With our hit identification approach we deliver high-quality compounds with confirmed activity against a biological target. We determine validated hits with the best chance of success to develop into a drug-like compound. These target compounds are called “hits” and are often the starting points for chemistry activities.
One of the most prominent ones is high throughput screening (HTS). Over the past decades, unbiased HTS remained one of the core approaches of many pharmaceutical and biotechnology companies to identify novel starting points for drug development. In fact, a recent analysis of clinical candidates suggests that random HTS generates ~30% of novel leads. The quality of the outcomes from the HTS campaigns depends on several factors such as robustness and quality of the primary assay, buffer composition, readout technology, kinetics including incubation times and temperatures, composition of the compound library, quality of automation, as well as the post-screen hit-triaging strategy. Evaluating the hits in order to select hit compounds that are worth pursuing form HTS campaigns as a chemical lead in a drug discovery program is a major challenge. Therefore, we have appropriate follow-up assay cascades in place, because they are crucial for any successful hit-finding effort.
Pivot Park Screening Centre is organized in a matrix structure. Internal members (including a project leader, one to two assay developers, one to two robot operators, and also an account manager) and external outsourcing partner members form a project team. Projects have clear milestones, deliverables, acceptance criteria, and timelines; they typically start with kickoff meetings and scheduling progress report meetings. Followed by either the transfer of existing assay cascades from our customers or the development of novel screening assay cascades from scratch. Subsequently optimizing and miniaturizing to a uHTS-ready format.
Pivot Park Screening Centre receives and screens customer libraries ranging from thousands to millions of compounds. We mainly screen in 384- or 1536-well formats of both echo-compatible and noncompatible plates or alternatively screens our own ~0.3 million diverse compound library. Fully automated data analysis follows. Identified active compounds are typically retested and then redelivered in REMP tubes. The compounds are profiled in primary and follow-up assays for hit triaging and subsequent dose-response curve (DRC) testing and biophysical characterization for confirmed hit characterization.
Our passionate team has longstanding experience in hit identification utilizing the latest techniques, including both the chemistry and the biology necessary for the identification and refinement of these high-quality hits. Providing you with a starting point that already has many of the characteristics that you look for in your final drug.
During our hit identification process we reduce the amount of potential false positives; thus also reducing the risk of identifying a series of compounds that are suboptimal for development. This means that you are not spending your resources on the wrong compounds. A successful hit identification campaign relies on the use of a high-quality and chemically diverse compounds. Here you can find out more about our compound library.
With our expertise in assay development and screening activities we support your hit identification efforts. Transfer your assays to our facility, where our team miniaturizes and validates them for ultra High Throughput Screening. Just a target? No problem, our skilled assay development team designs your assay based on your unique needs.
When miniaturisation and automation of the assay are ready, our screening team starts its hit identification efforts. This not only includes access to our large, chemically diverse compound library but also to our complete infrastructure, including fully automated data analysis software.