The VIB Compound Screening Facility (CSF) has built up expertise in assay development and compound screenings and has acquired several high quality chemical libraries for primary screening purposes. Required robotic systems and equipment are available at CSF.
Services at the VIB Compound Screening Facility
Core Services
CSF has the expertise and equipment to perform a full screening project. This includes:
• Preparation of assay plates
• Compound screening
• Analyzing the effect of the compounds by using microscopes or plate readers
Additional Services
We can advice on and assist in assay development, i.e. optimizing, validating and downscaling the assay to 96-well or 384-well plate format. After hit compound identification, services for further compound characterization can be provided, i.e. determining the EC50 values, identifying the active substructures of a compound through analysis of structural analogues and initial lead optimization of identified hit compounds. We can also perform detailed bimolecular interaction analysis by using Biacore technology to study the interaction between a compound and its target protein.
Ultimately, the deliverable of CSF is a set of chemical compounds in dry format or dissolved in DMSO, which target the biological process under study. We are operated by technical personnel specialized in the necessary technologies.
Platform at the VIB Compound Screening Facility
Compound collection
Our compound screening collection amounts to a total of 42,000 compounds. The collection comprises three different chemical libraries acquired through ChemBridge Corporation; DIVERSet™ (22,000 compounds), CNS-Set™ (10,000 compounds) and NOVACore (10,000 compounds). For selection of the DIVERSet™ compounds, a range of filtering methods are applied to ensure maximal diversity with a minimal number of compound, and to remove unstable, toxic and non-drug-like compounds. This library can be used in initial screening programs that require high diversity and qualitative lead-like compounds. For the CNS-Set™ library, additional computational methods are applied to select compounds with increased probability of oral bioavailability and blood-brain-barrier penetration. NOVACore is a diverse and drug-like library comprising compounds that are synthesized via combinatorial chemistry. The main focus here is ‘novelty’; all compounds are recently synthesized by ChemBridge and contain mainly proprietary ChemBridge building blocks. All NOVACore compounds have a low molecular weight, which allows more margin for further lead optimization. The three libraries can be used as primary screening tools for a wide range of biological assays. After hit identification, similar compounds for additional testing can be selected from ChemBridge’s main stock collection of more than 500,000 compounds.
Compound storage
To maintain compound integrity during larger periods of time, we use 4titude’s PlateStable™ conditioned storage system. All library compounds are stored in a 100% nitrogen atmosphere to minimize water uptake and the damaging effects of atmospheric oxygen. This significantly reduces the well-known problems with DMSO-dissolved compounds such as degradation, dilution and precipitation.
High-throughput screening equipment
We have established a state-of-the-art high-throughput platform for screening chemical compound libraries. The platform consists of robotic systems that make it possible to prepare assay plates and to add compounds to the assay system in a high-throughput fashion. The exerted effects of the compounds can be analyzed by using different equipment for visual (microscopy-based) or digital (plate reader-based) read-out.
For prices and project information, please contact Dominique Audenaert, CSF manager.
