2025 Dinner Short Courses* (In-Person Only)

This course focuses on proteolysis targeting chimeras (PROTACs) and will cover topics relevant to developing them as oral therapeutics. The course will include an in-depth look at their physicochemical properties and how these influence solubility and permeability. It will examine ADME topics focusing on in vitro assays for stability, polarity, transporters, drug-drug interactions (DDIs), Cytochrome P450 (CYP450) inhibition, and more. Topics will include looking at what is known about how PROTACs are metabolized in vivo and strategies to deliver them with adequate PK/PD.

This course is designed to provide an overview and best practices in the use of chemical biology probes and assays that have been developed for applications in early drug discovery. Next-generation chemoproteomic technologies such as proximity labeling proteomics (BioID, MicroMap, and MultiMap) and their application to drug discovery will be discussed. Chemists and biologists working in lead generation, assay development, phenotypic screening, target discovery and deconvolution, target engagement and mechanism-of-action (MoA) studies will all benefit from attending this course. The instructors will share their knowledge and expertise around the use of various technologies and chemistries, and there will be time for open discussion and exchange of ideas.

This course offers a comprehensive introduction to DNA-Encoded Library (DEL) screening platforms and their growing role in modern drug discovery. Participants will learn about DEL selection strategies, best practices for identifying novel hits, and key parameters for designing robust and diverse library collections. Special emphasis will be placed on the application of DEL screening across multiple classes of therapeutic targets such as enzymes, protein–protein interactions, and membrane protein and the strategic use of different DEL modalities, in both traditional solution-based DNA-encoded libraries and one-bead-one-compound (OBOC) formats. Attendees will also explore how DEL data can be analyzed and applied to accelerate hit validation and hit-to-lead progression.

With the passing of the FDA Modernization Act 2.0, there is a greater interest in the drug discovery community to develop and use physiologically relevant in vitro models for drug candidate testing and IND filings. This course will help attendees understand what it takes to design and develop relevant 3D organoid/spheroid models through the various stages of assay development, automation compatibility and data analysis. The utility of these models in answering specific biological questions and the importance of developing a robust, scalable 3D model–based assay for preclinical decision-making will also be demonstrated through case studies.

Complex membrane proteins are important therapeutic targets and together represent the majority of protein classes addressed by therapeutic drugs. Significant opportunities exist for targeting complex membrane proteins with antibodies, but it has been challenging to discover therapeutic antibodies against them. This course will examine emerging technologies and strategies for enabling the isolation of specific and functional antibodies against GPCRs, ion channels, and transporters, and highlight progress via case studies.

High-quality recombinant proteins are an essential tool for the successful discovery and development of novel therapeutics. Often these protein targets are difficult to produce with success dependent predominantly on the biological and biochemical properties of an individual protein. For this reason, failures in protein production using more standard traditional bacterial approaches have become prevalent. This course will focus on both the insect and mammalian expression systems, which have demonstrated the ability to express complex proteins for a wide variety of applications. We will discuss the concepts, uses, and optimization of these systems along with sharing experimental troubleshooting lessons learned. The course combines instruction and case studies in an interactive environment.

This course aims to introduce the fundamentals of Fragment-Based Lead Discovery (FBLD) to attendees. The first section will focus on the concepts of using fragments for hit generation. Special emphasis will be placed on practical pitfalls and the many ways to advance fragments to leads and drugs. The second part of the course will discuss the variety of fragment screening methods and when they are best applied. The composition of fragment libraries will also be discussed in detail. The attendees should come away from this course with a solid understanding of what FBLD is and how to apply it.

This short course will review biophysical methodologies used to investigate the structure–function relationships of G protein-coupled receptors (GPCRs). Through selected examples, we will highlight how these techniques contribute to GPCR structure determination and support drug discovery efforts. Topics will focus on nuclear magnetic resonance (solution and solid-state) and also include surface plasmon resonance (SPR).

This course will provide an overview of ASMS as a biophysical assay technique. The focus will be on the main applications of ASMS: (1) for highthroughput screening and (2) ASMS for compound binding studies. Case studies will be presented as well.

Conjugated modalities such as antibody-drug conjugates (ADCs), oligonucleotide conjugates, and peptide-drug conjugates are revolutionizing precision medicine. However, their success relies on smart linker strategies that ensure stability, controlled payload release, and manufacturability. This intensive 2-hour course will explore the latest innovations in linker chemistry, site-specific conjugation, formulation and delivery considerations, and scalable manufacturing approaches. Participants will gain practical insights into optimizing linker design for enhanced efficacy, reduced toxicity, and regulatory compliance.

Deep generative modeling is rapidly transforming de novo drug discovery and streamlining the entire process. This artificial intelligence (AI) Toolkit course explores how the Three Waves of AI—from predictive AI to generative AI and the emerging era of Agentic AI—are transforming pharmaceutical innovation. Participants will learn how AI and machine learning (ML) are re-shaping molecular design, enabling the creation of novel compounds with precision-tailored properties. The course delves into the fundamentals of Large Language Models (LLMs), foundational models, and autonomous AI systems, highlighting their potential role in re-inventing the pharmaceutical landscape. Along the way, we'll dissect three pivotal techniques for biopharma-specific LLMs: prompt engineering, retrieval augmented generation (RAG), and fine-tuning. This course is designed for medicinal chemists, molecular modelers, and project managers seeking to harness the capabilities of modern Generative AI concepts and integrate them into their work.

Characterizing and understanding the interactions of potential therapeutic agents with their targets is fundamental to drug discovery. After first reviewing the fundamentals of pharmacology, we will conduct an in-depth exploration of pharmacology assays and screening funnels as they apply to the validation of hits and their optimization into clinical candidates. A key aim will be to distill important, but often poorly known, pharmacology and screening information in a concise format. This course will surface pitfalls and offer mitigations strategies on a range of relevant topics with a goal of providing practical information to help prosecute drug discovery projects more effectively from project inception all the way to clinical trials.