Proteases

Proteases

The Protease Database is the Aureus Sciences' knowledge base containing proteases, modulators-relevant chemical information associated with quantitative biological activities and mechanisms of action.

      Main Features
    • Structure-activity data culled from international scientific journals and patents (US, Euro & international)
    • Includes proteases from human, parasites, virus or other species
    • Detailed descriptions of the experimental methods and conditions used to generate activity data points
    • Data organized in relational tables according to: chemical information, protein target information, bioactivity and experimental methods

      AurSCOPE Proteases Database Protocols

      Uses

    • Medicinal chemists, cheminformaticians, pharmacologists and biologists use the knowledge base to:
    • Retrieve ligands tested as inhibitor or activator of a protease
    • Retrieve selective molecules for a specific protease vs. another protease
    • Assess ligands’ mechanism of action, study structure activity relationships to guide compound optimization
    • Access in vitro and in vivo pharmacological activity data, materials and methods used
    • Search records via text and numeric queries (biological activity and biological data field searches)
    • Export data to SD files, .txt and .xls formats
      Chemical Information
    • Registered ligands always associated with at least one quantitative experimental biological data
    • Compound descriptions including structure, name, synonyms, pharmaceutical codes, therapeutic class, calculated physicochemical parameters and SMILES
    • Druggability assessments using graphical representation based on Lipinski/Weber rules
      Protein Target Information
    • Hierarchically organized protease target by names, acronyms and synonyms
    • Target descriptions including species and transfection method
    • Description of drug-resistant protease variants and of in vitro engineered mutants
    • Links to Uniprot (SwissProt), GenBank and Protein Data Bank (PDB) where available
      Bioactivity and Experimental Methods
    • Detailed biological material descriptions (species, tissue, cell, etc.)
    • Extensive in vitro (enzymology, cell toxicity, infection, coagulation) and in vivo experimental methods
    • Drug target selectivity
    • In vivo protocols described by all experimental model details and compound route of administration
    • Pharmacokinetics data where appropriate
    • All activity data points with normalized parameters and units
    • Reference to the journals, patents and links to PubMed and Espacenet
      Semantics and Quality Controls
    • Standardized Thesauri, Glossaries, Ontology Management-based process with hierarchies
    • All registered data updated regularly utilizing validated Glossaries/Thesauri
    • Specialized quality control at every production step
    • Databases updated and released every three months

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