Prestwick GPCR Drug Library

A set of approved drugs
known to interact with a GPCR

G protein-coupled receptors (GPCRs) are the most successful targets in pharma and approximately 40% of approved drugs interact with this family. Among the 800 GPCRs described more than 140 orphan GPCRs are functionally unknown and their endogenous ligands remain unidentified. Prestwick GPCR Drug Library is a collection of 265 approved drugs known to interact primarily with a GPCR. The use of this GPCR library may allow characterization of orphan GPCRs (deorphanization) and facilitate pharmacology research and drug innovation.

Key features

  • A unique collection of 265 small molecules approved drugs (FDA, EMA and other agencies)
  • High degree of chemical and pharmacological diversity
  • A constant quality control ensures high purity and stable compounds – Mean MW: 320

 

Application

  • Deorphanization
  • Repurposing
  • Assay validation

How provided?

  • Pre-dissolved in DMSO ready for screening at precise 10 mM concentration and tailored volumes (100 ┬ÁL to 1 mL) in 96 or 384 well plates, and customizable (volumes, plating)
  • As dry powder in vials starting from 10 mg, with cherry-picking possibility

A database ready for use

  • Always provided with a highly annotated database as structural data file (SDF), IsisBase (DB) as well as an XLS file. Annotation includes target, therapeutic class/effect, side effects, patent and AMDET information
  • A file containing names and structures may be obtained on request prior purchasing
  • Additional amounts of substances: Re-supply of any hit-compound up to 100 mg provided

 

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