Assay development

ChemDiv’s team of trained and highly experienced scientists is proud to offer unparalleled expertise in developing and accommodating assays for HTS format and designing orthogonal assays for early identification and removal of false positive hits from further costly follow up processes. Not being limited to a third party libraries for screening and by offering our proprietary focused discovery sub-libraries assembled from the ChemDiv’s ever-growing collection of 1.6 million small molecules, being synthesized based on unique ideas of novel templates, provides tremendous benefits for high throughput hit hunting. Unique design of these sublibraries provides a very robust way for early mini-SAR analysis for identification and confirmation of hit series, which then become seed templates for hit expansion, hit-to-lead exploration, and medicinal chemistry lead optimization.

A robust screening platform encompassing automated liquid handling and multimode signal detection equipment have been assembled at ChemDiv to be able to provide access to screening assays for multiplicity of targets, such as receptors, enzymes, signaling pathways etc., which play major role in different therapeutics areas (oncology, immunology, CNS, metabolic diseases).

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 2000,
  • 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;

Selection of cell line with endogenous xxx expression and Ca²⁺ response to agonistOptimization

• Agonist dose response curve
• Optimum plate type, cell density and FBS concentration (minimal acceptable concentration), HEPES presence (helpful in some cases)
• Optimum dye loading conditions: concentration/ T°C/time dependence/probenecid concentration (for cells like CHO)
• Optimum FLIPR conditions: solutions addition height and speed, mixing parameters
• DMSO tolerance
• Reagents stability at RT

Validation

• NIH validation protocol
• Statistics (Z’-factor; S/B; S/N; %CV)
• Edge and drift effects

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