GPCR Technology – Overview
G protein coupled receptors (GPCRs) are the largest, most druggable target class and are popular and effective therapeutic targets for treatment of inflammation, pain, neurological disorders, diabetes and cancer.
DiscoveRx® offers the largest collection of validated functional GPCR assays for screening and profiling. Our industry leading panel of over 400 naturally coupled cell lines are designed to detect GPCR signaling for both known and orphan GPCRs based on
second messenger signaling,
arrestin binding, and
receptor internalization. All assays utilize the same homogeneous, chemiluminescent read-out based on β-galactosidase enzyme fragment complementation (EFC) to confer universality and flexibility for identification of lead candidates in agonist, antagonist, inverse agonist, or allosteric modes.
Revolutionary GPCR Profiling Panel
| Feature |
Available Assays
|
| Unique receptors (known GPCRs) |
200 |
| Arrestin recruitment |
178 |
| 2nd messenger detection (cAMP / Calcium) |
131 |
| Internalization |
78 |
| Receptors in more than 1 mode |
135 |
| Receptors in all 3 modes |
40 |
| Orphan receptors |
76 |
| Non-Human ortholog receptors |
71 |
Therapeutic panels
metabolic, cancer, cardiovascular, digestive/renal, inflammation, neurological, psychiatric, reproductive, respiratory, sensory |
10 |
Technology Platforms
Our leading PathHunter® β-Arrestin technology is a direct, universal platform for measuring compound action independent of G protein signaling through β-Arrestin recruitment to the GPCR.
We also offer second messenger detection of cAMP and calcium mobilization in naturally coupled systems.
The new PathHunter® GPCR internalization platform provides a convenient, cost effective, highly quantifiable and easy to automate platform for determining receptor recycling and kinetics.