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Hit-to-lead
We conduct hit-to-lead projects in an efficient cycle of rational design, synthesis and biological evaluation. Typically two to four hit series are evaluated in parallel, with a view to establishing the scope for further optimization. One or two series are then selected for progression into lead optimization studies.
The process involves:
- Design and synthesis of new analogues to quickly determine structure-activity relationships (SAR)
- Increasing compound potency and selectivity
- Improvement of drug-like properties
- Using computational chemistry to generate binding hypotheses and to investigate SAR
- Early assessment of ADME properties
- Ranking of hits or hit series to select the most promising for lead optimisation
We work closely with you to define the compound profile required, prioritizing compounds for detailed evaluation and interpreting results from high throughput screening and ADME/PK assessment. Our medicinal chemists have a track record of delivering high quality lead series within tight timelines in a broad range of target classes and therapeutic areas.
If you’d like to know more about our services, discuss custom assays, specific research, or get a quote, please contact us.
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