Many therapeutically relevant targets remain resistant to traditional small-molecule screening approaches. These “undruggable” targets require innovative strategies to uncover new, ligand-efficient starting points.

At SpiroChem, we have developed the Rescue Package — an integrated workflow that combines macrocycle screening, biophysical characterization, and crystal soaking validation. This powerful approach enables the identification and structural validation of hits where conventional methods often fail.

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Step 1: Macrocycle Library

Our unique and diverse macrocycle library provides access to novel chemical space beyond traditional small molecules.

  • 8,200 to 960 semi-peptidic compounds, ready for screening (10 mM in DMSO)
  • Molecular weight < 900 Da
  • Designed for high conformational flexibility and enhanced binding potential

Step 2: Biophysical Screening

We leverage state-of-the-art affinity-based screening techniques to detect even the weakest or most transient interactions.

  • Quantification of binding affinity and kinetics
  • Detection of weak interactions often missed in HTS campaigns
  • Scalable and broadly applicable across diverse target classes

Step 3: Crystal SmartSoak® Validation

Our Crystal SmartSoak® platform provides structural confirmation and visualization of the identified hits.

  • High-resolution crystallographic validation of binding modes
  • Structural insights for rational lead optimization
  • Enables structure-based drug design for challenging targets

Why Choose the Rescue Package?

By combining advanced chemistry, sensitive biophysics, and high-quality structural biology, the Rescue Package helps transform previously inaccessible targets into actionable opportunities for drug discovery.


💡 Interested in learning more?

Get in touch with our team to discuss how the Rescue Package can support your discovery programs.