Compound Screening Platform

We collaborate with researchers at the Center as well as national/international cooperation partners and custom-design screening assays for the identification of novel bioactive molecules. Here, a major focus is devoted to the development of phenotypic assays for high-content-screening (HCS) in order to better reflect the biology of the underlying disease state. We use machine learning techniques to analyze high-content images. We provide state-of-the-art equipment and screening techniques as well as oversee the in-house diversity and focused compound libraries.

Biochemical assays:

• Protein-Protein-Interaction (PPI) assays:
  • AlphaScreen interaction assay (homogenous assay)
  • TR-FRET (HTRF) interaction assay (homogenous assay)
  • DELFIA time-resolved fluorescence assay (ELISA based assay)
  • Microscale thermophoresis (MST)
  • Pull down assays (GST, StrepTagII, His, GFP-Trap, etc.) 
• Enzymatic assays:
  • DUBs (AMC, IQF-diUb, AlphaScreen, etc.)
  • Protease cleavage assay (e.g., AMC substrates)
  • Kinase assays (AlphaScreen, HTRF, ELISA)
  • Phosphatase assays (AlphaScreen, HTRF)   
• Protein-Compound and Nucleic Acid-Compound Interactions:
  • Microscale thermophoresis

Cell-based HCS/HTS assays:

• High-Content Screening (HCS) using the Operetta System:
  • Stem Cell screening
  • 3D cell systems
  • Morphology analysis (e.g., neurons)
  • Cellular profiling using Cell painting assay
  • Cellular substructures (e.g., spots, organelles, etc.)
  • Cellular translocation analysis (e.g., between Nucleus and Cytoplasm)
  • Protein-Protein Interactions (e.g., BiFC, FRET)
  • High-Content Image Analysis with specialized software and Machine Learning/Deep Learning
• High-Throughput Screening (HTS):
  • Protein-Protein Interactions (NanoBRET)
  • Fluorescence-based reporter assays
  • Cell viability assays
  • Apoptosis assays

Diversity libraries (30,000 bioactive compounds):

• ChemDiv subset
  • Diversity selection of 10,000 compounds
  • Approx. 50% of the compounds have the ability to cross the blood brain barrier (information from calculations) 
• Enamine subset
  • Diversity selection of 10,000 compound 
• ChemBridge subset
  • Diversity selection of 5,000 compounds
• ChemDiv Protein-Protein Interaction (PPI) subset
  • Diversity selection of 5,000 compounds
  • Focus on PPI inhibition

Focussed libraries:

• Prestwick FDA approved drugs 
• Medchem Express FDA approved drugs
• Repurposing library 
• GPCR compound library