Lead optimisation

The Information Symphony: Data orchestration for a changing industry managing data on a platform for innovation. By Chris Molloy A leading ballet conductor (1) recently told me of courses which he runs for senior business leaders. He allows them to conduct an orchestra: first, very strictly, with close direction applied to each instrument; he then […]

Simultaneous Visualisation of Attrition and Timelines: Funnel Diagrams. By Dr Linda Hirons, Dr Craig Johnstone and Colin Sambrook-Smith In drug discovery both attrition and timelines are important factors to consider when applying process improvement to lead optimisation. In our attempts to improve the visualisation of both of these factors simultaneously, we developed funnel diagrams, which […]

Small Scale Benchtop Automation: Broadening the adoption of lab automation By Dr John Comley Driven by the need to enable technically challenging or repetitive processes, many labs in drug discovery that were not previously adopters of laboratory automation are being increasingly drawn to the potential of simple small-scale benchtop automation.     The immediately obvious […]

Exploring the horizons of small molecule drug discovery the evolution and application of the ideal fragment library By Dr David Myszka and Dr Jane Paul With the pharmaceutical industry facing unprecedented challenges in small molecule drug discovery, this paper argues that, with the correct design of the fragment library, Fragment-Based Drug Discovery has emerged as […]

A roadmap for achieving self-sustainability of academic high throughput screening core facilities By Dr Peter R. McDonald, Dr Anuradha Roy and Dr Rathnam Chaguturu Many academic HTS centres, faced with the high costs of drug discovery and decreasing federal funding, are struggling to survive. Just as with any small business, a sound business plan is […]

By Dr Aaron Heifetz The promise of stem cell technology as a tool for drug discovery, drug development and as a therapeutic modality is no longer in the future but part of contemporary healthcare. The speed which stem cells have been integrated into biomedical product development has surprised many, but stem cells in the form […]

Combining chemists expertise and a computer’s advanced capabilities to generate good ideas. By Dr Matthew Segall, Edmund Champness, Dr Chris Leeding, Dr Ryan Lilien, Dr Ramgopal Mettu and Dr Brian Stevens Drug One of the defining challenges of drug discovery is the need to make complex decisions regarding the design and selection of potential drug […]

8 Years of Surveying Ion Channel Screening – Has anything changed? By Dr John Comley No review of ion channel screening over the past decade can avoid discussing the pivotal role played by automated electrophysiology. Arguably this technology, more than any other, has opened up the field to wider investigation, made ion channels more accessible […]

In Vivo Preclinical Imaging – An Essential Tool in Translational Research By Dr John Comley In vivo imaging of small animals (mainly mice) is increasingly being deployed across the drug development process, particularly in the oncology/cancer therapeutic area. One of the main applications is monitoring the treatment response for early indications of efficacy. The most […]

Next Generation Flow Chemistry and Biology Platforms: The Impact on Small Molecule Drug Discovery By Dr J Mark Treherne, Dr David M Parry and Christopher N Selway Can the next generation of flow chemistry and biology platforms be fully integrated to transform the efficiency of small-molecule drug discovery for pharmaceutical industry? There have been many […]

Epigenetics: An Emerging Target Class for Drug Screening By Dr John Comley Heightened awareness of the potential importance of epigenetic targets in many disease areas, and growing vendor interest in developing new assays to screen DNA methylation and histone modifications encouraged HTStec to undertake market research in this area in June 2010. The study concluded […]

Moving Forward With Label-Free Technology By Dr Jennifer Hartigan, Cindy Liu and William Downey Label-free technology is gaining acceptance and opening doors for new drug discovery. Relatively new in the well-established world of high throughput screening (HTS), label-free technology provides opportunities for probing biomolecular interactions without spatial-interference, auto-fluorescent or quenching effects of labels. Endogenous targets […]

Current Trends in Label-Free Drug Discovery Technologies By Philip Rawlins Drug Discovery Label-free technologies have been used throughout drug discovery for the detection and characterisation of molecular interactions. The implementation of automated systems, increased sensitivity and the development of new technologies have recently broadened the use of label-free methods from primary screening through to mechanism-of-action […]

Bulk Reagent Dispensers: Ubiquitous liquid handling tool for microplate filling By Dr John Comley The initial success of the bulk reagent dispenser (BRD) as an automated liquidhandling product can be attributed to its simplicity and low cost. Its current role as an essential dispensing tool in those labs requiring microplate filling and assay assembly has […]

Overcoming Bottlenecks in Drug Discovery By Dr Trevor Perrior Developing a new drug is an expensive and time-consuming process. The best current estimate puts the cost of developing a single new drug at close to $1 billion. After a drug candidate has entered the clinical trial process it takes, on average, 5.1 years for it […]

High Throughput Flow Cytometry for Discovery at UNMCMD and the NIH Molecular Libraries Initiative By Dr Larry A. Sklar and Dr Bruce S. Edwards Commercial flow cytometers became widely established in research and clinical laboratories in the 1980s. Once the domain of immunologists and hematologists for cell sorting and analysis, the need for sample handling […]