Exhibitor Tutorial
Daniel Thomas, PhD
Dr
GSK
Maureen Beresini
Genentech
1. Facilitating a multidimensional approach to delivering binding kinetics in drug discovery
Recent advances in cutting-edge liquid handling and plate reader technologies have enabled the acquisition of mechanistic data at a scale and quality not previously possible. Consequently, this has made the development, prosecution and deconvolution of higher throughput screens for real time kinetic characterisation a reality, ensuring an exciting future for early drug discovery.
Examples of the impact these newly developed technologies are delivering at different points across early drug discovery from hit validation to candidate selection will be presented. These case studies will focus on data from complementary biochemical and cellular systems, generated using a variety of well-established technologies and emerging next wave methods. Opportunities to profoundly impact drug discovery through the value of decision-making combined with an ability to effectively reduce attrition at each stage will be critical in defining future successes as an industry. Improving our understanding of both on and off-target kinetics that underpin potency will be an important component in achieving this goal
2. Accelerating Biochemical Assay Development through Flexible, Easy-to-Use Automation
Assay development is a crucial, early activity for initiating drug discovery projects. Robust and relevant assays must be put in place as rapidly as possible for identifying new chemical matter and assessing potential tool compounds as well as for establishing structure-activity relationships to drive compound progression. Assay development can be a complex, iterative, and time-consuming process. Statistical design of experiments (DoE) is one approach to streamlining the process by promoting the evaluation of multiple assay factors simultaneously, and the use of automation greatly facilitates its application. Additionally, DoE may be combined with more traditional assay development strategies to advance assays efficiently. This workshop will highlight some elements in the application of the dragonfly® discovery to the execution of DoE. Additionally, it will describe the broader application of this liquid handling platform in assay development. The dragonfly® designer software fosters the use of automation across various stages of assay development because of its easy-to-use interface with flexible design features.