There have been many false dawns in small-molecule drug discovery, promising individual technologies and integrated platforms to improve the efficiency of drug discovery. Although high-throughput screening, combinatorial chemistry and computational methods have all led to the rapid expansion of novel hit molecules and target-focused libraries, conventional medicinal chemistry is still the most effective way to optimise those early hits into the development compounds that can become drugs. This lengthy optimisation process is increasingly being outsourced to various locations worldwide with lower overheads and reduced long-term liabilities, as there has been no other expedient alternative to driving down costs to improve the earnings of pharmaceutical companies in the short term. However, effective integration and intelligent automation of the next generation of flow chemistry and biology technologies now has the real potential to transform this iterative process by enabling a step change in the efficiency, as well as a radical shortening of the timescales required to discover a candidate compound ready for development. It is envisaged by the authors that new small molecule integrated technology platforms will become sufficiently disruptive to challenge the efficiency of the latest monoclonal antibody discovery platforms.