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
Keynote Session: The Vanguard of Chemical Biology
7:40 pm - 8:10 pm
"Behavior-Based Discovery of New Optochemical Genetic Tools"
8:10 pm - 8:15 pm
Discussion
8:15 pm - 8:45 pm
"Novel Approaches to Infectious Disease Targets"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:25 pm
"Optical Control of the Cytoskeleton"
9:25 pm - 9:30 pm
Discussion
Monday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Small Molecule Probes, Drug Candidates and New Approaches in Chemical Biology
9:00 am - 9:30 am
"Small Molecule Modulators of Conformationally Dynamic Protein Complexes"
9:30 am - 9:35 am
Discussion
9:35 am - 10:05 am
"Fragment to Pharmacophore to Candidate: Invention of INCB054329, a Potent and Selective BRD Inhibitor in Clinical Trials for Oncology"
10:05 am - 10:10 am
Discussion
10:10 am - 10:40 am
"Developing Small Molecule Inhibitors of RNA Splicing Kinases for the Modulation of Protein Isoforms"
10:40 am - 10:45 am
Discussion
10:45 am - 11:15 am
Coffee Break
11:15 am - 11:45 am
"Deciphering the Human Microbiome Using Chemistry"
11:45 am - 11:50 am
Discussion
11:50 am - 12:05 pm
"Molecular Probes for Determination of Sub-Cellular Compound Exposure in Gram-Negative Bacteria"
12:05 pm - 12:10 pm
Discussion
12:10 pm - 12:25 pm
"DELs in Cells: Phenotypic Screening with DNA-Encoded Cyclic Peptides"
12:25 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
Chemical Biology with Proteins, Mini-Proteins, and Peptides
7:30 pm - 8:05 pm
"Chemoenzymatic Platforms for the Discovery of New Peptide Therapeutics"
8:05 pm - 8:10 pm
Discussion
8:10 pm - 8:45 pm
"Homogenous Antibody Drug Conjugates Enabled by Cysteine Arylation"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:25 pm
"Discovery and Characterization of Novel Microproteins"
9:25 pm - 9:30 pm
Discussion
Tuesday
7:30 am - 8:30 am
Breakfast
8:30 am - 9:00 am
Group Photo
9:00 am - 12:30 pm
Novel Chemistries and Methods for Chemical Biology and Therapeutics
9:00 am - 9:30 am
"Comprehensive Drug Target Profiling Using Complementary (Chemo-)proteomics Approaches"
9:30 am - 9:35 am
Discussion
9:35 am - 10:05 am
"Unravelling and (Re)engineering Biosynthetic Pathways"
10:05 am - 10:10 am
Discussion
10:10 am - 10:40 am
"Spying on Cellular Communication"
10:40 am - 10:45 am
Discussion
10:45 am - 11:15 am
Coffee Break
11:15 am - 11:30 am
"Biocatalysis for Complex Molecule Synthesis"
11:30 am - 11:35 am
Discussion
11:35 am - 11:50 am
"Chemogenetic Approach for Allosteric Activation of Neurotransmitter Receptors on Living Cells"
11:50 am - 11:55 am
Discussion
11:55 am - 12:25 pm
"The Cellular Response to Drugs Quantified by Fitness Profiling: A Genetic Networks' Perspective"
12:25 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
Chemical Biology: Phenotype, Target Engagement, and Mechanism of Action
7:30 pm - 8:05 pm
"It's About Time: Mechanistic PK-PD Models for Time-Dependent Inhibitors"
8:05 pm - 8:10 pm
Discussion
8:10 pm - 8:45 pm
"Drug-Target Engagement in Live Cells"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:25 pm
"Generating Resistance Alleles of Epigenetic Drug Targets"
9:25 pm - 9:30 pm
Discussion
Wednesday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Novel Chemistries and Methods for Chemical Biology and High-Throughput Experimentation
9:00 am - 9:30 am
"Enabling Chemistry Technologies - Accelerators of Drug Discovery"
9:30 am - 9:35 am
Discussion
9:35 am - 10:05 am
"Design and Application of DNA Encoded Libraries at Roche"
10:05 am - 10:10 am
Discussion
10:10 am - 10:40 am
"High Throughput Experimentation in the Optimization of Metallaphotoredox Catalyzed Alpha-Hydroxy Arylation Reactions"
10:40 am - 10:45 am
Discussion
10:45 am - 11:20 am
Coffee Break
11:20 am - 11:50 am
"Approaches to Cellular Characterization of Small Molecule Protein Binders"
11:50 am - 11:55 am
Discussion
11:55 am - 12:25 pm
"Drug Discovery for Challenging Targets Using DNA-Encoded Chemistry"
12:25 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
7:00 pm - 7:30 pm
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
7:30 pm - 9:30 pm
Chemistry and Biology of Natural Products
7:30 pm - 8:05 pm
"New Methods for the Synthesis of Biologically Active Molecules"
8:05 pm - 8:10 pm
Discussion
8:10 pm - 8:45 pm
"Directing Biosynthesis Through Protein-Protein Interactions"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:25 pm
"Redox Catalysis for Complex Molecule Synthesis"
9:25 pm - 9:30 pm
Discussion
Thursday
7:30 am - 8:30 am
Breakfast
9:00 am - 12:30 pm
Bivalent Molecules and Other Novel Approaches to Control of Function
9:00 am - 9:30 am
"Clinical Candidate AZD5153 Is a Novel Bivalent Inhibitor of BET Bromodomains"
9:30 am - 9:35 am
Discussion
9:35 am - 10:05 am
"Targeted Protein Degradation as a Novel Therapeutic Approach"
10:05 am - 10:10 am
Discussion
10:10 am - 10:40 am
"Bifunctional Molecules for Modulating Human Immune Responses"
10:40 am - 10:45 am
Discussion
10:45 am - 11:20 am
Coffee Break
11:20 am - 11:50 am
"'Stay on Target' — Targeting Kinetically Privileged First Responders in Electrophile Signaling"
11:50 am - 11:55 am
Discussion
11:55 am - 12:25 pm
"Low Throughput Studies of Reactivity to Enable High Throughput Applications"
12:25 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: Novel Therapeutics
7:30 pm - 8:05 pm
"Expanding the Druggable Genome with Cereblon Modulators"
8:05 pm - 8:10 pm
Discussion
8:10 pm - 8:45 pm
"Targeting Transcription Addiction in Cancer"
8:45 pm - 8:50 pm
Discussion
8:50 pm - 9:25 pm
"Probing Neurogenetic Disorders Using Patient-Specific Stem Cells and Chemogenomics"
9:25 pm - 9:30 pm
Discussion
Friday
7:30 am - 8:30 am
Breakfast
9:00 am
Departure