Objective

The availability of kinetic information of compounds in early phases of drug discovery is useful in driving the med chem strategy.The challenge in earlier phases of a drug discovery is that there are compounds from multiple series requiring the profiling of large numbers of compounds. In contrast, detailed mechanistic characterisation of compounds is usually very low throughput, often due to the limited capacity of automation. The FLIPR Tetra® System (Molecular Devices) enables liquid sample transfer and is equipped with a CCD based camera that simultaneously detects fluorescence from all wells. This system is well established for high throughput cellular assays. The present study aims to evaluate the FLIPR Tetra® to check its suitability for running high throughput Biochemical kinetic assays. A kinetic assay utilising a fluorescence peptide was optimised on the FLIPR Tetra®. Automation parameters including low volume plate definition, reagent transfer and mix steps were optimised to generate kinetic curves. Concentration response kinetic curves were generated successfully using FLIPR Tetra®. Assay quality was found comparable to the original assay. The simultaneous read function enabled collection of earlier time point data than traditional approaches. The study confirmed that FLIPR Tetra® has the capacity to deliver high quality Biochemical kinetic data. We predict greater than ten fold increase in our current assay throughput.