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Consortium makes fragment
screening more accessible
The European Lead Factory (ELF) makes
compound and fragment screening
more accessible to small companies
and academia. An Innovative Medicines
Initiative (IMI)-funded project, the ELF
established a Joint European Compound
Library (JECL). It combines 300,000
compounds from participating pharma
companies (largely proprietary) with an
additional 200,000 compounds that ELF
synthesized based on contributed design
ideas from around Europe.
One of the reasons fragment-based screening has become so popular is because
it's easier to work with a few thousand compounds rather than a few million
when dealing with HTS libraries. Investments in instrumentation and reagents are
greatly reduced, as is the number of highly-skilled workers required to carry out
the campaigns. All of this makes FBDD a far less expensive enterprise than HTS,
opening up compound discovery to small companies and even academia.
The cost of maintenance is a key issue that is sometimes overlooked in
comparing HTS with FBDD. Library compounds must be checked regularly to
test their stability. Aqueous solubility must also be insured, as concentrations
in excess of 500 µM can be required on primary screens and even higher on
secondary screens. Aggregators are an unfortunate artifact of combinatorial
Why is fragment-
based screening
so popular?
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