Prestwick GPCR Drug Library

GPCR Drug Library by Prestwick Chemical Libraries : a set of approved drugs known to interact with a GPCR

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 or receptors. The human genome alone contains approximately 800 GPCRs making it the largest family of membrane proteins.

Among those GPCRs, more than 140 orphan GPCRs are functionally unknown and their endogenous ligands remain unidentified. The 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.

GPCR Drug Library: A unique and diversified library of drugs, all targeting GPCRs

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


Request an XLS or SD file!


GPCR Drug Library: Multiple applications for various purposes

  • Assay validation with proven pharmacologically active compounds
  • Repurposing/ repositioning: A useful tool for researching new targets of marketed drugs
  • Start of new optimization process
  • Others…to come

GPCR Drug Library: Multi-format suitable for different research modalities

  • In powder form, 10-100mg with cherry-picking options
  • Pre-dissolved at 10mM in DMSO, ready for screening (any volume from 100µL to 1mL)
  • In 96 or 384 well plates (Greiner/ Micronics) or in customers’ plates
  • Optional 2D barcodes offer
  • Customization for volume or mapping
  • Stability in DMSO: 5 years at -20°C
  • Shipping under dry ice conditions
  • Always provided with a highly annotated database as structural data file (SDF), IsisBase (DB) as well as an XLS file
  • Database annotation includes target, therapeutic class/effect, side effects, patent, ADMET information, BBB crossing…
  • Re-supply of any hit-compound guaranteed up to 100 mg



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