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Webinar: Hit Discovery for GPCRs: HTS or Virtual Screens?

Explore this on-demand webinar "Hit Discovery for GPCRs: HTS or Virtual Screens?” presented by Carleton Sage, PhD, Vice President of Computational Sciences at Beacon Discovery/Eurofins.


Survey of expression of GPR174 in primary cells compared to that observed in immortalized cell lines.

G protein-coupled receptors (GPCRs) constitute the largest class of transmembrane proteins in the human genome and play important roles in disease pathogenesis, and therefore are one of the largest classes of drug targets including blockbuster drugs such as Cimetidine, Olanzapine, and Clopidogrel. Over 100 GPCRs in the human genome are classified as orphans: receptors whose endogenous ligands and biological function remain unknown, thus these targets represent promising, yet challenging targets for drug discovery.

In this webinar, Dr. Sage will present examples of diverse and complementary approaches to hit discovery performed in two ongoing drug discovery projects: he will discuss both the HTS campaign for the orphan receptor GPCR174 including target rationale, assay development requirements and challenges, hit identification and hit confirmation and validation.

In addition, we will address how we approached the Serotonin 2B receptor, discussing the target selection rationale, a massive virtual screening approach including validation of docking approaches as well as shape and chemical features for hit identification, assay development for hit validation, and early lead series identification.


Superposition of 5HT2B crystal structures demonstrating variation in ligand binding.

Original Broadcast Date: June 24, 2021

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