Oleneva Polina, Zabolotna Yuliana, Horvath Dragos, Marcou Gilles, Bonachera Fanny, Varnek Alexandre
Laboratoire de Chémoinformatique, UMR7140 CNRS/UniStra, University of Strasbourg, 4 rue Blaise Pascal, 67081, Strasbourg, France.
Mol Inform. 2023 Apr;42(4):e2200208. doi: 10.1002/minf.202200208. Epub 2023 Feb 6.
In order to analyze the Chimiothèque Nationale (CN) - The French National Compound Library - in the context of screening and biologically relevant compounds, the library was compared with ZINC in-stock collection and ChEMBL. This includes the study of chemical space coverage, physicochemical properties and Bemis-Murcko (BM) scaffold populations. More than 5 K CN-unique scaffolds (relative to ZINC and ChEMBL collections) were identified. Generative Topographic Maps (GTMs) accommodating those libraries were generated and used to compare the compound populations. Hierarchical GTM («zooming») was applied to generate an ensemble of maps at various resolution levels, from global overview to precise mapping of individual structures. The respective maps were added to the ChemSpace Atlas website. The analysis of synthetic accessibility in the context of combinatorial chemistry showed that only 29,7 % of CN compounds can be fully synthesized using commercially available building blocks.
为了在筛选和生物相关化合物的背景下分析法国国家化合物库(Chimiothèque Nationale,CN),将该库与ZINC现货库和ChEMBL进行了比较。这包括对化学空间覆盖范围、物理化学性质和Bemis-Murcko(BM)骨架群体的研究。鉴定出了超过5000个CN独特骨架(相对于ZINC和ChEMBL库)。生成了容纳这些库的生成地形映射(GTM)并用于比较化合物群体。应用分层GTM(“缩放”)以生成从全局概览到单个结构精确映射的各种分辨率级别的映射集合。相应的映射已添加到ChemSpace Atlas网站。在组合化学背景下对合成可及性的分析表明,仅29.7%的CN化合物可以使用市售构建块完全合成。