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Fragment-based drug discovery (FBDD) is one
of the most popular processes for finding lead
compounds. It's even more widely used today
by pharma companies than high-throughput
screening (HTS). Although HTS has overall been
a success — judging by the number of drugs
discovered with this approach and taken to
market — the requirement for large investment
in R&D has limited its application to the large
pharma companies.
With a rise in the number of explorative targets, there
is a need not necessarily for bigger libraries, but
rather for ones that contain more diverse molecules,
especially from new chemical spaces. In turn, this
requires affinity-based screening technologies to be
more flexible in order to characterize binding events
of more heterogeneous targets and ligands.
Strengths of
fragment-based
drug discovery
A number of technical concerns and limitations
have put into question the success and
efficiency of HTS. Though it has uncovered many
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More hits and broader
chemical space coverage
