Elizabeth Heimrich

Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165

Stephen T. Wrobleski, Ryan Moslin, Shuqun Lin et al. · Journal of Medicinal Chemistry · 2019 · 369 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +15

Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain

James R. Burke, Lihong Cheng, Kathleen M. Gillooly et al. · Science Translational Medicine · 2019 · 282 citations

Life Sciences, Immunology, Pharmacology +14

Discovery of 6-Fluoro-5-(<i>R</i>)-(3-(<i>S</i>)-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4<i>H</i>)-yl)-2-methylphenyl)-2-(<i>S</i>)-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1<i>H</i>-carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers

Scott H. Watterson, George V. De Lucca, Qing Shi et al. · Journal of Medicinal Chemistry · 2016 · 146 citations · Full text

Life Sciences, Medicinal Chemistry, Pharmacology +17

Discovery of Branebrutinib (BMS-986195): A Strategy for Identifying a Highly Potent and Selective Covalent Inhibitor Providing Rapid in Vivo Inactivation of Bruton’s Tyrosine Kinase (BTK)

Scott H. Watterson, Qingjie Liu, Myra Beaudoin Bertrand et al. · Journal of Medicinal Chemistry · 2019 · 113 citations · Full text

Life Sciences, Medicinal Chemistry, Pharmacology +15

Identification of <i>N</i>-Methyl Nicotinamide and <i>N</i>-Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2)

Ryan Moslin, Yanlei Zhang, Stephen T. Wrobleski et al. · Journal of Medicinal Chemistry · 2019 · 92 citations · Full text

Life Sciences, Medicinal Chemistry, Pharmacology +17