High Throughput Screening Approach to Lead Discovery

New Modalities, Technologies, and Partnerships in Probe and Lead Generation: Enabling a Mode-of-Action Centric Paradigm

“…High throughput screening remains a very valid and robust strategy to identify suitable starting points for drug discovery . Increasing diversity and quality of small molecules in screening collections is however required to offer the best target space coverage and the best lead-like compounds. ,,, Historically, the enhancement of screening collections has been performed through compound acquisition from chemical suppliers and brokers. , However, this model requires a large budget to cover a sufficiently large and diverse number of compounds . Another model exploited by several major pharmaceutical companies has been to outsource the synthesis of small molecule libraries designed by chemists of the ordering company.…”

Novel 1,2-dihydroquinazolin-2-ones: Design, synthesis, and biological evaluation against Trypanosoma brucei

“…16-18 A new synthetic batch of 1 was prepared and showed an approximately 2-fold reduction in potency (EC 50 = 1.89 μM) in our T. brucei cell proliferation assay compared to the initial GSK assay result (EC 50 = 0.84 μM). 6 This minor shift may be attributed to a number of factors, including minor differences in the biological assay protocols, as well as differences in sample purity between the new batch of 1 compared to the original GSK sample collection batch.…”

Genomics, Other “Omic” Technologies, Personalized Medicine, and Additional Biotechnology-Related Techniques

“…High-throughput screening (HTS) provides for the bioassay of thousands of compounds in multiple assays at the same time (Cik and Jurzak 2007 ;Rankovic et al 2010 ). The process is automated with robots and utilizes multi-well microtiter plates.…”

“…Chemical genomics is an emerging "omic" technology not discussed above. The development of highthroughput screening and high-throughput chemistry coupled with "omic" technologies has changed the drug discovery paradigm and the approach for the investigation of target pharmacology (Kubinyi and Müller 2004 ;Kubinyi 2007 ;Flaumenhaft 2007 ;Rankovic et al 2010 ) (see Fig. 8.11 ).…”