Conference Day One

7:30 am Registration & Coffee

8:15 am Chairman’s Opening Remarks

Discovery Day: Building Cutting Edge Tools, Uncovering New Targets & Assessing the Feasibility of Candidates to Build the Next Generation of Kinase Drugs

Assay Development, Kinome Exploration & Kinase-Focussed Drug Discovery Principles

8:30 am Voruciclib, a CDK9 inhibitor, Downregulates MYC and MCL1 and Inhibits Proliferation in Heme and Solid Tumor Models

  • Sandra Wiley Director of Translational Sciences, MEI Pharma


  • Targeting transcription and phosphorylation-mediated protein degradation as an indirect mechanism to downregulate MYC and MCL1
  • Voruciclib synergizes with KRAS G12C and BCL2 inhibitors in preclinical solid tumor and heme malignancy models
  • Voruciclib, in combination with venetoclax, is under clinical investigation in AML

9:00 am Drug Screening with the Gold-standard Assay Against the Largest Kinome Available Reveals Unexpected Drug-Enzyme Relationships


  • Mono-specificity is difficult to achieve and rarer than advertised
  • WT versus mutant and phosphorylation status matter greatly
  • Multiple assays are required for a complete pre-clinical assessment

9:30 am Understanding the Global Atlas of Motifs for the Human Protein Kinome


  • Experimental profiling of kinases
  • Computational application and evaluation of performance
  • Illumination of MS phosphoproteomics data

10:00 am Morning Refreshments & Speed Networking

11:00 am Discovery and Validation of Biomarkers for Patient Stratification


  • Identification of predictive drug response biomarkers by Oncolines® cancer cell panel profiling
  • Comparative profiling of small molecule oncology drugs to identify biochemical mechanism of action
  • Validation of drug response biomarkers in disease models and in proof-of concept clinical studies

11:15 am [VIRTUAL] Automated High-Throughput Analysis of Non-Equilibrium Inhibition In Kinase Inhibitor Discovery


  • Discovering kinase inhibitors with non-equilibrium modalities to increase the residence time and possible decoupling of pharmacokinetics and pharmacodynamics.
  • High-throughput analysis of kinetic data for slow-onset inhibitors
  • High-throughput analysis of kinetic kinact/KI data for irreversible inhibitors

11:45 am Exposing Novel Kinase Polypharmacology and Drug Escape Mechanisms in Cells With NanoBRET

  • Jim Vasta Senior Scientist - Target Engagement Research, Promega Corporation


  • Enabling live cell kinase profiling: Exploring the landscape of DDR kinase inhibitors in cells
  • Kinome-wide live cell profiling reveals novel interactions for type II kinase inhibitors
  • Protomer selectivity of RAF dimer inhibitors informs on the mechanism of inhibition within the RAS-RAF signalosome

12:15 pm Enzymatic Assays for Kinase Inhibitor Discovery


  • Enzymatic assays drive kinase inhibitor discovery programs
  • Multiple assay formats and readouts are available, but some have distinct advantages
  • Mass spectrometry is an underutilized tool for kinase inhibitor assays, but has great potential

12:45 pm Lunch Break

1:45 pm Building Ultralarge Next Generation Libraries for the Discovery of Novel and Selective Kinase Inhibitors


  • Novel libraries to expand the searchable chemical space for kinases
  • Specific challenges of kinase inhibitors for brain penetration and selectivity and the importance of multiparameter optimization
  • Robotic synthesis and automation of assays to support AI drug discovery

2:15 pm Monitoring Continuous Enzyme Activity with Fluorogenic Sensor Assays Enables Data-Rich Decisions for Improved Kinase & Phosphatase Drug Discovery


  • Advantages of PhosphoSens® technology as a continuous activity assay (a progress curve in every well)
  • Kinome selectivity profiling at low or high ATP with insight into compound dependent kinetics and MOA
  • Deep characterization of kinase inhibitor potency for reversible or irreversible inhibitors

2:45 pm The Future is Here: Automation Demonstrates its Value as a Precision Tool for Accelerating Drug Discovery


  • Robotics-enabled process for inhibitor profiling, providing an unparalleled depth of data capture, going beyond the current state-of-the-art of biochemical assay setup
  • 9 orders of magnitude range in liquid volume handling and contact-free digital dispensing for true, non-serial, independent experimentation enabling experiments to be designed exclusively for each molecule
  • Differentiated triage strategies enable data utilization to support machine learning and more traditional hit discovery activities for program progression – no more single-shot screening!

3:15 pm Afternoon Break & Poster Session

Inhibitor or PROTAC – Overcoming Tumor Resistance & Improving Durability

4:00 pm [VIRTUAL] Degradation Is Not Always Superior to Enzymatic Inhibition: Lessons Learned from EGFR Heterobifunctional Degraders


  • Targeted degradation of EGFR failed to suppress resistance common to EGFR targeted therapies
  • Degradation resulted in decreased efficacy relative to non-degrader controls
  • Comparing degrader vs non-degrader controls highlighted an unexpected role for ER stress contributing to the efficacy of canonical EGFR targeted therapies

4:30 pm Full Audience Activity – Roundtable Discussion

  • Sandra Wiley Director of Translational Sciences, MEI Pharma


At your table discuss the following questions:

  • What are the 3 most important factors to consider when selecting your modality of choice?
  • In your mind, what are the central pros of a PROTAC degrader vs a traditional inhibitor?
  • What feature would you prioritize as your ‘dealbreaker’ when making a final decision regarding modality?

5:00 pm Chairman’s Closing Remarks

5:15 pm End of Conference Day 1

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