High Throughput Screening

What Is High Throughput Screening?

High throughput screening (HTS) is the testing of large numbers (from several hundred thousand up to a few million) of diverse small molecules, predominantly of molecular weight 400-650 Da. It has been a mainstay of hit identification for drug discovery since the early 1990s. Since then, there have been many advances in high throughput screening that mean it remains a preferred approach for hit identification today:

• Increasing scale and quality of the libraries
• Significant miniaturisation of assays
• Advancement of detection technologies
• Establishment of automation

High Throughput Screening at Domainex

At Domainex we offer high throughput screening using a variety of assay formats (biochemical, cell-based) in 384- or 1536-well format. We can access commercially available diversity libraries of lead-like compounds or focussed compounds directed towards target classes, modalities or therapeutic area, on your behalf. Various library sizes are available, to suit your budget and project needs. Alternatively, if you would prefer to provide your own library, Domainex would be happy to screen it for you.

Diversity or focussed compound selections can also be supplemented with target specific sets based on the output from ligand or structure based virtual screens conducted against Domainex’s curated database of ~5 million compounds (see our virtual screening page for more details). In addition to screening small molecule libraries, Domainex can supplement biochemical screening with the high concentration screening of fragment libraries against our library with >1,000 members (see our FragmentBuilder page for more details).

High-Quality Protein Supply

Our highly experienced Protein Science team routinely produce very high-quality target proteins using standard bioinformatics and literature-informed approaches or, if required, by deploying our proprietary technology Combinatorial Domain Hunting (CDH). Domainex deploys proteins for use in parallel in X-ray crystallography, biophysical screening, and for use in assay development/high throughput screening.

What Happens After High Throughput Screening?

With confirmed hits in hand, the next step is to evaluate the compounds, identify areas for improvement (e.g. potency or selectivity) and to establish structure-activity relationships (SAR). Domainex will provide you a team of highly-skilled medicinal chemists  and computational chemists, with experience in developing hits into lead compounds and development candidates. Domainex can also provide structural biology services in order to obtain high-resolution crystal structures of the hit compounds bound to your target of interest, which can help guide this elaboration process.