Hit characterisation and mode-of-action assays

Lead compound refinement

Our specialised assays are designed to help you refine hit lists and guide lead finding and optimisation, to provide a deeper understanding of compound behaviour in vitro and, ultimately, in vivo. Our team of screeners, protein scientists, structural biologists and chemists collaborates closely with you to deliver comprehensive insights that support your decision-making process, from off-target assays and species selectivity assays to comparative analyses of cell-based high-content screening, biophysical assays and biochemical data.

Setting up an experiment at an automated multimode detection device

Mode-of-action determination

Recognising when mathematical assumptions fail is crucial, especially for tight binding and time-dependent inhibition, common with potent or covalent inhibitors. We provide variable (pre)incubation times and jump dilution assays for detailed binding kinetics analysis in high-throughput screening, as well as variable enzyme concentration assays to identify tight binders. Our high-substrate assays are specifically designed to help you efficiently identify competitive and uncompetitive orthosteric inhibitors.

Kinetic and thermodynamic analyses

The Nuvisan team provides valuable insights into the kinetics of inhibitor–target interactions (k_on, k_off/residence time), offering more than just affinity measurements. Using methods such as our proprietary kinetic probe competition assay (kPCA) and surface plasmon resonance (SPR), we can help predict in vivo efficacy and selectivity, especially for slow binders, and enhance the outcomes of cell-based assays. By uncovering structure–kinetic relationships, we support your lead optimisation efforts. For thermodynamic analyses, we discuss options tailored to your project, including isothermal titration calorimetry (ITC), SPR and equilibrium and kinetic probe competition assays.

Tailored assays to probe alternative mechanisms

Tailored assays are developed to explore alternative mechanisms of your drug molecule, providing insights into, for example, irreversible binding, kinetic selectivity and the effects of activators on compound behaviour. These assays support highly accurate predictions of in vivo performance and aid in overcoming challenges in drug discovery.

Biophysical solutions

Our biophysical platform can support you with your lead identification and optimisation efforts.

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High-content assays

Our high content assay services provide precise and comprehensive cellular analysis.