Drug Discovery Capabilities

RECEPTOR PHARMACOLOGY

 

Beacon has a long history working with GPCRs and has built state-of-the-art labs employing the latest proprietary know how and the latest assay platforms to interrogate receptor pharmacology.

 

GPCR Assay Development

 

  • Extensive GPCR assay development capabilities

    • Particularly for more challenging orphan GPCRs

  • Novel approaches to target expression and cell line construction

    • Custom expression constructs, multiple promoters to tune expression

  • Multiple assay platforms

    • Radioligand binding (receptor occupancy ligand association/dissociation kinetics)

    • G-protein & second messenger modulation 

      • HTRF cAMP & IP-One (Cisbio), IP accumulation, GTPgS

    • G-protein dependent and independent events

      • beta-arrestin recruitment, Receptor internalization and recycling

    • Additional Signaling / Cell Biology

      • Multiple HTRF assays (pERK1/2, pAkt), Arachidonic acid release, ELISA (including MesoScale multi-parametric system)

    • Label Free, Dynamic mass redistribution - DMR (Corning, Epic®), High content (GE InCell Analyzer)

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The Beacon HTS Collection

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Comprised of 600k diverse, commercially-sourced and proprietary compounds: 

  • GPCR focused, 

  • 30% of collection is proprietary

  • Almost 100k compounds physically removed from commercially-sourced libraries after PAINS/REOS/internal data filtering

  • Highly characterized in a large number of HTS campaigns using multiple assay platforms and screening modes

  • Detailed knowledge of compounds likely to be promiscuous or possessing unattractive chemical features, based on previous hit follow-up efforts

 

The Beacon Database

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  • Internally developed to meet specific needs

  • Robust data visualization tools

  • Efficient data QC and primary screen analysis

  • Hits can be rapidly profiled against a large panel of historical data sets

    • Rapid elimination of promiscuous or otherwise undesirable molecules

    • Minimizes resources wasted on unproductive chemistry

  • Rapid focus on compounds that are more likely to be on-target and suitable for hit expansion

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