HTS/HCS Drug Discovery and Hit-to-Lead Drug Development

This site is specific for researchers interested in utilizing the D3SR Arm, which specializes in HTS/HCS probe and drug discovery using cellular and biochemical systems. We also specialize in three-dimensional (3D) HTS/HCS of complex cell-based models, organoids and tumor organoids (cell line or patient derived). This facility is newly renovated and features a new state-of-the-art custom robotic automation platform (the Explorer G3) that integrates new HTS/HCS instrumentation and equipment from PerkinElmer, Tek-Matic, and other leading vendors.

The Explorer G3 Work Station (PerkinElmer) is a custom designed automation platform that is fully enclosed, maintaining a clean sterile environment through a HEPA filtration system. The Explorer G3 has three levels, the main deck, and a middle and lower deck used to house instrumentation and equipment. The Explorer G3 has a track system robotic arm that integrates equipment on both the main and middle decks.

  • Janus G3 Automated Liquid Handling platform (96-and 384-channel MDT heads and pintool) 
  • Opera Phenix Plus HCS system (4 sCMOS cameras with live cell chamber)
  • Envision multi-mode plate reader (hybrid system of filters and quad monochromators) The
  • BioSpot (custom liquid handling platform for precise droplet delivery)
  • Liconic STX220 Cell Culture Incubator
  • Liconic STX500 Drug Library Storage Freezer. •Liconic LPX220 Plate Hotel
  • ELx405 Plate Washer (BioTek)
  • Centrifuge with Loader (Agilent)
  • 4titude 4AS Automated heat sealer/peeler (Books)
  • MultiFlo Bulk Liquid Dispenser (BioTek)

Other Equipment Utilized for Assay Development Not Integrated with The Explorer G3

  • Generation 1 Opera Phenix HCS system
  • Janus Automated Liquid Handling platform (96- channel MDT heads and 8-channel Varispan)
  • Envision multi-mode plate reader (Filter based)
  • Columbus server
  • 4-foot bio-safety cabinet (safety level II)

Compound Libraries

Kinase Inhibitor Library (SelleckChem): 875 compounds including clinically relevant or FDA approved kinase inhibitors.

Spectrum Collection (Discovery Systems): 2,320 compounds approved drugs (50%), diverse natural products (30%), and other bioactive compounds (20%).

Custom Drug-Like Diversity Sets (120,000 compounds): These libraries are intended for discovering drug-like molecules that can be translated into novel intellectual property. Inherent to these libraries are derivatives of each chemical scaffold, which can yield SAR (structure-activity relationship) that can guide downstream medicinal chemistry efforts. These libraries have been filtered to remove undesirable compounds (PAINS)

  • Diversity Library 1 has 20,000 compounds (Life Chemicals).
  • Diversity Library 2 has 50,000 compounds (ChemBridge)
  • Diversity Library 3 has 50,000 CNS specific compounds (ChemBridge)

Other Drug Discovery Core Facilities

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Computational Chemistry and Biology Core Facility

The Computational Chemistry and Biology (CCB) Core Facility provides a wide array of advanced tools and services for computational modeling simulations chemical and biological systems. 

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Medicinal Chemistry Core Facility

The Medicinal Chemistry Core Facility can provide a range of services related to chemical synthesis and lead drug development. 

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Mass Spectrometry (MS) Core Facility

The MS core facility utilizes advanced mass spectrometry instrumentation and techniques to assist researchers with their proteomic, metabolomics, and small molecule research.