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
7:40 pm - 8:05 pm
"Inhaled Janus Kinase 1 (JAK1) Inhibitors for Asthma"
8:05 pm - 8:15 pm
Discussion
8:15 pm - 8:40 pm
"'Super-Soft' Selective Glucocorticoid Receptor Agonist (SEGRA-ss) for Dermatology"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:15 pm
"HIV Nucleoside Reverse Transcriptase Translocation Inhibitors (NRTTIs) for Extended Duration Dosing"
9:15 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Immuno-Modulation for the Treatment of Cancer: Recent Medicinal Chemistry Advances
9:00 am - 9:30 am
"Selective Inhibition of Tryptophan-2,3-Dioxygenase (TDO)"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Novel Adenosine 2A Receptor Antagonist AZD4635: From the Brain to the Tumor Microenvironment"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Preventing Treg Trafficking into the Tumor Microenvironment: Discovery of Potent and Selective CCR4 Antagonists"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Synthetic and Medicinal Chemistry Approaches to Novel STING Agonists with Robust Antitumor Activity"
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
New Paradigms in SBDD: Understanding Ligand Conformation to Aid Molecular Design
7:30 pm - 8:00 pm
"Use of NMR-Guided Conformational Design for the Identification of a Novel, Selective Orexin-1 Antagonist Series Yielding a Clinical Candidate"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"The Role of Solution Conformation in Structure-Guided Fragment Optimization"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Free Ligand NMR Signatures to Drive SAR and Enhance Structure Based Drug Design"
9:20 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Hijacking the Ubiquitin Proteasome System: Recent Progress in the Development of Targeted Protein Degraders
9:00 am - 9:30 am
"Advances in the Medicinal Chemistry of Targeted Protein Degradation"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Molecular Recognition of Ternary Complexes: A New Dimension of Drug Design for Targeted Protein Degradation"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Group Photo / Coffee Break
11:00 am - 11:30 am
"New Therapeutic Modalities Enabled and Inspired by Heterobifunctional Degraders"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Optimisation of a Series of RIP2 PROTACs: Delivering on the Promises of Low Dose and Extended Duration of Action"
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
Novel Solutions to ADME Challenges
7:30 pm - 8:00 pm
"Harnessing Preclinical Data as a Predictive Tool for Human Brain Tissue Targeting"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"PT2977: A Best-in-Class HIF-2a Antagonist with Improved ADME Properties and Pharmacokinetics for the Treatment of Clear Cell Renal Cell Carcinoma"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Strategies for Optimizing Projected Human ADME Properties: Application to the Discovery of a Clinical Candidate for the Inhibition of DGAT2"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Emerging Approaches for the Treatment for Non-Alcoholic Steatohepatitis (NASH)
9:00 am - 9:30 am
"Translating Discovery Science to Develop Cures for NASH"
9:30 am - 9:40 am
Discussion
9:40 am - 10:10 am
"Discovery of a Ketohexokinase (KHK) Inhibitor for the Treatment of NAFLD/NASH: Fragment-to-Candidate via Structure-Based Drug Design and Parallel Chemistry"
10:10 am - 10:25 am
Discussion
10:25 am - 10:45 am
Coffee Break
10:45 am - 11:15 am
"Non-Steroidal FXR Agonists: Tropifexor and LMB763"
11:15 am - 11:30 am
Discussion
11:30 am - 12:00 pm
"Selective Inhibitors of Lysyl Oxidase Like 2/3 (LOXL2/3) for the Treatment of Fibrotic Diseases"
12:00 pm - 12:15 pm
Discussion
12:15 pm - 12:30 pm
Poster Previews
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
Targeting RNA with Small Molecules
7:30 pm - 8:00 pm
"RNA-Targeted Small Molecules: A Problem in Drug Discovery"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"Discovery of RO7034067, a Selective SMN2 Splicing Modifier for the Treatment of Spinal Muscular Atrophy"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Identification of Development Candidate eFT226, a First in Class Inhibitor of eIF4A RNA Helicase"
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
"The Discovery of Reldesemtiv (CK-2127107): A Second-Generation, Selective, Small Molecule Fast Skeletal Muscle Troponin Activator (FSTA)"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Discovery of a Diacylglycerol Acyltransferase 2 (DGAT2) Inhibitor for the Treatment of NASH"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Discovery of GLPG2451, a Novel Potentiator for the Treatment of Cystic Fibrosis"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Moving Beyond Once-Daily Regimens: The Search for a Novel NNRTI to Enable a New Paradigm for HIV-1 Treatment"
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: Molecular Complexity: The Challenge of Modern Clinical Candidates
7:30 pm - 8:30 pm
"Molecular Complexity: The Challenge of Modern Clinical Candidates"
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