Direct-to-Biology (D2B)
Accelerate the Design-Synthesis-Test-Analysis Cycle
The Direct-to-Biology (D2B) platform integrates medicinal chemistry, miniaturized chemical synthesis, high-throughput biological screening and computer-aided drug design into a continuous workflow. With D2B capability, the design-synthesis-test-analysis cycle can be compressed from months to 2-3 weeks.
D2B is particularly powerful in hit expansion and hit-to-lead stages. In the early stages, teams often need to assess hundreds to thousands of compounds, and D2B provides a more cost-effective way to accelerate these projects. WuXi Biology and Testing’s D2B platform is now systematically developing more compatible reactions and building block libraries to support broader discovery needs.
An Integrated High-Throughput Workflow
Typical Timeline Per D2B Cycle
Integrated Design-Synthesis-Test-Analysis Cycle
Each cycle begins with library design informed by medicinal chemistry, computer-aided drug design, and the available biological data. Thousands of new compounds are synthesized, quality checked, and transferred directly into fit-for-purpose biological assays. Results are then evaluated through structure-activity relationship analysis to guide the next design cycle.
This coordinated workflow reduces handoffs between disciplines and helps your team prioritize compounds using timely, comparable data in 2-3 weeks.
High-Throughput Synthesis and Assays
Automated synthesis and quality control in 384-well plates support rapid generation of D2B compound libraries at the nanomole scale. The resulting compounds can be evaluated using multiple high-throughput biological assays in 384- or 1536-well formats, depending on the target, readout, and program objective.
Additional measurements, such as high-throughput ADMET, can be incorporated to provide context beyond biological potency and help identify compounds that merit re-synthesis and confirmatory testing.
Applications Across Emerging Modalities
The direct-to-biology approach supports rapid exploration of structure-activity relationships not only for small molecules but also for new modalities, including proximity inducers, peptides and complex conjugates, allowing teams to compare focused design ideas and advance promising chemical matter more efficiently.
Explore Solutions for Your Program
Explore solutions by development phase, drug modality, therapeutic area, or integrated discovery needs.
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Frequently Asked Questions
Direct-to-Biology (D2B) is an integrated discovery approach that connects compound design, high-throughput synthesis, biological assays and multiplex data analysis. By accelerating Design-Synthesis-Test-Analysis cycle from months to just 2-3 weeks, D2B aims to not only speeds up decision-making but also generates large-scale, cost-effective wet-lab data, positioning D2B as a powerful AI-enabling platform that provides the robust, high-throughput datasets needed to train and validate machine learning models..
In the D2B model, chemical reactions are transferred into 384-well or 1536-well microplates. Each well acts as an independent miniaturized reaction unit, allowing a large number of chemical syntheses to run in parallel under very small volumes. Once synthesis is completed, molecules can move directly into subsequent screening without going through traditional separation and purification steps, thereby accelerating the continuous design-synthesis-test-analysis cycle.
The broader advantage of D2B is that it fundamentally changes the pace of drug discovery. Its biggest difference compared to traditional workflow is compressing the design-make-test-analysis cycle from months to just 2-3 weeks. This can support faster hit triage, rapid exploration of structure-activity relationships, and earlier go/no-go decisions.
An assay is well suited for D2B if it can be successfully miniaturized and integrated into a high-throughput, automated workflow. The key is that the assay must be robust enough to tolerate or specifically detect the target molecule in the presence of residual reaction impurities. In our experience, a wide breadth of assays work very well. This includes cell-based and biochemical assays—particularly those measuring protein-protein interactions and cellular activity—as well as ADMET assays, which allow for the early, integrated evaluation of molecular properties.
We are systematically expanding the applications and modalities for D2B, particularly in complex cell models such as iPSC-derived cells and organoids. Crucially, as the industry shifts towards Non-Animal Models (NAMs), D2B will seamlessly integrate with these advanced biological systems, becoming the standard approach for exploring undruggable targets in highly physiologically relevant environments.