Medicinal chemistry

The California Institute for Regenerative Medicines Human iPSC Initiative By Dr Thomas J. Novak This article discusses large-scale generation of patient-derived induced pluripotent stem cells (iPSCs) to accelerate the understanding of disease biology and drug discovery. In 2012, the California Institute for Regenerative Medicine (CIRM) announced its Human iPSC Initiative, an ambitious effort to generate […]

When Two Are Not Enough: Lead Optimisation Beyond Matched Pairs By Dr Noel M. O’Boyle, Dr Roger A. Sayle and Dr Matt Segall Lead optimisation projects progress by making successive enhancements to one or more starting structures. This is a classic multi-objective optimisation procedure where the goal is not only to improve potency but also […]

Managing Data Challenges In The New R&D Environment By Dr Paul Denny-Gouldson The discovery and development of drugs is changing. The realm once dominated by ‘big pharma’ is becoming increasingly fragmented into more agile and flexible consortia. The dramatic change of focus on drug type from small molecule to large molecule, and even large-small molecule […]

Share Share Tweet Email The Development of Cell-Based Assays For Pain Drug Discovery The Development of Cell-Based Assays For Pain Drug Discovery By Dr Paul Karila and Dr Charlotta Blom Since the completion of the Human Genome Project and the beginning of the so-called genomics era in the 1990s, a molecular target-based approach has been […]

BioPharma and CROs Collaborating In Early Drug Discovery By Dr John Montana and Cornelis E.C.A. Hop BioPharma and CROs are riding the latest wave – discovery research – together with a vigour and gusto that might have seemed implausible five years ago. How these collaborations are structured, and how well they function, can vary widely, […]

Opportunities For Phenotypic Screening In Drug Discovery By David C. Swinney Renewed awareness of the value of phenotypic screening to drug discovery creates many new opportunities to increase drug discovery success and productivity. These opportunities include identification of translational phenotypic biomarkers, development of new assays that translate to human disease and refinement of paradigms to […]

Reconfiguring Drug Discovery Through Innovative Partnerships By Dr Robert Grundy, Iain James, Chas Bountra and Timothy Harrison Attrition rates in drug discovery and development remain stubbornly high, despite large investments by the pharmaceutical industry. The cost of developing a new drug has been estimated at between $1.3 billion and upwards of $4 billion, if one […]

Targeted Chemical Libraries: The keys to unlock the ubiquitin system By Dr Jason Brown and Dr J. Mark Treherne Is novel chemistry the final frontier for ubiquitin system drug discovery?     Although the widespread use of target-focused libraries has led to the rapid expansion of novel chemistry as research tools in drug discovery to […]

Library Logistics: Managing Comprehensive Compound Collections By Dr Jorg Kroll and David Booth Compound management may seem straightforward but in reality, as the number of new compounds increases dramatically year-on-year, the management of large collections has become increasingly challenging. As highthroughput technologies have become the norm, Bayer HealthCare, a global healthcare company, has seen its […]

Rules For Drug Discovery: Can simple property criteria help you to find a drug? By Dr Matthew Segall The years since the publication of Lipinski’s Rule of Five (Ro5) (1) in 1997 have seen the growth of a minor industry, dedicated to generating new ‘rules’ for drug discovery. Fuelled by what Kenny and Montanari have […]