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 Staff / Welcome and Introduction from the Chairs
7:40 pm - 9:30 pm
7:40 pm - 8:05 pm
"Inhaled Administration for Intra-Cellular Targets Exemplified by the Discovery of FRAP1 (mTOR kinase) Inhibitors"
8:05 pm - 8:20 pm
Discussion
8:20 pm - 8:45 pm
"Discovery of NVP-MIW491: Dermal Delivery of an LXR Agonist for the Treatment of Meibomian Gland Dysfunction"
8:45 pm - 8:55 pm
Discussion
8:55 pm - 9:20 pm
"Development of a Colon-Targeted Pan-SIK Inhibitor for the Treatment of IBD"
9:20 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
New Frontiers in Oncology Therapies
9:00 am - 9:30 am
"IL4i1 Inhibitors from Target Validation Through to First-In-Human Studies in Cancer Patients"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Identification of Dencatistat: An Isoform Selective CTPS1 Inhibitor for Multiple Oncology Indications"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Structure- and Property-Based Design of Macrocyclic pan-KRAS Inhibitors"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Discovery of MOMA-341, a Chemically Distinct, Potent and Selective Covalent Inhibitor of Werner Syndrome Helicase (WRN)"
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 the interests and needs of all scientists and the challenges they face in their careers. Specifically, the program promotes meaningful conversations amongst colleagues of all career stages about barriers to career advancement and strategies to support the professional growth of all members of the community. The GRC Power Hour™ is open to all conference participants.
4:00 pm - 6:00 pm
Poster Session
6:00 pm - 7:00 pm
Dinner
7:30 pm - 9:30 pm
Deconvolution Strategies for Phenotypic Screens
7:30 pm - 8:00 pm
"Discovery and Optimization of the First Specific Ribosome Biogenesis Inhibitor Targeting the AAA-ATPase NVL"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"Phenotypic Screening and Target Deconvolution: Identification of a Chemical Series with Antiviral Activity Against Sarbecovirus with a Novel Mechanism of Action"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Identification of HbF-Activating CELMoDs™ Through Phenotypic Screening and the Subsequent Development of the ZBTB7A/WIZ Dual Degrader BMS-986470 for the Treatment of Sickle Cell Disease"
9:20 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Innovations in Medicinal Chemistry to Advance Peptide Therapeutics
9:00 am - 9:30 am
"Oral Peptide Inhibitors of IL-1β for ASCVD"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Orally Bioavailable Macrocyclic Peptide Cyclin A/B RxL Inhibitors to Treat Cancers with High E2F Activity"
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 FOG-001, a Clinical Stage Helicon Inhibitor of the Beta-Catenin/TCF4 Interaction"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Advances in Peptide Conjugates: Exemplified by Macrocyclic Peptidic Degraders"
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
Overcoming Challenges in Achieving and Measuring Effective Therapeutic Concentration
7:30 pm - 8:00 pm
"Discovery of GS-4182, a Lenacapavir Prodrug to Treat HIV Infection with Once-Weekly Oral Administration"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"Rapid Optimization of RUVBL1/2 Inhibitors Enabled by Single-Molecule Tracking"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Discovery of a Clinical Gut-Restricted KEAP1-NRF2 Inhibitor for the Treatment of Inflammatory Bowel Disease"
9:20 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
9:00 am - 9:30 am
"Inhibition of Multiple System Atrophy with a New Class of Stacking Ligands for Fibrillar α-Synuclein"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Discovery of [11 C]MK-7337, A Novel High-Affinity Alpha-Synuclein PET Ligand for Imaging in Idiopathic Parkinson’s Disease Patients"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Discovery of Novel Azaindazole GluN2B NAMs"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
"Discovery of VENT-02: a Highly Brain-Penetrant NLRP3 Inhibitor for the Treatment of Neuroinflammatory Disorders"
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
Use of Artificial Intelligence and Machine Learning in Medicinal Chemistry, Challenges, Opportunities and the Limits
7:30 pm - 8:00 pm
"AI in Drug Discovery: Revolution, Evolution, or Complete Nonsense"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
"Are Co-Folding Methods Ready for Prime Time?"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
"Painting a Picture of AI at AstraZeneca: An HPK1 Case Study"
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(s); Complete the GRC Evaluation Forms; Election of the Next Vice Chair(s)
9:00 am - 12:30 pm
Late-Breaking Topics: First Disclosures of Clinical Candidates
9:00 am - 9:30 am
"Discovery of a First-in-class Molecular Glue Degrader, BMS-986463, for the Treatment of Advanced Malignant Solid Tumors"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
"Discovery of Clinical Candidate PF-07293893: A Novel and Selective AMPKγ3 Activator for the Treatment of Heart Failure"
10:15 am - 10:30 am
Discussion
10:30 am - 11:00 am
Coffee Break
11:00 am - 11:30 am
"Discovery of GS-1427: A Potent, Selective, Oral Small Molecule Inhibitor of α4β7 for the Treatment of Inflammatory Bowel Disease"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
Late-Breaking Topic
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: Keynote Session: Humanizing Drug Discovery
7:30 pm - 8:30 pm
"Humanizing 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