CONFERENCE DAY ONE
Wednesday, December 11, 2024
8:00 am Check-In & Light Breakfast
8:50 am Chair’s Opening Remarks
Streamlining Hit Generation with High-Throughput & Unbiased Covalent Screens to Define Innovative Warheads for Hard-to-Drug Targets
9:00 am Covalency Offers Unique Opportunities for Difficult Targets
Synopsis
- Covalency provides opportunities for difficult drug targets
- Screening identifies a starting point for a TF target
- Proteomics is an essential tool for covalency focused efforts
9:30 am Mass Spectrometry Screening & Hit Optimization Strategies for Efficient Covalent Drug Discovery
Synopsis
- Maximizing throughput for MS-based covalent screens
- Integrating data generated from MS screens to identify potent and selective hit compounds
- Triaging hits to identify the most tractable compounds
10:00 am Panel Discussion: Debating Systematic & Scalable Screening Methods to Rationally Discover & Develop Covalent Handles with Optimized Reactivity & Selectivity
Synopsis
- Debating the pros and cons of target-agnostic and target-focused screening to identify the best use cases
- What are the best methods for finding tractable hits?
- Discussing how to balance reactivity with sensitivity within screening cascades
- Streamlining hit to lead by sifting through hits and appropriately triaging
11:00 am Morning Break & Speed Networking
Synopsis
Our speed networking session is the ideal opportunity to get face-to-face time with many of the brightest minds working to discover and develop covalent modalities. Introduce yourself to the attendees that you would like to have more in-depth conversations with, benchmark against industry leaders, and establish meaningful business relationships that you can pursue for the rest of the conference and beyond
Accelerating the Development of Unbiased & Scalable Platforms to Access & De-Risk Novel Chemistry Amenable for Covalency & Propel Discovery Pipelines
12:00 pm Practical Approaches to Accelerate Covalent Drug Discovery
Synopsis
- Exploring early profiling and selection of actionable targets
- Assessing hits to predict target traceability
- Enabling biochemical and chemoproteomics assays to build programs
12:30 pm Mechanistic Study of Reversible & Irreversible Covalent Inhibitors
Synopsis
- The emergence of reversible covalency addresses off-target safety concerns, countering challenges posed by irreversible covalent inhibitors. Yet, characterization of this novel mechanism is hindered by limited assays and tools
- Establishing enzyme kinetic assays, incorporating slow binding Ki Kinact measurement and jump dilution to enable the determination and differentiation of reversible from irreversible covalency mechanism
1:00 pm Session Reserved for WuXi AppTec
1:30 pm Lunch Break & Networking
Spearheading the Specific Covalent Targeting of More Abundant Residues Beyond Cysteine to Access Novel Binding Pockets & Expand the Druggable Proteome
2:30 pm Specific Covalent Targeting of Histidine, Tyrosine & Lysine to Expand the Druggable Proteome
Synopsis
- Development of novel warheads for covalent screening of histidine, tyrosine and lysine residues
- Enhancing the capture and mass spectrometry detection of sensitive peptide-ligand pairs
- Integration of structural information to prioritize novel binding pockets for further development of covalent or non-covalent compounds
3:00 pm Targeting of Histidine Residues to Increase the Pool of Potential Targets Amendable for Covalent Drug Discovery
Synopsis
- Showcasing how to identify and map histidine residues across a wide range of proteins to determine their potential as covalent drug targets
- How to marry the right electrophiles with histidine moieties
- Ligand-first versus electrophile-first approaches to target Histidine residues
3:30 pm Afternoon Networking Break
Advancing Chemoproteomic Platforms & Probes to Better Interrogate Novel Biology & Amplify the Druggable Proteome Outside Oncology
4:00 pm Towards a Chemical Biology Platform for the Systematic Discovery & Evaluation of Novel Covalent Chemistry
Synopsis
- Exploring insights into flexible library setup to synthesis novel covalent warhead libraries
- Showcasing MS and proteomics-based discovery and profiling assays for novel covalent warhead motifs
- Examining setups to screen and profile novel covalent libraries
4:30 pm Roundtable Discussion: Fueling the Covalency Renaissance by Strategizing the Chemistry Toolbox to Target Residues Beyond Cysteine with Orthogonal Reactivity
Synopsis
- Which amino acids are seen as the next frontier in covalent drug discovery?
- What is the mass spectrometry or alternative screening toolbox for other amino acids?
- How can we build drug-like warheads that hit other sidechains? Should we be screening these more promiscuous warheads?
- What are the different methods to validate non-cysteine covalency in simplified systems?
5:00 pm Covalent Fragment-Based Ligand Discovery to Drug Refractory Targets
Synopsis
- How can covalent fragment-based ligand discovery be leveraged to tackle so-called undruggable targets?
- What are the advantages of a target-centric approach to covalent fragment-based ligand discovery?
- What approaches (biochemical and cell-based) can be deployed to progress covalent fragment starting points to mature lead molecules within a drug discovery campaign?
5:30 pm Chairs Closing Remarks
5:35 pm End of Conference Day One
ACCESS THE FULL PROGRAM
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