Explore the Agenda
8:00 am Check-In & Coffee + Light Breakfast
8:45 am Chair’s Opening Remarks
Establishing Confidence in Novel Biology to Prioritize Targets with the Greatest Therapeutic Potential
9:00 am De-Risking Orphan GPCR Discovery to Transforming Novel Biology into Clinical-Stage Therapeutics
- Establishing confidence in novel GPCR targets through rigorous biological and translational validation
- Overcoming the scientific challenges associated with discovering therapies against receptors with limited historical characterization
- Accelerating progression from target hypothesis to clinical development through an integrated discovery strategy
9:30 am Challenging GPCR Assumptions to Strengthen Confidence in Target Validation & Mechanism of Action
- Investigating how incomplete biological understanding can lead to incorrect conclusions about GPCR target engagement and therapeutic activity
- Applying modern pharmacology tools and experimental approaches to distinguish genuine biology from misleading assay outputs
- Sharing case studies that demonstrate the importance of validating mechanism, target engagement and translational relevance before advancing programs
10:00 am Morning Break & Speed Networking
Join our speed networking session tailored for GPCR professionals, like yourself, to connect with fellow industry peers to facilitate rapid yet meaningful exchanges of insights and expertise. Elevate your networking experience during this session designed for impactful connections within the space.
Characterizing Signaling Complexity to Deliver More Selective & Effective Therapeutics
10:45 am Decoding Compartmentalized GPCR Signaling: How Receptor Location Shapes Drug Responses
- Defining how signaling from the plasma membrane, endosomes and other intracellular compartments drives distinct biological outcomes
- Connecting compartmentalized GPCR signaling to downstream gene regulatory programs, neuronal remodeling and cellular adaptation
- Considering how spatial signaling principles may inform GPCR pharmacology and therapeutic selectivity
11:15 am Presentation Details to be Announced
11:45 am Unraveling GPCR Signaling with Probes & Biosensors: An End-to-End 5-Star Matrix Approach
- Investigating functional selectivity, pathway bias and the molecular mechanisms that govern GPCR activation
- Leveraging advanced probe design and real-time biosensor technologies to measure and characterize receptor signaling events
- Applying the 5-Star Matrix framework to standardize, integrate and streamline GPCR drug discovery across the R&D value chain
12:15 pm Networking Lunch
Advancing Screening Technologies to Unlock Challenging Drug Discovery Opportunities
1:15 pm Navigating the Complexities of GPCRs in DNA-Encoded Library Screening
- Addressing the unique challenges of applying DNA-encoded library screening to dynamic, conformationally complex GPCR targets
- Developing protein reagents and stabilization strategies to generate ligand-free GPCRs in active conformation, suitable for DEL screening
- Advancing DEL binders into functional chemical tools and agonists through iterative screening and orthogonal pharmacological validation
1:45 pm Enabling DNA-Encoded Library Screening Against Challenging Peptide- Binding GPCR Targets
- Integrating reagent generation and tool compounds to establish screening-ready GPCR systems against peptide-binding receptors
- Applying biophysical and biochemical characterization approaches to improve confidence in target quality prior to screening
- Leveraging DEL technologies to identify novel small-molecule starting points against obesity-related GPCR targets
2:15 pm Poster Presentation Session
Take this opportunity to showcase your latest research and innovations with your peers and understand the strategies of your fellow GPCR experts. Visit the website for the full T&Cs of submitting a poster.
2:45 pm Afternoon Break & Networking
Pioneering Next-Generation Therapeutic Modalities to Overcome Traditional Drug Design Limitations
3:15 pm Panel Discussion: Comparing Small Molecules, Peptides & Antibodies to Identify the Optimal Modality for Clinical, Commercial & Patient Success
- Which modality delivers the greatest advantage across efficacy, safety, tissue penetration and durability, and does the answer depend on the target?
- How much should patient-centric considerations such as dosing frequency, convenience and route of administration influence development decisions?
- When evaluating a new GPCR program, how much does modality choice influence commercial differentiation, partnering opportunities and long-term value creation?
3:45 pm Engineering Dual-Target & Multi-Receptor Therapeutics to Achieve Superior Clinical Outcomes
- Enhancing efficacy through simultaneous modulation of complementary pathways
- Overcoming biological limitations associated with traditional single-target approaches
- Unlocking new opportunities through rational polypharmacology and multi-receptor design
4:15 pm From GPCR Biology to the Clinic: Advancing SKM104 MA L2, a Novel GPCR-Targeting ADC
- Applying lessons learned from GPCR-directed ADC discovery programs to refine target selection, antibody engineering and translational strategy
- Overcoming challenges associated with receptor expression, internalization and tumor heterogeneity to unlock additional GPCR opportunities in oncology
- Progressing SKM104 MA L2 through integrated optimization of target biology, antibody properties and payload design