Target Identification & Validation

We provide many different approaches to look for drug target such as:

Target to hit

  • Chemical library (>5.000 in house compounds available for biological screening)
  • Organic synthesis of small molecules & heterocyclic compounds
  • Drug hemisynthesis from natural products
  • Small to large scale compound purification
  • Chiral resolution of racemic compounds
  • Determination of physicochemical properties and complete characterization of organic compounds by spectral and elemental analyses
  • Bio-guided isolation and structural determination of natural substances
  • Preparative isolation of natural products at the gram scale (prepHPLC, prepCPC, prepTLC)
  • Lab scale extraction of natural products
  • Our Robotein Platform encompasses an Octet system that allows high-throughput analyses of protein interactions in 96- and 384-well microplates. It enables real-time and label-free determination of affinity, kinetics and concentration. This makes it highly suitable for the characterization of drug candidates.
  • Our GIGA imaging platform encompasses a Becton Dickinson’s (BD) Pathway 855 High-Content Bioimager, which is a high performing imaging solution for live or fixed cell samples combining image quality, flexible image capture and live-cell analysis.BD Pathway system provides fluorescence intensity measurements, kinetic imaging and morphological analysis, including sub-cellular imaging. Images can be captured in either confocal or wide field mode to deliver high-resolution images for subsequent analysis.

Hit to lead

The GIGA focuses on the study of membrane receptors with a particular interest in G protein coupled receptors of unknown or elusive function.

The lab has a large expertise in:

  • Development of original in vitro/ex vivo assays for the identification of active compounds
  • Molecular cloning, epitope-tag fusion and mutagenesis of receptors/protein of interest
  • Calcium assays
  • cAMP measurement
  • Resonance Energy Transfer technology (BRET and FRET)
  • Co-Immunoprecipitation
  • Critical assessment of existing assays for use in screening setting
  • Elucidation of active molecule mechanisms and signaling pathway
  • Discovery of original compounds modulating a protein/target
  • Complete pharmacological profile of active molecules (pharmacodynamics)
  • Analysis of signal pathways
  • Targeted mutagenesis for binding pocket determination
  • Receptor localization and trafficking
  • Receptor tissue expression
  • Chemical library screening (medium throughput)
  • Determination of chemical stability (non-enzymatic degradation), stability in biological fluids (plasma, saliva, gastric juice)
  • Assessment of passive absorption and permeability
  • Identification of drug transporter substrates
  • Prediction of blood brain barrier permeability
  • Evaluation of metabolic stability 
(Microsomal Stability, Plasma Stability, Hepatocyte Stability)
  • Protein Binding Assays (plasma, microsomal, brain)
  • CYP profiling and inhibition
  • Advanced mass spectrometry analysis of drugs and metabolites (identification and resolution of chemical structures)
  • Quantitative determination of the distribution in organs and tissues of small rodents by LC-MS
  • In silico prediction and PK/PD modeling of human ADME profile
  • Good Laboratory Practice (GLP) compliant toxicity studies in mice, rats or rabbits
  • Extended single dose (microdose) toxicity studies with hematology, clinical
  • Chemistry, necropsy, and histopathology data
  • Neurotoxicity, cardiotoxicity (ECG, BP) and respiratory toxicity
  • 28-days or 90-days repeated toxicity studies with non-compartmental toxicokinetics
  • Design of preclinical safety studies for authorization
  • Local clinical trial centre to cover phase I and II clinical studies jointly with University Hospital of Liège (close interaction with clinical experts)
  • Pharmacokinetic assessment in human
  • Metabolism assessment with identification of drug metabolites in human (in various sample matrices)
  • Comparison of drug biotransformation in human and animal
  • Identification of structural features: analysis of relationships of drug structure and biological responses to understand target and untargeted drug effects.
  • Degradation products identification or impurities profiling of active pharmaceutical ingredients and drug products
  • Bioanalysis of natural or xenobiotic components
  • Metabolism elucidation of food supplements
  • Biomonitoring of oxidative stress biomarkers
  • Evaluation of formulation and drug delivery technologies