Journal of Chemical Information and Modeling · 2017 · 113 citations · 10 references
PharmacyBioinformaticsMedicinal ChemistryComputational Medicinal ChemistryDrug DesignDrug DiscoveryChemical Library DesignChemical Space AnalysisChemical Space ExplorationComputational Drug DiscoveryDe Novo Drug DesignLibrary DesignBioactive Chemical SpaceCell-based AssaysCell-based Pharmacological AssaysCell-based Screening AssaysChemical Space DesignLibrary Diversity GenerationUnfolded Protein Response
We describe a new library generation method, Machine-based Identification of Molecules Inside Characterized Space (MIMICS), that generates sets of molecules inspired by a text-based input. MIMICS-generated libraries were found to preserve distributions of properties while simultaneously increasing structural diversity. Newly identified MIMICS-generated compounds were found to be bioactive as inhibitors of specific components of the unfolded protein response (UPR) and the VEGFR2 pathway in cell-based assays, thus confirming the applicability of this methodology toward drug design applications. Wider application of MIMICS could facilitate the efficient utilization of chemical space.
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Open Babel: An open chemical toolbox
Noel M. O’Boyle, Michael Banck, Craig A. James et al. · Journal of Cheminformatics · 2011 · 11.1K citations · Full text