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
Non-Oral Drug Delivery
Discussion Leader: Christopher Plummer (Merck Research Laboratories, USA)
7:40 pm - 8:05 pm
Mark Zak (Genentech, USA)
"Inhaled Janus Kinase 1 (JAK1) Inhibitors for Asthma"
8:05 pm - 8:15 pm
Discussion
8:15 pm - 8:40 pm
Kevin Dack (LEO Pharma A/S, Denmark)
"'Super-Soft' Selective Glucocorticoid Receptor Agonist (SEGRA-ss) for Dermatology"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:15 pm
Izzat Raheem (Merck, USA)
"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
Discussion Leader: Michael Ellis (Celgene, USA)
9:00 am - 9:30 am
Brendan Parr (Genentech, Inc., USA)
"Selective Inhibition of Tryptophan-2,3-Dioxygenase (TDO)"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Michelle Lamb (AstraZeneca, USA)
"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
Mikhail Zibinsky (FLX Bio, Inc., USA)
"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
Wes Trotter (Merck, USA)
"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
Discussion Leader: Ashley Jarvis (Evotec (UK) Ltd, United Kingdom)
7:30 pm - 8:00 pm
Thorsten Nowak (C4X Discovery, United Kingdom)
"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
Tom Heightman (Astex Pharmaceuticals, United Kingdom)
"The Role of Solution Conformation in Structure-Guided Fragment Optimization"
8:40 pm - 8:50 pm
Discussion
8:50 pm - 9:20 pm
Elisabetta Chiarparin (AstraZeneca, United Kingdom)
"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
Discussion Leader: Matthew Bourbeau (Amgen, USA)
9:00 am - 9:30 am
Christopher Nasveschuk (C4 Therapeutics, USA)
"Advances in the Medicinal Chemistry of Targeted Protein Degradation"
9:30 am - 9:45 am
Discussion
9:45 am - 10:15 am
Alessio Ciulli (University of Dundee, United Kingdom)
"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
Steve Staben (Genentech, USA)
"New Therapeutic Modalities Enabled and Inspired by Heterobifunctional Degraders"
11:30 am - 11:45 am
Discussion
11:45 am - 12:15 pm
John Harling (GlaxoSmithKline, United Kingdom)
"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
Discussion Leader: Julia Haas (Array BioPharma, USA)
7:30 pm - 8:00 pm
Nandini Patel (Pfizer, Inc., USA)
"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
Rui Xu (Peloton Therapeutics, USA)
"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
Michael Wiley (Eli Lilly and Company, USA)
"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)
Discussion Leader: Ralf Glatthar (Novartis Institutes for BioMedical Research, Switzerland)
9:00 am - 9:30 am
Arun Sanyal (Virginia Commonwealth University, USA)
"Translating Discovery Science to Develop Cures for NASH"
9:30 am - 9:40 am
Discussion
9:40 am - 10:10 am
David Price (Pfizer Inc., USA)
"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
Valentina Molteni (Genomics Institute of the Novartis Research Foundation, USA)
"Non-Steroidal FXR Agonists: Tropifexor and LMB763"
11:15 am - 11:30 am
Discussion
11:30 am - 12:00 pm
Dieter Hamprecht (Pharmaxis Ltd, Australia)
"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
Discussion Leader: Darby Schmidt (Rheostat Therapeutics, USA)
7:30 pm - 8:00 pm
Jennifer Petter (Arrakis Therapeutics, USA)
"RNA-Targeted Small Molecules: A Problem in Drug Discovery"
8:00 pm - 8:10 pm
Discussion
8:10 pm - 8:40 pm
Hasane Ratni (F. Hoffmann-La Roche Ltd, Switzerland)
"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
Justin Ernst (eFFECTOR Therapeutics, USA)
"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
Discussion Leader: Joshi Ramanjulu (GlaxoSmithKline, USA)
9:00 am - 9:30 am
Grace Chuang (Cytokinetics, USA)
"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
Kentaro Futatsugi (Pfizer, Inc., USA)
"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
Steven Van der Plas (Galapagos, Belgium)
"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
Christopher Burgey (Merck, USA)
"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
Discussion Leader: Carolyn Dzierba (Bristol-Myers Squibb, USA)
7:30 pm - 8:30 pm
Martin Eastgate (Bristol-Myers Squibb, USA)
"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