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Discovery Platforms

Fragment-Based Drug Discovery (FBDD)

Fragment Based Drug Discovery (FBDD) has been established as an efficient tool in search of more accessible drug-like chemical space. Our FBDD group has developed a unique and well-designed fragment library with superb structural novelty and diversity based on our building block collections. Accompanied by our state-of-the-art screening platform equipped with various cutting-edge biophysical and biochemical screening technologies, our FBDD platform is capable of efficiently discovering novel fragment hits with optimum physicochemical properties. Continuous hit and lead generation from fragment hits are usually carried out by rational design based on structure information from our structural biology team. The FBDD service at PharmaBlock is committed to providing effective and high-quality drug discovery solutions to clients.

Screening Process

• Library Design: Assay Development and Optimization

• Fragment Screening: Primary Fragment Screening

• Primary Hit Validation: Dose Response Primary Hit Confirmation

• Orthogonal Hit Validation

• Structural Biology

• Hit and Lead Generation

Screening of Fragment Libraries

• Ligand-detected NMR

• SPR, BLI (Octet)

• X-ray crystallographic

• Thermal shift

• Biochemical assays

Physicochemical Properties of Fragments

• The molecular weight is ≤300 Da;

• Number of hydrogen-bond donors ≤3;

• Number of hydrogen-bond acceptors ≤3;

• The LogP is ≤3.

• Number of rotatable bonds (NROT) ≤3

Fragment Library at PharmaBlock

> 6000 fragments and growing daily