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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