Michael A. Galella

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

Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy

Andrew K. Dilger, Kumar B. Pabbisetty, James R. Corte et al. · Journal of Medicinal Chemistry · 2021 · 97 citations · Full text

Medicine, Medicinal Chemistry, Pharmacology +15

Discovery of Potent and Muscle Selective Androgen Receptor Modulators through Scaffold Modifications

James J. Li, James Sutton, Alexandra A. Nirschl et al. · Journal of Medicinal Chemistry · 2007 · 56 citations · Full text

Life Sciences, Medicinal Chemistry, Pharmacology +17

Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists

James J.‐W. Duan, Zhonghui Lu, Bin Jiang et al. · ACS Medicinal Chemistry Letters · 2019 · 54 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +17