A successful fragment-based lead discovery (FBLD) campaign largely depends on the content of the fragment collection being screened. To design a successful fragment collection, several factors must be considered, including collection size, property filters, hit follow-up considerations, and screening methods. In this chapter, we will discuss each factor and how it was applied to the design and assembly of one or more fragment collections in a major pharmaceutical company setting. We will also present examples and statistics of screening results from such collections and how subsequent collections can be improved. Lastly, we will provide a summary comparison of selected fragment collections from literature.
CITATION STYLE
Na, J., & Hu, Q. (2011). Design of Screening Collections for Successful Fragment-Based Lead Discovery. In Methods in Molecular Biology (Vol. 685, pp. 219–240). Humana Press Inc. https://doi.org/10.1007/978-1-60761-931-4_11
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