Back to the Future: Reimagining automation as a precision tool for drug discovery

About 50 kinase inhibitors have been approved by the FDA for different indications to date. The journey from target validation to approval is fraught with challenges with irreproducibility and error accumulation contributing to spiraling costs and a lack of efficacy continuing to drive excessive attrition rates.  The identification and characterisation of novel inhibitors is a challenging, yet absolutely critical task which sets the tone for future successes and failures.  Accurate hit identification followed by high resolution, kinetic molecular profiling enhances outcomes ensuring better data-driven decision making early on in the drug discovery process, not only saving time and resources, but also leading to superior molecular design.

Arctoris has developed a robotics-enabled process for fully automated inhibitor profiling, providing an unparalleled depth of data capture, going beyond the current state-of-the-art of biochemical assay setup. Validated against a number of kinases, our technology platform can deliver fully validated assays within days and profiling activities within hours. Reagent characterisation, assay development, calibration, and optimization are expedited through systematic multifactorial experimental design, facilitated using high density plate formats and versatile automated liquid handling solutions. Arctoris’ Ulysses platform affords 9 orders of magnitude range in liquid volume handling, with picolitre precision and contact-free digital dispensing for true, non-serial, independent experimentation enabling experiments to be designed exclusively for each molecule. Fully automated protocols can be optimized, validated, versioned, and explicitly encoded within hours.  We will showcase the application of the Ulysses platform

Data highlighting novel advances in hit marking and high resolution reconfirmation activities, combined with cutting edge machine learning, enabling the rapid development of lead molecules, will be shown.