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April 21, 2021Drug Discovery Today20 citationsOpen Access

The European Lead Factory: An updated HTS compound library for innovative drug discovery

HVHerman van VlijmenJOJean‐Yves OrtholandVLVolkhart M.‐J. Li

Key Points

  • The aim is to assess the physicochemical and diversity properties of the updated compound collection for drug discovery.
  • Analyzed the updated compound library for diversity and drug-like properties.
  • Utilized high-throughput screening techniques for validation and assessment.
  • Compared the library's compounds to existing commercial screening libraries.
  • The updated compound library is shown to be highly diverse and drug-like.
  • It complements existing commercial screening libraries in physicochemical properties.
  • The library brings together compounds from various therapeutic areas and new synthesis.

Abstract

Through the European Lead Factory model, industry-standard high-throughput screening and hit validation are made available to academia, small and medium-sized enterprises, charity organizations, patient foundations, and participating pharmaceutical companies. The compound collection used for screening is built from a unique diversity of sources. It brings together compounds from companies with different therapeutic area heritages and completely new compounds from library synthesis. This generates structural diversity and combines molecules with complementary physicochemical properties. In 2019, the screening library was updated to enable another 5 years of running innovative drug discovery projects. Here, we investigate the physicochemical and diversity properties of the updated compound collection. We show that it is highly diverse, drug-like, and complementary to commercial screening libraries.

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Cite This Study

Vlijmen et al. (2021) studied this question.

synapsesocial.com/papers/6a0f1984b7d829a1276c8dbehttps://doi.org/10.1016/j.drudis.2021.04.019
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