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
Medicinal Chemistry Enabling Novel Strategies for Intracellular and Targeted Delivery
7:40 pm - 8:10 pm
"Development of Novel Insulins Capable of Glucose-Regulated Delivery to Mitigate Hypoglycemia Risk"
8:10 pm - 8:15 pm
Discussion
8:15 pm - 8:45 pm
"Optimization of Lipid Nanoparticles for mRNA-Based Therapeutics"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Discovery of Potent BRD4 Degraders and Their Delivery as Antibody Conjugates"
9:20 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Recent Developments of Immune Modulators
9:00 am - 9:30 am
"Discovery and Evolution of Potent and Selective Heme-Displacing IDO1 Inhibitors"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Discovery of STING Agonist with Systemic Anti-Tumor Response"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Target Based Identification and Optimization of Toll-Like Receptor 7/8 Antagonists"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Discovery of GS-9688, a Selective Toll-Like Receptor 8 Agonist for Hepatitis B Cure"
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
High Quality Leads from Encoded Screening Technologies
7:30 pm - 8:00 pm
"DNA-Encoded Libraries: Hit Generation from Vast Chemical Spaces"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"Hit-to-Lead with DNA-Encoded Libraries: Autotaxin and DDR1"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"From Haystack to Needle: Clinical Candidate Using Encoded Libraries at GSK"
9:20 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Recent Advances in Neuroscience
9:00 am - 9:30 am
"Discovery of CoREST Complex-Selective HDAC Inhibitors with Pro-Synaptic Effects for the Treatment of Synaptopathies"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Optimization and Identification of Brain Penetrant, M4 Subtype-Selective Muscarinic Receptor Positive Allosteric Modulator (M4 PAM) Clinical Candidate"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Group Photo / Coffee Break
11:00 am - 11:30 am
"Discovery of LY3154207, a Potent, Selective and Orally Available Positive Allosteric Modulator of the Dopamine D1 Receptor"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"TRPA1 as a Neuronal Regulator of Inflammation in the Lung: Discovery of a Clinical Candidate for the Treatment of Asthma"
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
Expanded Modalities in Targeting Cancer
7:30 pm - 8:00 pm
"Allosteric Covalent Inhibitors of the Mutant GTPase KRASG12C "
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"ARV-110, an Orally Bioavailable PROTACâ„¢ Protein Degrader Molecule for the Treatment of Men with Metastatic Castration Resistant Prostate Cancer"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Development of Selective Estrogen Receptor Covalent Antagonists (SERCA) for the Treatment of ERαWT and ERαMUT Breast Cancer"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Enabling and Inspiring Drug Discovery via Innovations in Synthesis
9:00 am - 9:30 am
"Synthesis Inspired Design: Benzocyclobutyl Amines as Aniline Surrogates Within the IDO Program"
9:30 am - 9:40 am
Discussion
9:40 am - 10:10 am
"Optimization of the Arylomycins Results in a New Class of Gram-Negative Antibiotics"
10:10 am - 10:20 am
Discussion
10:20 am - 10:50 am
Coffee Break
10:50 am - 11:20 am
"Design and Synthesis of Carbonucleoside Inhibitors of PRMT5 for the Treatment of Cancer: A Desymmetrization Approach"
11:20 am - 11:30 am
Discussion
11:30 am - 12:00 pm
"Impacting the Pipeline Through Discovery Synthesis Groups: Cystic Fibrosis, HCV and Immunology"
12:00 pm - 12:10 pm
Discussion
12:10 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
New Approaches for the Treatment of Heart Failure
7:30 pm - 8:00 pm
"Learning from Recent Efforts in Heart Failure Drug Discovery"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"The Journey of Neprilysin Inhibitors"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Identification of an APJ Receptor Agonist Clinical Candidate for Heart Failure"
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 CAD-1883, a Clinical-Stage Positive Allosteric Modulator of the SK Channel for the Treatment of Essential Tremor and Spinocerebellar Ataxia"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Discovery of LNP023, a First-in-Class, Oral Factor B Inhibitor for Treatment of Rare Alternative Complement Pathway Driven Diseases"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Discovery of CC-90009, a CRBN E3 Ligase Modulating Drug (CELMoD) with Selective GSPT1 Degradation for the Treatment of Acute Myeloid Leukemia"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Discovery of JNJ-61393215, a Selective Orexin-1 Receptor Antagonist"
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: Hunting the Future of Drug Discovery
7:30 pm - 8:30 pm
"Hunting the Future of Drug Discovery"
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