High throughput screening (HTS). Biological screening.

High throughput screening (HTS) of diverse compound libraries is a highly significant source of hit compounds. Assay automation and technology advances continue to have a significant impact on the range, mode and disease relevance of HTS campaigns. HTS assay is just the beginning of the hit finding approach and is followed by a well-considered cascade of counter, orthogonal, selectivity, and secondary assays that identify the best hit series, which helps to form the foundation for the next hit to lead phase.

Successful hit identification and subsequent expansion is hugely dependent on the library structure and quality. ChemDiv libraries that are purposefully built with arrays of recently synthesized compounds greatly improve the chances of finding highly promising hits. A reliable screening deck provides the information that helps organizations make critical decisions about the next steps in R&D process.

ChemDiv has assembled a robust high throughput screening platform encompassing automated liquid handling and multimode signal detection equipment for assays to be ran in up to 1536-well plate formats. Multimode reading capability provides access to screening assays with multiplicity of targets, such as receptors, enzymes, signaling pathways etc. that play a major role in different therapeutics areas (oncology, immunology, CNS, metabolic diseases).

ChemDiv offers logistics and compound handling support to High Throughput Screening (HTS) performed at our facilities, which substantially reduces time and eliminates costs associated with compounds shipments and plate preparations. Decades of stellar experience of being a worldwide manufacturer and supplier of chemical libraries to drug discovery institutions, uniquely positions ChemDiv, with its logistics infrastructure, to be able to backtrack every hit to its specific QC data for the original compound on the plate. Our proprietary focused discovery sub-libraries assembled from the ChemDiv’s ever-growing collection of 1.6 million small molecules, being synthesized based on novel templates ideas, provide tremendous benefits for high throughput hit hunting in terms of both potential hit novelty and follow up synthetic hit expansion. The unique design of these sublibraries provides a very robust way for early chemoinformatics-based identification and confirmation of hit compounds with immediate mini-SAR cluster analyses offering seed scaffolds, or starting points, for hit expansion, hit-to-lead exploration, and medicinal chemistry lead optimization.

We have assembled a robust screening infrastructure to be able to work with targets of major therapeutics areas. Our technical park of Discovery Division includes:

Equipment

• Liquid Handling
  • Biomek 4000,
  • Biomek NX,
  • Biomek FX work station
  • 96/384-well plate readers;
    • FLIPR-Tetra (Molecular Devices)
    • Microbeta PLUS 1450 (PerkinElmer),
    • scintillation counters;
    • Victor2V and Victor 3 multimode;
    • SpectraMax Plus 96/384;
    • Mach III (Tomtec) 96-well cell harvester;
    • Beckman and GUAVA 96/384 well format Flow Cytometers.

Readout capabilities

• Luminescence: Reporter genes; ELISAs;
• Fluorescence: FLINT, FRET, TR-FRET, FP, GFP; ELISAs
• Radio-Isotope: Receptor assays (ligand-binding/competition), SPA, metabolic enzymes

Absorbance: OD, ABS spectra

Ready to deploy assays

• In vitro assays:
  • FLIPR (cytoplasmic and mitochondrial calcium),
  • LANCE (cytoplasmic cAMP/cGMP),
  • ELISA,
  • Western,
  • Kinase activity, Enzymatic activity
• Cell Assays:
  • cell growth,
  • cell cycle analysis,
  • apoptosis/necrosis,
  • in vitro chemoinvasion,
  • high content high throughput microscopy
• Molecular and Cell Biology:
• Custom Expression / Reporter Constructs;
• Transient/stable transfection.
• Cell lines and primary cultures;

Custom Assay Development (per Clients’ specification).

Please contact our team at chemdiv@chemdiv.com to discuss your specific needs and application.