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Screening of focused ligand libraries

Identify potential drug candidates that interact with the selected target in a quantitative kinetics binding assay

Ligand screening is an essential step in drug discovery, where robust methodology and high-quality data are essential for validating molecular interactions in a live cell environment. With LigandTracer, the interaction affinity and kinetics of focused ligand libraries can be quantified directly on cells, tissue, or immobilized targets in a real-time binding assay.

This approach enables you to identify the most promising ligands early on saving time and resources while ensuring high-quality data for downstream optimization and minimizing the need for animal studies.

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For complex systems like GPCRs, live-cell competition assays enable high-resolution screening of ligands in native membrane environments. This method quantifies both displacement and replacement rates of bound labeled ligand by competing ligands, making it suitable for evaluating ligand interactions in dynamic receptor states.

Gained information

  • Precise hit selection based on kinetic behavior
  • Comparative ranking of binding affinities
  • Evaluation of ligand modifications (e.g., mutations, tags, conjugates) on binding kinetics
  • Evaluation of binding mechanism

Key publications

These publications illustrate the application well. Click here for more examples

Affinity maturation and optimization of CD44v6-targeting antibodies for molecular radiotherapy.
Mortensen ACL, Hofström C, Persson H, Dahllund L, Frejd FY, Nestor M.
Nucl Med Biol. 2025. 144-145:109012.
Summary
PubMed

Design, Synthesis, and Biological Evaluation of Small-Molecule-Based Radioligands with Improved Pharmacokinetic Properties for Imaging of Programmed Death Ligand 1.
Krutzek F, Donat CK, Ullrich M, Stadlbauer S.
J Med Chem. 2023. 66(23):15894-15915.
Summary
PubMed

Selection of an optimal cysteine-containing peptide-based chelator for labeling of affibody molecules with 188Re.
Altai M, Honarvar H, Wållberg H, Strand J, Varasteh Z, Rosestedt M, Orlova A, Dunås F, Sandström M, Löfblom J, Tolmachev V, Ståhl S.
Eur J Med Chem. 2014. 87:519-528.
Summary
PubMed