase and Rapamycin-Regulated Signals for E2F Regulation in T Lymphocytes P Brennan, JW Babbage, G Thomas, D Cantrell Molecular and cellular biology 19 (7), 4729-4738, 1999 | 181 | 1999 |
A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP (2), an atypical bromodomain OB Cox, T Krojer, P Collins, O Monteiro, R Talon, A Bradley, O Fedorov, ... Chemical science 7 (3), 2322-2330, 2016 | 179 | 2016 |