Experiences in fragment-based drug discovery

An inhibitor of Bcl-2 family proteins induces regression of solid tumours

Tilman Oltersdorf, Steven W. Elmore, Alexander R. Shoemaker et al. · Nature · 2005 · 3.4K citations

Medicine, Molecular Biology, Oncology +14

Discovering High-Affinity Ligands for Proteins: SAR by NMR

Suzanne B. Shuker, Philip J. Hajduk, Robert Meadows et al. · Science · 1996 · 2K citations

Pharmacy, Medicinal Chemistry, Pharmacology +14

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

Gideon Bollag, Peter Hirth, James Tsai et al. · Nature · 2010 · 1.8K citations

Medicine, Oncology, Pharmacology +14

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

James Tsai, John Tayu Lee, Weiru Wang et al. · Proceedings of the National Academy of Sciences · 2008 · 1.3K citations · Full text

Medicine, Oncology, Pharmacology +15

Entropic Contributions to Rate Accelerations in Enzymic and Intramolecular Reactions and the Chelate Effect

Michael I. Page, William P. Jencks · Proceedings of the National Academy of Sciences · 1971 · 1K citations · Full text

Natural Sciences, Biochemistry, Chemistry +11