Fragment Based Drug Design (FBDD): a fragment hit to drug candidate case study

Interferonopathies are a class of auto-immune diseases caused by up-regulation of interferon signalling and activation of interferon stimulated genes (ISG). Common examples include Systemic Lupus Eruthematosus (SLE), Sjögren’s Syndrome & Scleroderma.

The kinases IKKe/TBK1 are promising targets for novel interferonopathy drugs.

Trevor Perrior explains how Domainex employed a Fragment Based Drug Design (FBDD) approach, using the technology platform FragmentBuilder, to develop an interferonopathy drug candidate.

Watch this webinar to hear Trevor explain each step of the project, including:

• Fragment screening to identify a very efficient and selective motif for IKKe & TBK1.
• Structural based drug design (SBDD) to elaborate hits to give potent inhibitors with high selectivity with the known chemical class of aminopyrimidines
• PK profiling by further optimisation of physicochemical properties

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