Sunday
2:00 pm - 9:00 pm
Arrival and Check-in
6:00 pm - 7:00 pm
Dinner
7:30 pm - 7:40 pm
Introductory Comments by GRC Site Staff / Welcome from the GRC Chair
7:40 pm - 9:30 pm
Novel Strategies Targeting Immunotherapies
7:40 pm - 8:10 pm
"The Identification and Development of Monocyte-Specific NLRP3 Inhibitors"
8:10 pm - 8:20 pm
Discussion
8:20 pm - 8:50 pm
"Design of a Myeloid-Targeted BET-Bromodomain Inhibitor"
8:50 pm - 8:55 pm
Discussion
8:55 pm - 9:25 pm
"Discovery of AZD0011, an Orally Bioavailable Arginase Inhibitor that Reactivates T-Cell Anti-Tumor Response"
9:25 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Small Molecule Antivirals for the COVID-19 Pandemic and Beyond
9:00 am - 9:30 am
"Optimization of Oral and Inhaled Drug Combinations to Treat and Prevent CoV-2 Infections with Protease and Polymerase Inhibitors"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"New Remdesivir Formulations for Early Treatment of Respiratory Viral Infections"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Emvododstat (PTC299) Mechanism of Action Offers Versatility Across Therapeutic Areas, from AML to COVID-19"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Design of a SARS-CoV-2 Main Protease Inhibitor Administered Orally for the Treatment of COVID-19"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Rare and Tropical Disease Therapeutics
7:30 pm - 8:00 pm
"Optimization of N-Heteroaryl Indazole LRRK2 Inhibitors for CNS Drug Discovery"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"Substrate Reduction Therapy with Thienopyridines for the Treatment of Metachromatic Leukodystrophy"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Next Generation Oxazolidinone Antibiotics for the Treatment of Tuberculosis"
9:20 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
Group Photo
9:00 am - 12:30 pm
Driving Drug Discovery with Synthetic Methods and Technologies
Designed by Danica Rankic (Pfizer, USA)
9:00 am - 9:30 am
"High-Throughput PROTAC Synthesis for Direct, Biological Assaying"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Advancing Chemical Biology and Drug Discovery Through Innovative Chemistry"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Synthesis and Functionalization of Cyclopropanes and Cyclobutanes"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Synthetic Macrocyclic Peptides that Target Protein-Protein Interactions: The Discovery and Early Development of a PCSK9 Inhibitor"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Harnessing the Potential of Ubiquitin Ligases: Targets and Effectors for Protein Degradation
7:30 pm - 8:00 pm
"Discovery and Characterization of IRAKIMiDs: Degraders Targeting Both IRAK4 and IMiD Substrates for Oncology Indications"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"Orally Available ER-Targeting PROTACs with In Vivo Activity: Conception, Cascade, Construction and Conformational Understanding"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Discovery and Evaluation of Small-Molecule Inhibitors of the E3 Ligase Casitas B-Lineage Lymphoma B (CBL-B)"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Novel Pain and Addiction Therapeutics to Combat the Opioid Crisis
9:00 am - 9:30 am
"NIDA's Efforts to Combat the Opioid Crisis"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Design and Evaluation of Naltrexone Prodrugs as Long-Acting Injectables for Treating Addiction"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Medicinal Chemistry Navigates the Crossroads for Nociceptin Opioid Receptor GPCR-Targeted Small-Molecules for Treating the Dual Opioid Crisis of Pain and Addiction"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Discovery of Allosteric NTRK1 Inhibitors for the Treatment of Pain"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
How Cryo-EM Structures Are Enabling Drug Discovery
7:30 pm - 8:00 pm
"Progress and Prospects for CryoEM in Structural Biology"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"Application of Cryo-EM for Structure-Based Design Against Membrane Protein Targets for Inflammation and Metabolic Disease"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Structure-Based Design of a Novel Series of NaV1.7 Inhibitors Using Cryo-Electron Microscopy"
9:20 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
Business Meeting
Nominations for the Next Vice Chair; Fill in Conference Evaluation Forms; Discuss Future Site and Scheduling Preferences; Election of the Next Vice Chair
9:00 am - 12:30 pm
Late-Breaking Topics: First Disclosures of Clinical Candidates
9:00 am - 9:30 am
"Discovery of Inupadenant, a Novel A2A Receptor Antagonist that Retains Activity in Adenosine-Rich Microenvironments"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"The Discovery of CK-136, a Selective Cardiac Troponin Activator"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Discovery and Early Clinical Development of LY3372689, an O-GlcNAcase (OGA) Enzyme Inhibitor"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Discovery of GS-4875: A First in Class TPL2 Kinase Inhibitor for Inflammatory Diseases and Beyond"
12:15 pm - 12:30 pm
Discussion
12:30 pm - 1:30 pm
Lunch
1:30 pm - 4:00 pm
Free Time
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Keynote Session: From Targeted Small Molecules to Targeted Cell Therapies
7:30 pm - 8:30 pm
"From Targeted Small Molecules to Targeted Cell Therapies"
8:30 pm - 8:55 pm
Discussion
8:55 pm - 9:15 pm
General Discussion
9:15 pm - 9:30 pm
Closing Remarks
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure