Pre-Conference Day

As covalent programs mature, early warhead design decisions increasingly determine whether compounds progress or stall during translation. This workshop will examine how chemistry choices interact with PK/PD behavior, developability constraints and translational expectations, helping teams design warheads that remain viable through optimization and into IND enabling studies.

This session will address:

• Exploring non-acrylamide chemotypes and beyond to evaluate how alternative warhead chemistries electrophiles, alongside electrophile choice, placement, and scaffold context drive covalent engagement and selectivity

• Leveraging chemoproteomics and cellular covalent screening to profile target engagement and proteome-wide reactivity, enabling data-driven optimization and prioritization of warhead strategies

• Learning from real-world case studies, including deprioritized programs to uncover key pitfalls, unexpected liabilities, and transferable insights that improve decision making and reduce late-stage risk

Covalent development generates complex kinetic and selectivity data that are often difficult to reconcile across assays and systems. This workshop will focus on how kinact/KI, target engagement and selectivity readouts can be integrated to build translational readiness, supporting clearer alignment between discovery data, PK/PD strategy and downstream development planning.

This session will address:

• Assessing how kinetic, selectivity and target engagement data can be integrated across biochemical and cellular systems to build a consistent view of covalent behavior

• Comparing approaches to generating and contextualizing kinact/KI measurements, including their applicability and limitations across enzyme and non‑enzyme targets

• Linking kinetic and selectivity profiles with early safety and PK/PD considerations to support translational planning and downstream development strategy