Conference Day One, Wednesday September 3, 2025

7.30 Check-In & Light Breakfast

8:25 am Chair’s Opening Remarks

Reimagining Drug Discovery to Achieve Screening Excellence for Hard-to-Drug Targets

8:30 am Exploring the Cytokinome: Leveraging Fragment-Based Screening for Difficult-to-Drug Targets

Synopsis

  • Taking a combined approach to evaluating different screening techniques for hit identification within the cytokinome
  • Diving into fragment-based screening and its role in supporting the drug discovery process
  • Showcasing how fragment-based screening provides deeper insights into target biology for difficult-to-drug targets

9:00 am Unlocking Hit Discovery of Functional Binders to Target Membrane Proteins

Synopsis

  • Untangling the structural complexity and instability of membrane proteins outside their native membrane environment
  • Enabling the direct incorporation of membrane proteins from cell membranes into stable Salipro nanoparticles
  • Showcasing the latest advancements in hit identification of functional binders using soluble and functional membrane proteins

Refining Library Designs to Unlock Diversity & Precision for Powerful Starting Points

9:30 am Enabling Diversity with Phage Library Screening: Maximizing Hit Rates with Structure-Based Design

  • Gustavo Bezerra Associate Director - Structural Biology, Bicycle Therapeutics plc

Synopsis

  • Incorporating structure-guided approaches into Bicycle molecules design and optimization
  • Focusing on the benefits of using structural biology as a component of phage display campaigns
  • Confirming hits derived from phage libraries through orthogonal assays and structural analyses to verify binding and activity

10:00 am Session Reserved for Vernalis

10.30 Morning Refreshments & Speed Networking

Synopsis

A unique chance to make the most of in-person networking and forge new connections with the rapidly

expanding landscape of biopharmaceutical companies specialized in hit identification and screening. Designed

to maximize your introduction to industry peers that share the same objectives of effectively finding hits for hardto – drug targets.

11:30 am Expanding the Peptide Universe: Chemically Engineering Macrocycles for Next-Gen Hit Discovery

Synopsis

  • Introducing non-natural peptide macrocycles by chemoselective and site-selective modification of natural peptides
  • Diversifying phage-displayed peptide libraries by integrating synthetic structural motifs that exceed natural peptide chemical space
  • Discovering screening innovations enabling multi-cyclized, non-natural peptides to mimic antibody functionality

12:00 pm Transforming Hit Discovery for Biologics: Understanding the Differences Early for Successful Hits

Synopsis

  • Exploring the unique challenges of hit discovery for biologics to engage with specialized libraries and tailored screening methods
  • Prioritizing physiological relevance as critical factors in hit selection for biologics compared to binding affinity
  • Adopting human iPSC-derived, multi-faceted screening strategies that go beyond traditional cell-based assays to establish physiological translation

12.30 Lunch & Networking

1:30 pm Panel Discussion: From Diversity to Novelty – Upgrading Library Designs for High-Throughput Screening

Synopsis

  • Constructing diverse compound libraries with a focus on novel chemotypes for large-scale screening
  • Perfecting our understanding of DELs to expand chemical diversity and coverage of target classes
  • Determining the most appropriate libraries for a given target to maximize hit opportunity

Crafting Robust Assays to Enhance Sensitivity & Accuracy for Reduced False Positives

2:15 pm Highlighting the Limitations of Small Molecule & Genetic Screening for Phenotypic Project

Synopsis

  • Surfacing the weaknesses and blind spots of both small molecule and genetic screening
  • Offering mitigation strategies – when available – to address existing limitations
  • Proposing an evidence-backed framework to determine how to best utilize each approach

2.45 Afternoon Poster Session & Networking

Synopsis

An interactive poster session to showcase your novel work on new modalities, ‘undrugged’ targets, and a combination of hit screening methods to all attendees through informative, data-backed posters.

3:45 pm Innovating Biochemical Assays to Ensure Strong Binding Affinity for Hits with ASMS

Synopsis

  • Executing high-throughput screening for different target types to get label-free compound binding using externalized ASMS
  • Conducting primary screening and validating results for both druggable and challenging targets
  • Assessing compound library size and its impact on binding assay outcomes based on various parameters

4:15 pm Boosting Confidence in Early-Stage Drug Candidates Through Orthogonal Readouts & SAR Analysis

  • Brian Sparling Director & Head, Medicinal Chemistry, Accent Therapeutics

Synopsis

  • Integrating multiple assay platforms to validate hit specificity for targeting DHX9 and KIF18A
  • Adopting a SAR analysis approach for fine-turning compound structure and improving bioactivity
  • Combining assay expertise with deep cancer biology to succeed in hit binding and minimize off-target effects

4:45 pm Chair’s Closing Remarks

5:00 pm End of Conference Day One