Kinases

Kinases

The Kinase Database is the Aureus Sciences' knowledge base encompassing kinases, modulator-relevant chemical data associated with quantitative biological activities and mechanisms of action.

All chemical and bioactivity data are organized in an Oracle database according to the Aureus relational data model.
 

      Main Features
    • Structure-activity data culled from international scientific journals and patents (US, Euro & international)
    • Covers all kinases with published SAR data,with a special focus on human kinome
    • 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 Kinases Database Protocols

      Uses
       Medicinal chemists, cheminformaticians, pharmacologists and biologists use the  knowledge base to:

    • Retrieve ligands tested as kinase inhibitor or activator
    • 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 kinase target by names, acronyms and synonyms
    • Target descriptions including species, action site and transfection method
    • Description of clinically relevant drug-resistant kinase variants and of in vitro engineered mutants
    • Links to Uniprot (SwissProt), GenBank and Protein Data Bank (PDB) where available
    • Detailed biological material descriptions (species, tissue, cell, etc.)
    • Extensive in vitro (enzymology, cell proliferation, binding, flux) and in vivo experimental methods
    • Drug target selectivity
    • In vivo protocols, including preclinical models of antitumor activities, 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

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