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High-Throughput Screening Core

Overview of Services

The mission of the High-Throughput Screening (HTSC) Core is to assist users with several aspects of early drug discovery, including target-based assay development and optimization, automated screening of small molecule libraries, and post-screen hit validation.

HTS is one of the most important tools in modern-day drug discovery. The premise of HTSC is to automate and miniaturize the assay process, thereby significantly decreasing the cost and time commitments of screening a biological target against thousands of chemical compounds.

The HTSC is comprised of a fully equipped wet lab, an equipment room, a cell culture room, and an office, totaling 1200 sq. ft. The space houses liquid handling equipment, plate readers, an Echo acoustic dispenser, 5 -30°C freezers for compound storage, a tissue culture incubator, a biosafety cabinet, and 3 data analysis workstations.  The lab is equipped with the necessary components to perform all aspects of protein purification, assay development and optimization, protein crystallization, and high-throughput screening.

Compound libraries

The HTS core currently offers a library of over 100,000 diverse, drug-like compounds and a number of specialty compound sets available for screening. Researchers at UIC who wish to deposit novel compounds or natural product fractions into our collection are encouraged to do so.

Current libraries include:

  • Enamine’s Discovery Diversity set (10,000 compounds)
  • ChemDiv SMART library (10,000 compounds)A 10K subset of SMART ChemDiv library that (1) is pruned for known frequent hitters (PAINS and alike), (2) is balanced in terms of diversity of chemical scaffolds, (3) functional groups are equally represented, (4) has several representative analogs for each of the scaffolds in the library. www.chemdiv.com/products/screening-libraries/smart-library/ 
  • ChemDiv PPI library (10,000 compounds): A 10K subset of the ChemDiv protein-protein interaction library, curated to follow rules 1-4 above.
  • >50,000 compounds from the ChemBridge DiverSet and ExpressPick libraries  
  • MicroSource Spectrum Collection (2,700 compounds and purified natural products)
  • a growing compilation of unique compounds synthesized by UIC chemists (~300 compounds to date)
  • Targeted sets from TargetMol:
    • Epigenetics Inhibitor Library (380 compounds)
    • Autophagy Library (623 compounds)
    • Anti-Metabolism Disease Compound Library (816 compounds)
    • Anti-Cardiovascular Disease Compound Library (515 compounds)
    • Anti-obesity Compound Library (85 compounds)
    • Bioactive Compound Library (5370 compounds)
    • Endocrinology-Hormones Library (297 compounds)
    • Coagulation and anticoagulation Compound Library (153 compounds)
    • GPCR Compound Library (730 compounds)
    • Nuclear-receptor Inhibitors Library (239 compounds)
    • Kinase Inhibitors library (900 compounds)
    • Anti-diabetic Library (179 compounds)
    • Ion Channel Inhibitor Library (362 compounds)
    • Adrenergic Library (117 compounds)
    • Serotonin Library (134 compounds)
    • Cytokines inhibitor Library (182 compounds)
    • TGF-beta Smad Compound Library 45 compounds)
    • Wnt&Hedgehog&Notch Compound Library (74 compounds)
    • Angiogenesis Related Compound Library (378 compounds)
    • CNS-Penetrant Compound Library (90 compounds)
    • Calcium Antagonists Library (48 compounds)
    • Chromatin Modification Compound Library (192 compounds)
    • Anti-Aging Library (833 compounds)
    • Bioactive Plus Compound Library (200 compounds)
    • Protease Inhibitor Library (162 compounds)
    • PI3K/Akt/mTOR Inhibitor Library (190 compounds)
    • Anti-virus Compound Library (157 compounds)
    • Anti-infection Compound library (605 compounds)
    • Anti-cancer Approved Drug Library (313 compounds)
    • Anti-cancer Clinical Compound Library (560 compounds)
    • Histone Modification Research Compound Library (152 compounds)
    • JAK STAT Compound Library (145 compounds)
    • NF-kB Signaling Compound Library (173 compounds)
    • DNA Damage & Repair Compound Library (475 compounds)
    • Antibiotics Library (250 compounds)
    • Antifungal Compound Library (66 compounds)
    • Immunology Inflammation Compound Library (876 compounds)
    • Potassium Channel Blockers Library (60 compounds)
    • Sodium Channel Blockers Library (62 compounds)
    • Cell cycle related Compound Library (130 compounds)
    • Apoptosis Compound Library (191 compounds)

 

High-throughput protein crystallization

The Echo acoustic dispenser is ideally suited to carry out high-throughput protein crystallization. Users can typically screen over 1000 crystallization conditions in under 2 hours. Crystallization plates contain 96 wells, with 3 sitting drop compartments per well, with a 100-500 nL protein + 100-500 nL crystallization reagent capacity per compartment.  all completed plates are sealed with an optically clear adhesive and stored in temperature-controlld, vibration-free incubators. The HTSC is stocked with various crystallization suites  from suppliers such as Hampton Research and NeXtal, with each suite containing 96 unique conditions. Users have the option to supply their own crystallization screens in 96 deep-well blocks.

Stocked crystallization screens (96 conditions each):

  • PEG/Ion HT (Hampton)
  • PEG Rx HT (Hampton
  • Salt Rx HT (Hampton)
  • Crystal Screen HT (Hampton)
  • Anions (NeXtal)
  • Cations (NeXtal)
  • MPDs (NeXtal)
  • ComPAS (NeXtal)
  • MCSG-1 (Microlytic)
  • MCSG-2 (Microlytic)
  • MCSG-3 (Microlytic)
  • MCSG-4 (Microlytic)
  • PACT Premier (Molecular Dimensions)

 

 

Leadership

Kiira Ratia, PhD | Director | (312) 355-1296 | kratia@uic.edu

Location and hours of operation

Location Hours

900 S Ashland Ave

Room 3368

 

Monday - Friday

9 am - 5 pm 

Links and Resources

  1. High-Throughput Screening Informational Site
  2. Getting Started Help Site

Contacts

Name Role Phone Email Location
Kiira Ratia, PhD
Director
 
(312) 355-1296
 
kratia@uic.edu
 
MBRB Room 3370
 

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