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
Discussion Leader: Izzat Raheem (Merck, USA)
7:40 pm - 8:10 pm
Dmitri Pissarnitski (Merck, USA)
"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
Kerry Benenato (Moderna Therapeutics, USA)
"Optimization of Lipid Nanoparticles for mRNA-Based Therapeutics"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Thomas Pillow (Genentech, Inc., USA)
"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
Discussion Leader: Alex Cortez (Genomics Institute of the Novartis Research Foundation, USA)
9:00 am - 9:30 am
Meredeth McGowan (Merck Research Laboratories, USA)
"Discovery and Evolution of Potent and Selective Heme-Displacing IDO1 Inhibitors"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Joshi Ramanjulu (GlaxoSmithKline, USA)
"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
Thomas Knoepfel (Novartis Pharma AG, Switzerland)
"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
Richard Mackman (Gilead Sciences, USA)
"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
3:00 pm - 4:00 pm
The GRC Power Hour™
The GRC Power Hour™ is designed to address challenges women face in science and issues of diversity and inclusion. The program supports the professional growth of all members of our communities by providing an open forum for discussion and mentoring.
Organizer: Darby Schmidt (Rheostat Therapeutics, USA)
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
Discussion Leader: Katerina Leftheris (Pliant Therapeutics, USA)
7:30 pm - 8:00 pm
Frederic Berst (Novartis Pharma AG, Switzerland)
"DNA-Encoded Libraries: Hit Generation from Vast Chemical Spaces"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Alexander Satz (Roche, Switzerland)
"Hit-to-Lead with DNA-Encoded Libraries: Autotaxin and DDR1"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Yun Ding (GlaxoSmithKline, USA)
"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
Discussion Leaders: Emily Peterson (Biogen, USA) and Brian Raymer (Alkermes, USA)
9:00 am - 9:30 am
Nathan Fuller (Rodin Therapeutics, USA)
"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
Christopher Butler (Pfizer, USA)
"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
Junliang Hao (Eli Lilly & Company, USA)
"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
Matthew Volgraf (Genentech, Inc., USA)
"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
Discussion Leader: Joachim Rudolph (Genentech, USA)
7:30 pm - 8:00 pm
Jason Kettle (AstraZeneca, United Kingdom)
"Allosteric Covalent Inhibitors of the Mutant GTPase KRASG12C "
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Lawrence Snyder (Arvinas, USA)
"ARV-110, an Orally Bioavailable PROTAC™ 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
Sudeep Prajapati (H3 Biomedicine, USA)
"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
Discussion Leader: L.-C. Campeau (Merck Research Laboratories, USA)
9:00 am - 9:30 am
Danica Rankic (Merck & Co., Inc., USA)
"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
Michael Koehler (Genentech, USA)
"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
Ryan Patman (Pfizer, USA)
"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
Stephen Greszler (Abbvie, Inc., USA)
"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
Discussion Leader: Brian Lawhorn (GlaxoSmithKline, USA)
7:30 pm - 8:00 pm
Christopher Larson (Sanford Burnham Prebys Medical Discovery Institute, USA)
"Learning from Recent Efforts in Heart Failure Drug Discovery"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Muneto Mogi (Novartis Institutes for BioMedical Research, USA)
"The Journey of Neprilysin Inhibitors"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Heather Finlay (Bristol-Myers Squibb, USA)
"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
Discussion Leader: Matthew Volgraf (Genentech, Inc., USA)
9:00 am - 9:30 am
Gregg Keaney (Cadent Therapeutics, USA)
"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
Stefanie Flohr (Novartis Pharma AG, Switzerland)
"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
Joshua Hansen (Celgene, USA)
"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
Brock Shireman (Janssen, USA)
"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
Discussion Leader: Janeta Popovici-Muller (Decibel Therapeutics, USA)
7:30 pm - 8:30 pm
Gregory Verdine (FogPharma / LifeMine Therapeutics, USA)
"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