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Hit profiling

 

The end of a screening campaign is the beginning of the next stage on the path to discover compounds worthy of lead optimization and ultimately clinical development. We employ orthogonal assays and selectivity testing as complementation to the primary screening campaign, to ensure the hits we report are selective and not artifacts. In cases where these aspects have not been dealt with in advance, and for subsequent profiling and qualification of hits, we offer a range of hit profiling services.

Exquiron will work towards addressing specificity, selectivity, potency, and mechanism of action (MOA) for primary hits, hits from SAR expansion, or for compounds that are already part of hit-to-lead or lead optimization efforts in the client’s drug discovery programs. Together we will identify suitable related targets or assay formats and optimize the chosen hit profiling assays, which may then be used to the test promising compounds emanating from lead optimization programs.

Dedicated assays may include selectivity panels with related targets, enzyme mechanistic assays, redox cycling assays, and others.

Hit profiling results will be analyzed with our software platform, and customized output allows seamless import into your data infrastructure.