There are over 300 human viruses that have no treatment, vaccine or antiviral. Unfortunately, only sixty-two drugs are approved by the US Food and Drug Administration (FDA) for the treatment of six different viral illnesses. Of these, 45% are for the treatment of HIV/AIDS. The remaining drugs offer treatments that target hepatitis B and C, herpes, influenza, and respiratory syncytial viruses. Antiviral drugs can play a significant role in the containment of an outbreak of an emerging virus. Vaccination of individuals during an outbreak can also prove effective; however, protection of an individual from the threat may not occur for two or more weeks after the initial vaccination. Hence, only a drug can be offered as a prophylactic treatment of individuals in an endemic area.

Industrial scale technologies developed and applied within the pharmaceutical industry for the purpose of drug discovery have recently been adopted by many research laboratories for the purpose of facilitating chemical genomics. Taking full advantage of these technologies will require education in high-throughput screening assay systems as well as new methods that exploit the capabilities of existing technologies.

Over the past few decades we have experienced a dramatic increase in the rate of emergence and re-emergence of infectious diseases. Many of these diseases, such as SARS, resulted in fewer than 1,000 deaths, but caused an estimated 2 per cent decline gross domestic product in East Asia. The economic impact of a pandemic influenza outbreak could result in the loss of millions of lives and cost an estimated 900 billion (US).

Historically (until the late 1980s), compounds discovered by phenotypical in vivo screens were at least characterised with implicit ADMET data. An attractive compound in these test systems was available at the (usually unknown) target; had a minimal toxicological profile (the animal did not die immediately) and gave phenotypical (High-Content) information in the animal used for the experiment.

The impact of screening and technology applications on drug discovery is the theme for this year’s SBS conference, hosted in Seattle. Supported by more than ten years of HTS and combinatorial chemistry strategies, the Society for Biomolecular Sciences believe that the time has come to consolidate, understand and critique the impact these technologies have had on providing hits, leads and utlimately, better drug candidates that will help the lives of millions of people across the world.

Drug (lead) discovery relies on massive screening of chemical libraries against various extra- and intracellular molecular targets to find compounds with the desired mode of action. Sequencing of the human genome1 has generated a large number (>40 per cent) of new molecular targets with unknown function (‘orphan targets’), as well as a large number of molecular targets with known function albeit non-tractable by standard high-throughput screening (HTS) due to the particular requirements of plate-based assays in robotic screening systems (‘non-tractable targets’). Examples of the latter are targets with very fast kinetics, targets with multiple modes of function for the same polypeptide chain or targets where the substrate of a particular enzyme is not known.

There has been a sea change in the way many biotech and pharma companies view the search for new drugs in neglected disease. Serono is a biotech company, with interests in neurology, reproductive health, oncology and dermatology – but we teamed up with the World Health Organization (WHO) to train two visitors in finding new medicines. From this simple example, we have learned much that shows that beyond simple corporate social responsibility we have much to benefit from with such collaborations.

Ultra high-throughput screening (UHTS) offers the possibility to discover novel pharmacophores. To benefit from UHTS special demands concerning assay quality and data analysis have to be met.

The pharmaceutical industry continues to face an ever-changing, increasingly competitive business environment. This makes it imperative for drug discovery and development efforts to incorporate new technologies in order to reduce time-to-market to survive in today’s competitive marketplace. This industry pressure to shorten the R&D process has seen high-throughput screening (HTS) technologies becoming a critical part of the drug discovery process.

In pharmaceutical drug discovery research, several technological advances have moved in vitro biological and biochemical experiments from the laboratory benchtop to fully automated high-throughput screening (HTS) robotic platforms.