product
DiscoverX GPCRscan® GPCR Profiling Services
22 February 2016 | By DiscoverX Corporation
GPCRscan is a functional cell-based GPCR assay panel for profiling drug compounds during drug discovery...
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GPCRs
news
Heptares and Pfizer to focus on GPCR targets
30 November 2015 | By Victoria White
Heptares and Pfizer have announced they are to research and develop potential new medicines directed at up to 10 G protein-coupled receptor (GPCR) targets across multiple therapeutic areas...
article
Exploiting functional selectivity of GPCRs in drug development
The large family of pharmaceutical targets represented by G-protein coupled receptors (GPCRs) are usually involved in a number of intracellular effector pathways, leading to many cellular outcomes. In recent years it has been uncovered that different ligands of a given GPCR may engage the pathways selectively, in that ligands that…
webinar
Biased ligands in Drug Discovery – the case of TRV027
30 June 2015 | By Cisbio Bioassays & Trevena, Inc.
TRV027 is a biased ligand; the in vitro profile and its translation into in vivo pharmacology is discussed during this webinar.
article
Building GPCR screening cascades for lead generation
Although this target class is already heavily investigated, there are still a significant number of opportunities for discovery of novel drugs targeting additional GPCRs. In this review, scientists from AstraZeneca R&D discuss the general build-up of GPCR screening cascades for discovery of chemical leads that can be further developed into…
article
Nuclear Magnetic Resonance as a tool for chemokine inhibitor discovery
Chemokines orchestrate leukocyte trafficking in the immune system, but unregulated or inappropriate chemokine activity plays a key role in many inflammatory, allergic and autoimmune diseases as well as metastatic tumour progression. The chemokine network is comprised of ~50 distinct ligands that specifically bind and activate a family of 20 G…
