Early drug discovery can be accelerated with DEL screening
Early drug discovery is the initial stage of the preclinical drug development process where a biological target first needs to be identified and evaluated. Following this, compound collections or chemical libraries are screened to identify novel hit compounds. The early-stage drug discovery process should ideally, after lead optimization, result in preclinical candidates. Traditionally, identifying such molecules could take years of research and vast amounts of resources.
Vipergen’s DNA Encoded Libraries (DELs) accelerate this process by enabling the screening of millions of small molecules encoded with DNA barcodes. DEL screening accelerates hit identification, significantly reducing the time and cost associated with early-stage drug discovery. Unlike conventional high-throughput screening (HTS), which often demands large-scale resources, DEL screening is conducted in a single test tube or even directly in living cells. This breakthrough methodology enhances efficiency, minimizes resource consumption, and streamlines the discovery of promising drug candidates.
Advantages of DNA-Encoded Library Screening
DNA-Encoded Libraries (DELs) offer several key advantages over traditional screening methods:
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Ultra-high screening capacity – Screen millions to billions of compounds in a single experiment.
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Reduced resource consumption – Requires significantly fewer reagents and assay plates compared to HTS.
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Direct target engagement – Enables screening in physiologically relevant environments, including living cells.
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Rapid hit identification – Accelerates drug discovery timelines by generating high-quality leads faster.
Partner with Vipergen to get an early lead
Vipergen is a trusted partner for outsourced early-stage drug discovery. Our drug discovery services provide pharmaceutical and biotech companies with access to innovative screening technologies that accelerate research and improve efficiency. Here’s why you should partner with us:
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High-Quality DNA Encoded Libraries (DELs) – Our proprietary Yoctoreactor technology ensures a perfect match between DNA barcodes and displayed compounds, enabling highly reliable screening.
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Direct screening in cells – Our cBTE technology allows screening directly in living cells, eliminating the need for purified or immobilized target proteins.
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Optimize Resources – Partnering with Vipergen allows your team to focus on core research while we handle the complexities of screening and hit identification.
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Proven Expertise – Since 2005, Vipergen has specialized in DNA-encoded library synthesis and screening, providing unparalleled experience and expertise in early drug discovery.
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Accelerate Research Timelines – Our team facilitates the hit identification process, rapidly generating promising candidates for lead optimization. Our capabilities extend to challenging drug targets, ensuring comprehensive support for your discovery pipeline.
Lead Optimization in Drug Discovery
Following the identification of hit compounds through DEL screening, the next crucial step in drug discovery is lead optimization. This process refines hit molecules to improve their potency, selectivity, and pharmacokinetic properties, ultimately producing optimized candidates ready for preclinical development.
Vipergen’s DEL technology provides distinct advantages for lead optimization campaigns. Our libraries are strategically designed to deliver an initial structure-activity relationship (SAR), incorporating both analogs of core scaffolds and stereoisomers of key building blocks. This data-driven approach enables rapid exploration of chemical space around the identified hit compounds, expediting the development of high-quality lead candidates.
Additionally, our DEL screening facilitates the identification of anchor points for constructing complex molecules, such as bivalent therapeutics and PROTACs. This capability significantly expands the scope of drug discovery, supporting the development of next-generation therapeutics.
Drug Discovery for Startups: DEL Screening Without a Lab
Fit with limited laboratory space for the startup
Vipergen DEL Screening Workflow: From Target to Validated Hits
Figure 1: Approximate timeline for DEL screening in vitro (top) or in cells (bottom). All timeframes are approximate and scales with number of screening slots, and quantity of hit resynthesis.
Choosing a DEL Screening Partner: Checklist Questions
- Library Diversity & Novelty
Well-balanced libraries that mix privileged motifs, novel scaffolds, and Fsp3-rich fragments boost first-shot success. Check out Vipergens DELs here - Protein compatibility
Before starting a DEL screen, Vipergen scientists always conduct a feasibility study. - Data Transparency
Vipergen delivers a hit list and report. This includes metrics from screens and chemical structure information. - Follow-up Chemistry Capabilities
Vipergen can assist with hit resynthesis off-DNA - IP Ownership
Hits are reserved for clients for 1 year, where they may resynthesize and test in relevant assays. During this year, clients may nominate chemical series which become exclusive for the client. - Startup-Friendly Terms
Vipergen have developed a Snap platform, where we have made it easy, fast and affordable to get an early lead.
When traditional DEL screening isn’t the right choice
Utilizing in vitro DEL screening might be difficult with:
- Hard-to-express or purify protein, where aggregations, low yield or mis-folding make it difficult to obtain milligram quantities of pure protein.
- Membrane-embedded proteins, where detergent micelles or nanodiscs are required to keep the target folded. This can mask binding sites and add background DNA stickiness.
- Allosteric or conformationally dynamic targets where buffers and detergents disrupt conformation.
- Proteins where post-translational modifications are important for function.
- Lipid dependent targets, where detergents can mask binding sites.
In these cases, utilizing Vipergen’s cellular Binder Trap Enrichment is a good option for a better return on investment.
Successful Drug Discovery with Vipergen
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Rapid hit identification – Reducing discovery timelines from years to months.
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Novel target engagement – Enabling drug development for previously undruggable targets.
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Efficient lead optimization – Providing high-quality leads with optimized properties.
Our fully integrated platform screens hundreds of millions of DEL compounds either in vitro or directly in cells, delivering qualified hits in weeks instead of months. Screening DELs in cells allows for the rapid discovery of hits against difficult to express targets, membrane proteins and protein complexes.
Our current DELs contain around 500 million small molecules, which for us gives the perfect chemical space exploration. Furthermore, we have developed the YoctoReactor technology to ensure high-fidelity DELs, where truncates are eliminated. Read about how we synthesize DELs here
Following screening we deliver a report containing hit list, including metrics from screens and chemical structure information. Hits are then reserved for the client for one year, where clients may nominate chemical series, which becomes exclusive for the client.
Explore Vipergen’s Full Range of Drug Discovery Services
Vipergen offers a comprehensive suite of drug discovery services, from early hit identification to lead optimization. Explore our advanced screening technologies and innovative solutions designed to accelerate drug development.