Fragments to LeadsTM

Fragment Based Drug Discovery uses of chemical fragments (that could be converted to novel chemical entities) in the presence of a protein target molecule and measures or detects binding by biophysical methods (X-ray, NMR, surface plasmon resonance) and biochemical assays (weakly active ~100mM). This is followed by structure-guided methods & medicinal chemistry to evolve the fragments in to real LEAD molecules.

Fragments To LeadsTM; offering from Sapient Discovery is a customized small molecule lead generation technology that incorporates elements of 3D structure of a protein target, virtual screening, small molecule fragment chemicals (molecular weight < 300D) and X-ray crystallography to identify leads. As part of Sapient Discovery's expert consulting services, Fragments to LeadsTM is routinely utilized to deliver custom leads to clients.


Bound fragment mM binding

Bound fragment 2 mM binding

Linked Fragments ~ μM to nM binding


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