Sébastien L. Degorce

Discovery of 5-{4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl}-<i>N</i>-methylpyridine-2-carboxamide (AZD5305): A PARP1–DNA Trapper with High Selectivity for PARP1 over PARP2 and Other PARPs

Jeffrey W. Johannes, Amber Balazs, Derek Barratt et al. · Journal of Medicinal Chemistry · 2021 · 129 citations · Full text

The Identification of Potent, Selective, and Orally Available Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase: The Discovery of AZD0156 (8-{6-[3-(Dimethylamino)propoxy]pyridin-3-yl}-3-methyl-1-(tetrahydro-2<i>H</i>-pyran-4-yl)-1,3-dihydro-2<i>H</i>-imidazo[4,5-<i>c</i>]quinolin-2-one)

Kurt G. Pike, Bernard Barlaam, Elaine Cadogan et al. · Journal of Medicinal Chemistry · 2018 · 111 citations · Full text

Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3

Scott Boyd, Joanna Brookfield, Susan E. Critchlow et al. · Journal of Medicinal Chemistry · 2015 · 92 citations · Full text

Drug Target, Selective Inhibitors, Chemical Biology +18

Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines

Sébastien L. Degorce, Michael S. Bodnarchuk, Iain Cumming et al. · Journal of Medicinal Chemistry · 2018 · 86 citations · Full text

Discovery of (<i>R</i>)-8-(1-(3,5-Difluorophenylamino)ethyl)-<i>N</i>,<i>N</i>-dimethyl-2-morpholino-4-oxo-4<i>H</i>-chromene-6-carboxamide (AZD8186): A Potent and Selective Inhibitor of PI3Kβ and PI3Kδ for the Treatment of PTEN-Deficient Cancers

Bernard Barlaam, Sabina Cosulich, Sébastien L. Degorce et al. · Journal of Medicinal Chemistry · 2014 · 85 citations · Full text

Pten Deficient Tumors, Pharmacotherapy, Pharmaceutical Chemistry +20