| Identification of a novel inhibitor of mitogen-activated protein kinase kinase MF Favata, KY Horiuchi, EJ Manos, AJ Daulerio, DA Stradley, WS Feeser, ... Journal of Biological Chemistry 273 (29), 18623-18632, 1998 | 3632 | 1998 |
| Enzymes: a practical introduction to structure, mechanism, and data analysis RA Copeland John Wiley & Sons, 2023 | 2206* | 2023 |
| Evaluation of enzyme inhibitors in drug discovery: a guide for medicinal chemists and pharmacologists RA Copeland John Wiley & Sons, 2013 | 1633 | 2013 |
| Drug–target residence time and its implications for lead optimization RA Copeland, DL Pompliano, TD Meek Nature reviews Drug discovery 5 (9), 730-739, 2006 | 1542 | 2006 |
| Selective killing of mixed lineage leukemia cells by a potent small-molecule DOT1L inhibitor SR Daigle, EJ Olhava, CA Therkelsen, CR Majer, CJ Sneeringer, J Song, ... Cancer cell 20 (1), 53-65, 2011 | 1002 | 2011 |
| A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells SK Knutson, TJ Wigle, NM Warholic, CJ Sneeringer, CJ Allain, CR Klaus, ... Nature chemical biology 8 (11), 890-896, 2012 | 882 | 2012 |
| Purification and cloning of aggrecanase-1: a member of the ADAMTS family of proteins MD Tortorella, TC Burn, MA Pratta, I Abbaszade, JM Hollis, R Liu, ... Science 284 (5420), 1664-1666, 1999 | 864 | 1999 |
| 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 | 833 | 2015 |
| Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2 SK Knutson, NM Warholic, TJ Wigle, CR Klaus, CJ Allain, A Raimondi, ... Proceedings of the National Academy of Sciences 110 (19), 7922-7927, 2013 | 808 | 2013 |
| Coordinated activities of wild-type plus mutant EZH2 drive tumor-associated hypertrimethylation of lysine 27 on histone H3 (H3K27) in human B-cell lymphomas CJ Sneeringer, MP Scott, KW Kuntz, SK Knutson, RM Pollock, VM Richon, ... Proceedings of the National Academy of Sciences 107 (49), 20980-20985, 2010 | 775 | 2010 |
| Potent inhibition of DOT1L as treatment of MLL-fusion leukemia SR Daigle, EJ Olhava, CA Therkelsen, A Basavapathruni, L Jin, ... Blood, The Journal of the American Society of Hematology 122 (6), 1017-1025, 2013 | 731 | 2013 |
| The drug–target residence time model: a 10-year retrospective RA Copeland Nature Reviews Drug Discovery 15 (2), 87-95, 2016 | 643 | 2016 |
| Selective Inhibition of EZH2 by EPZ-6438 Leads to Potent Antitumor Activity in EZH2-Mutant Non-Hodgkin Lymphoma SK Knutson, S Kawano, Y Minoshima, NM Warholic, KC Huang, Y Xiao, ... Molecular cancer therapeutics 13 (4), 842-854, 2014 | 609 | 2014 |
| Residence time of receptor− ligand complexes and its effect on biological function PJ Tummino, RA Copeland Biochemistry 47 (20), 5481-5492, 2008 | 597 | 2008 |
| Cloning and characterization of ADAMTS11, an aggrecanase from the ADAMTS family I Abbaszade, RQ Liu, F Yang, SA Rosenfeld, OH Ross, JR Link, DM Ellis, ... Journal of Biological Chemistry 274 (33), 23443-23450, 1999 | 582 | 1999 |
| Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study A Italiano, JC Soria, M Toulmonde, JM Michot, C Lucchesi, A Varga, ... The Lancet Oncology 19 (5), 649-659, 2018 | 555 | 2018 |
| MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products JV Duncia, JB Santella III, CA Higley, WJ Pitts, J Wityak, WE Frietze, ... Bioorganic & medicinal chemistry letters 8 (20), 2839-2844, 1998 | 552 | 1998 |
| Mechanism of selective inhibition of the inducible isoform of prostaglandin G/H synthase. RA Copeland, JM Williams, J Giannaras, S Nurnberg, M Covington, ... Proceedings of the National Academy of Sciences 91 (23), 11202-11206, 1994 | 544 | 1994 |
| A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models E Chan-Penebre, KG Kuplast, CR Majer, PA Boriack-Sjodin, TJ Wigle, ... Nature chemical biology 11 (6), 432-437, 2015 | 536 | 2015 |
| Protein methyltransferases as a target class for drug discovery RA Copeland, ME Solomon, VM Richon Nature reviews Drug discovery 8 (9), 724-732, 2009 | 509 | 2009 |
