A membrane permeability database for nonpeptidic macrocycles
2025

Membrane Permeability Database for Nonpeptidic Macrocycles

Sample size: 4216 publication Evidence: high

Author Information

Author(s): Feng Qiushi, De Chavez Danjo, Kihlberg Jan, Poongavanam Vasanthanathan

Primary Institution: Uppsala University

Hypothesis

The study aims to create a comprehensive database of membrane permeability for nonpeptidic macrocycles to facilitate drug discovery.

Conclusion

The database provides valuable insights into the membrane permeability of nonpeptidic and semipeptidic macrocycles, aiding predictions for drug discovery projects.

Supporting Evidence

  • The database houses 5638 membrane permeability datapoints for 4216 nonpeptidic macrocycles.
  • It includes a new descriptor, the 'amide ratio' (AR), to classify macrocycles.
  • The resource is designed to be findable, accessible, interoperable, and reusable (FAIR).
  • The database will be updated biannually to include new data.

Takeaway

This study created a big online library that helps scientists find out how well certain drugs can get into cells, which is important for making new medicines.

Methodology

The study involved collecting and curating permeability data from literature, patents, and bioactivity repositories, resulting in a database of 5638 datapoints for 4216 macrocycles.

Limitations

The database does not provide conformations due to high computational costs and uncertainty in conformational sampling.

Digital Object Identifier (DOI)

10.1038/s41597-024-04302-z

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