Fragment-based lead design (FBLD), sometimes referred to as fragment-based drug discovery (FBDD), is an increasingly important strategy for the discovery of biologically active compounds.[1] FBLD generally uses libraries consisting of modest collections (100– 1000 compounds) of small molecular fragments (MW< 300 amu) that are screened against targets of interest.[2] Although such fragments do not bind as tightly (Kd values in the ...
