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
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Extensive GPCR assay development capabilities
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Particularly for more challenging orphan GPCRs
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Novel approaches to target expression and cell line construction
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Custom expression constructs, multiple promoters to tune expression
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Multiple assay platforms
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Radioligand binding (receptor occupancy ligand association/dissociation kinetics)
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G-protein & second messenger modulation
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HTRF cAMP & IP-One (Cisbio), IP accumulation, GTPgS
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G-protein dependent and independent events
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beta-arrestin recruitment, Receptor internalization and recycling
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Additional Signaling / Cell Biology
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Multiple HTRF assays (pERK1/2, pAkt), Arachidonic acid release, ELISA (including MesoScale multi-parametric system)
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Label Free, Dynamic mass redistribution - DMR (Corning, Epic®), High content (GE InCell Analyzer)
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The Beacon HTS Collection
Comprised of 600k diverse, commercially-sourced and proprietary compounds:
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GPCR focused,
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30% of collection is proprietary
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Almost 100k compounds physically removed from commercially-sourced libraries after PAINS/REOS/internal data filtering
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Highly characterized in a large number of HTS campaigns using multiple assay platforms and screening modes
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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
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Robust data visualization tools
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Efficient data QC and primary screen analysis
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Hits can be rapidly profiled against a large panel of historical data sets
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Rapid elimination of promiscuous or otherwise undesirable molecules
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Minimizes resources wasted on unproductive chemistry
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Rapid focus on compounds that are more likely to be on-target and suitable for hit expansion