Early Stage: Hit-to-Lead

The initial step in bringing a target compound to market involves identifying small molecule hits using various paradigm. These hits are then further developed and optimized to identify promising lead compounds.

Services we provide include:

• Analysis of high throughput screening (HTS) or virtual screening/assay results, including preliminary structure-activity relationship (SAR) evaluation, physical-chemical properties, identifying hit clusters, etc.
• Risk assessment, including structural liabilities and PAINS analysis
• Triage of hits generated through AI tools, and recommend targets for synthesis
• Hit confirmation: resynthesis/purification for confirming the structure and activity of hits
• Hit expansion by synthesis of selected analogs to evaluate scaffolds and explore basic SAR
• Preliminary assessment of ADME profile
• Select lead series (3-5 series) based on SAR and ADME results

FAQ

• What is Hit-to-Lead?

  Hit-to-Lead is the process of evaluating initial promising chemical series (hits) identified through screening, and converting them into drug-like candidates (leads).

• What services do you offer for Hit-to-Lead?

  We offer compound design, synthesis, in vitro assays, and initial ADME assays to scope out basic structure activity relationship (SAR), improving potency, selectivity, and properties of your series. This will enable decision on which series to take into lead optimization.

• What are the typical timelines for Hit-to-Lead projects?

  Hit-to-Lead timelines can vary depending on the complexity of the project, but typically range from 3-6 months.

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