Explore the Agenda
8:00 am Check In & Light Breakfast
8:50 am Chair’s Opening Remarks
Revolutionizing Target Discovery & Screening With Insights From High Throughput
Chemoproteomics Platforms to Expand the Druggable Proteome
9:00 am Leveraging the Unique Power of Chemoproteomics for Hit Identification & Screening to Transform Discovery of Therapeutic Candidates
- Explore the Frontier Platform which combines chemoproteomics, covalent fragment-based discovery, and AI to access more than 90% of the proteome
- Discover how a custom-built covalent fragment library that leverages the concept of enantiomer pairs was used to reveal immediate SAR through enantiomer-specific hits, enabled by chemoproteomic screening in live cells capturing proteome-wide engagement signatures
- Presenting novel quality-control metrics for large-scale chemoproteomic screening of covalent enantiomer libraries, complementing compound purity checks and improving triage of true hits for downstream assays
9:30 am Pocket Finding & Ligand Discovery by Chemoproteomics for Covalent Drug Discovery
- Outlining how combining fully functionalized libraries, automated protein-level enrichment, and DIA-MS provides a robust high-throughput chemoproteomic platform for proteome-wide screening of libraries
- Discover how protein level data provides convincing information for the presence of ligandable sites
- Discuss how the data informs about preferred chemotypes of electrophilic warheads for covalent drug design
10:00 am Adopting Chemoproteomics Platforms to Inform Target Discovery & Drug Previously Undruggable Targets
- Developing a robust, high-throughput chemoproteomics platform to identify novel binding pockets, facilitate efficient target discovery, and drug orphan receptors
- Characterizing ligandable sites and binding pockets to unlock a plethora of novel target sites for hard-to-drug proteins
- Discussing data showing the unique benefit of applying chemoproteomics to transform target discovery and maximize time and cost-efficiency of R&D
10:30 am Chemoproteomics-Based Discovery of CNS-Penetrant Covalent Inhibitors
- Development of a robust live cell chemoproteomics screening platform for covalent hit discovery
- Rapid MS-based proteomics led optimization of covalent screening hits to a brain-penetrant covalent inhibitor of a high-value CNS target
- Highlighting the advantages of developing covalent inhibitors for long-lived protein targets in the brain, while minimizing peripheral target occupancy
11:00 am Morning Break & Networking
Illuminating Post-Translational Modifications With Proteomics to Understand Disease
Mechanisms & Inform Therapeutic Strategy
11:45 am Quantitative Post-Translational Modifications (PTM) Omics to Support Drug Discovery
- Discussing optimized experimental PTM enrichment workflows for increased sensitivity and robustness
- Benchmarking novel mass spectrometers and proteomic data processing tools for enhanced coverage of the PTM-ome
- Sharing examples for the application of PTM data to guide decision-making in different stages of the drug discovery process
12:15 pm Round Table Discussion: Unlocking Greater Understanding of the Proteome Through Accurate Analysis of Post-Translational Modifications
- Capturing rare PTMs including tyrosine phosphorylation, glycosylation, and ubiquitination
- Overcoming limitations of instrument sensitivity to detect PTMs from limited samples and draw meaningful biomedical conclusions
- Evaluating the importance and feasibility of analyzing PTMs and selecting the appropriate instruments and workflows to do so
1:00 pm Lunch Break & Networking
Defining Gold-Standard Data Analysis Methodologies & Utilizing AI Capabilities to Generate
Unique Biomedical Insights From Large Proteomics Data Sets
2:00 pm Panel Discussion: Establishing a Consensus on Proteomics Methodologies & Data Sharing to Enable Reproducible Analysis & Reliable Interpretation of Data
- Defining robust, standardized proteomics methodologies, from sample collection and analysis to statistical protocols and generation of biomedical conclusions
- Developing a collaborative database to facilitate secure data visualization and sharing, maximizing the impact of available data
- Establishing collaborative projects amongst consortiums, academia, and industry to utilize existing datasets and generate a deeper understanding of proteomics to direct therapeutic development
2:45 pm Acrivon’s Generative Phosphoproteomics AP3 Platform Accelerates Pathway-Based Drug Design & Enables Rapid Clinical Translation
- Discuss the development of a computational pipeline and supporting infrastructure to analyze large-scale phosphoproteomics datasets and systematically characterize drug-regulated signaling network dynamics
- Applying a proprietary generative AI model to predict kinase–substrate relationships, enabling deeper pathway interrogation
- Utilizing these approaches to define differentiated AP3 drug response profiles and facilitate the identification of predictive biomarkers to support patient stratification and translational applications