Diversity screening versus focussed screening in drug discovery

Plate-Based Diversity Selection Based on Empirical HTS Data to Enhance the Number of Hits and Their Chemical Diversity

“…3 They assume even more significance when little or no prior knowledge about the target protein (such as active compounds modulating its activity and/or a solved 3D structure) disallows selection or design of focused screening libraries. In this article, we describe a molecular diversity-centric approach to select a small subset of the entire compound collection for screening.…”

High Throughput Screening Approach to Lead Discovery

“…It has been estimated that the total number of possible small organic molecules is between 10 40 and 10 100 [93]. Clearly, even if it was desirable, no organization would ever be able to cover this chemical space.…”

Functional expression of mammalian opioid receptors in insect cells and high-throughput screening platforms for receptor ligand mimetics

“…Pharmacological and molecular studies have demonstrated the existence of three opioid receptor subtypes, m, d and k stimulated the search for new drugs that can act as potent painkillers without causing dependence or addiction. Several approaches are used to achieve this goal, ranging from in silico modeling of putative ligands to the ligandbinding region of opioid receptors to the screening of libraries of chemical compounds or collections of natural products using available in vitro or cell-based highthroughput screening (HTS) systems [8,9]. Cultured insect cells occupy an important biotechnological niche, mainly by serving as hosts for baculovirus-vectorbased expression of recombinant proteins [10,11].…”