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FRAGMENT LIBRARIES

 


 

Crystal Structure of ROCK 1 kinase bound to fasudil / Structure of fasudil

The first example of fragment-based identification of an active molecule was described in 1996. The idea was to assay small molecules (molecular weight below 350) using NMR or X-ray techniques at high concentration against the protein of interest to identify active fragments. Two fragments showing affinity at different location of the site are then chemically connected to obtain a final molecule with high affinity to the receptor.

Since then, many examples have shown that fragment-based drug discovery is a powerful tool to help medicinal chemists attain optimisation of their molecules. However, no new active compound discovered only with this technique has currently reached the market (meaning connecting two fragments to obtain the lead compound). There is a need for second and third generation fragment compounds to master the hardest part of the technique - the connectivity between the fragments.

FRAGMENT LIBRARY 1
FRAGMENT LIBRARY 1

• original scaffolds
• excellent diversity
• highly soluble compounds
• high quality compounds

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