8:00 am Registration & Morning Networking Coffee

8:50 am Chair’s Opening Remarks

Deconvoluting Human Genetics to Understand Untapped GPCR Families & Expose the Relevance of GPCRs in Previously Unidentified Disease Indications

9:00 am Human Genetics-SAR: A Novel Approach to Decipher the Biology & Therapeutic Potential of Human GPCRs


  • How to approach the large-scale multiparametric profiling of naturally occurring human GPCR missense variations
  • How to leverage the power of human genetics by linking the molecular, cellular, and clinical consequences of rare GPCR missense variations to accelerate the discovery of disease relevant pathways

9:30 am Examining Commercial & Investor Perspectives to Fulfil the Future Opportunities of Next-Generation GPCRs


  •  What is investible when considering the GPCR landscape?
  • What do investors look for when investing in GPCR pipelines?
  • How to secure interest from collaboration partners?
  • What is the scope for other types of funding partners?

10:30 am Morning Break & Speed Networking


Our speed networking is the ideal opportunity to get face-to-face time with many of the brightest minds working in the field & introduce yourself to the attendees that you would like to have more in-depth conversations with. Benchmark against industry leaders & establish meaningful business relationships to pursue for the rest of the conference & beyond.

TRACK A: Target ID & Validation

Reinvigorating Biophysical Assays with Dynamic Confirmation Insights to Improve Candidate Selection

11:30 am Fireside Chat: Overcoming Diversity in Therapeutic Outcomes by Elevating Bias Signaling


  • How to leverage bias in candidate selection? How to identify the best signalling profile, and correlate cell signalling with efficacy?
  • What are the methods for revealing signaling bias for different G proteins? Understanding the preferential activation and recruitment of G protein and beta-arresting, respectively
  • Can we design biased ligands rationally? 
  • How to leverage AI to interpret data and inform drug design?

12:00 pm Chemogenetic Activation of Specific GPCR Signaling Pathways to Identify Novel Targets for Antidiabetic Drugs

  • Jurgen Wess Section Chief of Molecular Signaling Section, National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)


  • Leveraging designer GPCRs known as DREADDs (Designer Receptors Exclusively Activated by a Designer Drug) to selectively activate distinct classes of heterotrimeric G proteins
  • Using DREADDs to identify novel cellular targets for the treatment of major metabolic disorders
  • Optimizing DREADD technology to identify distinct GPCR signaling pathways involved in type 2 diabetes and obesity in vivo

TRACK B: Hit ID & Optimization

Pioneering Rational GPCR Drug Discovery with Structure-Based Design

11:30 am Pros & Cons of Positive Allosteric Modulation in GPCR Drug Discovery – Case Studies from Lilly Research Labs


  • Discussing the attributes of a target that make allosteric modulation a desirable MOA for drug discovery
  • Importance of profiling and understanding the key parameters of allosteric modulation (affinity, alpha, and beta) and their impact on target product profile
  • Emerging importance of GPCR structural biology in the design and optimization of allosteric modulators

12:00 pm Enabling Structure-Based Drug Discovery on GPCRs


  • Protein engineering strategies for enhancement of expression and stability
  • Biophysical methods to characterize small-molecule ligand binding
  • Selecting EM and/or X-ray for structure research to investigate ligand interaction
  • Time resolved X-ray crystallography to investigate receptor dynamics

12:30 pm Networking Lunch Break

Reinvigorating Biophysical assays with Dynamic Confirmation Insights to Improve Candidate Selection

1:30 pm Understanding the Role of GPCRs in the Tumor Microenvironment: Identification & Validation of Novel Immuno-oncology Targets


  • Identifying immunosuppressive GPCRs in the TME
  • Further validation of immuno-oncology targets ex vivo and in vivo
  • Illustration of Domain’s R&D efforts and GPCR pipeline 

2:00 pm Adopting NMR Spectroscopy to Address the Dynamic Aspects of Receptor-Drug Complexes

  • Joshua Ziarek Associate Professor of Pharmacology, Northwestern University


  • How is NMR spectroscopy addressing conformational and dynamic changes?
  • What data packages are associated with NMR and how are these analyzed?
  • Uncovering kinetics of the GPCR landscape and how these motions govern receptor activation? 

Streamlining Hit ID & Optimization with Advanced Screen Platforms to Accelerate Lead Generation

1:30 pm The Salipro® Platform Enables Discovery of Novel Therapeutics Against GPCRs


  • How to reconstitute wildtype GPCRs into Salipro® nanomembrane particles
  • DEL screening using purified wildtype GPCRs
  • Hit verification using SPR and CryoEM

2:00 pm Assay Development & High-Throughput Screening of the pH-Activated GPR65 & GPR68 Receptors

  • Laurent Meeus Chief Scientist & Business Unit Director, EuroscreenFast


  • • Development of recombinant cell lines expressing the pHactivated GPR65 and GPR68 receptors
  • Validation of cAMP and IPOne HTRF functional assays for GPR65 and GPR68 receptors for HT
  • HTS of a 260k compounds library for antagonist activity at the GPR65 and GPR68 receptors, and identification of validated hits

2:10 pm Advancing the Optimization of Lead Biologic Candidates using New Screening Platforms


  • What is the workflow to screening for highly specific biologics
  • How to enhance binding affinity of anti-GPCR antibodies with chemical optimization?
  • How to exploit the druggability of antibodies to target previously undrugged GPCRs?

2:30 pm Afternoon Networking Break

Addressing Complex Unknowns to Unlock Previously Undrugged Targets & Finally Spearhead the Revolution of GPCR Deorphanization

3:30 pm Roundtable Discussion: Leading Deorphanization with the Identification of Endogenous Ligands as a Compound to Advance Rationale Drug Development


  • How to validate proposed true orphan GPCR-ligand pairs and with what suite of assays?
  • What are the emerging methods for accomplishing deorphanization? Structural characterization, Mass spec etc  
  • How to reveal the therapeutically relevant signaling pathways activated by orphan GPCRs?  

4:00 pm Leveraging Structure Based Insights to Inform Novel Roles for Orphan GPCRs & Lead Cognate Ligand Identification


  • How to structural characterize orphan GPCRs using AlphaFold2?
  • How to use structural insights to inform the development of orphan GPCR ligands?
  • How to elucidate novel mechanisms with these insights?

4:30 pm Validation of GPR65 as a Novel Immuno-oncology Target using Advanced In Vitro & In Vivo Models


  • Identification of GPR65 as a novel immuno-oncology target as well as potent GPR65 inhibitors
  • Provide additional validation using primary tumorhistocultures and genetically engineered mice
  • Advancing biomarker development to accelerate clinical development

5:00 pm Chair Closing Remarks & End of Conference Day One