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GPCR Screening Library

2D Similarity-based GPCR Focused Screening Library
Receptor-based GPCR Targeted Library

Seven-transmembrane receptors, also known as G-protein-coupled receptors (GPCRs), are integral membrane proteins that contain seven membrane-spanning helices. This superfamily of cell surface signaling proteins plays a critical role in many physiological processes and diseases, including cancer. GPCRs and GPCR-related proteins upstream (e.g., ligands) and downstream (e.g., phosphodiesterase [PDEs] for cAMP degradation) from GPCRs account for approximately 17% of all protein targets for approved drugs. Thus, GPCRs are one of the most popular drug targets today. Almost one-third of the currently approved drugs rely on some kind of interaction with these receptors. Approved drugs targeting GPCRs and GPCR-related proteins are primarily small molecules and peptides. In the future, the number of GPCR targets, GPCR-based drugs and the types of drugs will continuously increase since approximately 100 of more than 360 human endogenous GPCRs are orphan GPCRs.

BOC Sciences has established a high-quality library of small GPCR compounds to screen for GPCRs with unknown function, yielding potential novel GPCR candidates.

Dynamics of the G-protein in the mechanism of activation of a GPCR.  Figure 1. Dynamics of the G-protein in the mechanism of activation of a GPCR. (Martins, S.; et al. 2012)

GPCR Screening Library Design

Given the importance of GPCR in small-molecule drug discovery, BOC Sciences offers a range of potential GPCR activity modulators. Our teams apply ligand-based (computational chemistry, 2D fingerprint similarity search) and receptor-based (molecular docking, high-throughput virtual screening) methods to select GPCR-focused screening compounds.

  • Our GPCR library contains more than 8,000 novel and scaffold-based compounds designed using a series of GPCR-associated scaffolds that mimic the β-turn motif of endogenous peptide ligands
  • Randomly selected samples from the entire GPCR library have been validated against GPCR targets, and agonists and antagonists have been identified

GPCR Screening Library Characteristics

  • A great number of small molecules that target G protein-coupled receptors for both high-throughput and high-content screening are provided
  • All small molecules in the GPCR screening library are biologically and pharmaceutically active
  • The library contains receptor-related small molecules, including 5-HT receptors, dopamine receptors, opioid receptors, adrenergic receptors, cannabinoid receptors, mGluR, and ETA-receptors, among others
  • No PAINS or toxic substances/unwanted functions: filtered by strict ‘Ro5-like’ physicochemical and most stringent in-house structural filters
  • Valuable tool for finding the most promising GPCR drugs
  • Bioactivity and safety confirmed by preclinical studies and clinical trials
  • Structural diversity, medicinal activity, and cellular penetration
  • Structural document, IC50, and other chemical and biological data are provided
  • All compounds are continually updated
  • Compound cherry-picking service is provided

What We Deliver

  • Delivered within 2 weeks in any customer-preferred format
  • Powders, dry films or DMSO solutions formatted in vials, 96 or 384-well plates
  • All compounds have a minimum purity of 90% assessed by 1H NMR and HPLC
  • Analytical data is provided

BOC Sciences provides professional, rapid and high-quality services of GPCR Screening Library design at competitive prices for global customers. Personalized and customized services of GPCR Screening Library design can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!

Reference

  1. Martins, S.; et al. GPCR screening and drug discovery: Challenges and latest trend. European Pharmaceutical Review. 2012. 17(2).
Our mission is to provide clients with a professional chemical library design platform. Empowered by high-quality services and effective research solutions, we are committed to helping customers achieve effective and successful research goals.

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Services Based on the Chemical Library Design Platform

Services Based on the Chemical Library Design Platform

BOC Sciences has rich experience in working with global customers in custom library synthesis of compounds and generating small to medium-sized libraries of target compounds. Our knowledge in generating a large number of target molecules in a remarkably shorter time enables quick biological screenings for affinities. With the target properties in mind, we deliver target molecules, by applying our extensive knowledge in drug discovery.

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