Dirk A. Heerding

Discovery of 7-Methyl-5-(1-{[3-(trifluoromethyl)phenyl]acetyl}-2,3-dihydro-1<i>H</i>-indol-5-yl)-7<i>H</i>-pyrrolo[2,3-<i>d</i>]pyrimidin-4-amine (GSK2606414), a Potent and Selective First-in-Class Inhibitor of Protein Kinase R (PKR)-like Endoplasmic Reticulum Kinase (PERK)

Jeffrey M. Axten, Jesús R. Medina, Yanhong Feng et al. · Journal of Medicinal Chemistry · 2012 · 619 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +13

Characterization of an Akt Kinase Inhibitor with Potent Pharmacodynamic and Antitumor Activity

Nelson Rhodes, Dirk A. Heerding, Derek R. Duckett et al. · Cancer Research · 2008 · 298 citations · Full text

Medicine, Oncology, Pharmacology +17

Discovery of a first-in-class reversible DNMT1-selective inhibitor with improved tolerability and efficacy in acute myeloid leukemia

Melissa B. Pappalardi, Kathryn Keenan, Mark Cockerill et al. · Nature Cancer · 2021 · 280 citations · Full text

Medicine, Oncology, Pharmacology +8

Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development

Jeffrey M. Axten, Stuart P. Romeril, Arthur Y. L. Shu et al. · ACS Medicinal Chemistry Letters · 2013 · 230 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +16

Allosteric Wip1 phosphatase inhibition through flap-subdomain interaction

Aidan G. Gilmartin, Thomas Faitg, Mark C. Richter et al. · Nature Chemical Biology · 2014 · 208 citations

Life Sciences, Biochemistry, Molecular Biology +14