Les A. Dakin

Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR)

Richard A. Ward, Mark J. Anderton, Susan Ashton et al. · Journal of Medicinal Chemistry · 2013 · 257 citations · Full text

Covalent Inhibitors, Drug Target, Thiol Reactivity +19

AZD1208, a potent and selective pan-Pim kinase inhibitor, demonstrates efficacy in preclinical models of acute myeloid leukemia

Erika Krasnickas Keeton, Kristen McEachern, Keith Dillman et al. · Blood · 2013 · 240 citations

Identification of (<i>R</i>)-<i>N</i>-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1<i>H</i>-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas

Rishi G. Vaswani, Victor Gehling, Les A. Dakin et al. · Journal of Medicinal Chemistry · 2016 · 214 citations · Full text

EZH2 Inhibitor Efficacy in Non-Hodgkin’s Lymphoma Does Not Require Suppression of H3K27 Monomethylation

William D. Bradley, Shilpi Arora, Jennifer Busby et al. · Chemistry & Biology · 2014 · 148 citations

Hematological Malignancy, Lymphoid Neoplasia, Medicine +10

Diving into the Water: Inducible Binding Conformations for BRD4, TAF1(2), BRD9, and CECR2 Bromodomains

Terry D. Crawford, Vickie Tsui, E. Megan Flynn et al. · Journal of Medicinal Chemistry · 2016 · 117 citations · Full text

Molecular Biology, Chemical Biology, Pharmaceutical Chemistry +17