| Sunday January 19, 2020 |
| 16:00 | Registration |
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| 17:00 | Opening Remarks |
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| 17:30 | Necessity is the Mother of Invention: Natural Products and the Chemistry They Inspire (KL01) |
Prof. Sarah E. REISMAN
(CALIFORNIA INSTITUTE OF TECHNOLOGY, Pasadena, United States) |
| 18:30 | Poster Session & Welcome Reception |
|
| 20:30 | End of Day 1 |
|
| Monday January 20, 2020 |
| 08:30 | Session 1: Predictive ADME Sciences: Striking a Balance Between In Silico and Experimental Work? |
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| Session Chair |
Dr Amit KALGUTKAR
(PFIZER, Groton, United States) |
| 08:30 | Structural Attributes Influencing Unbound Tissue Distribution (PL01) |
Dr Li DI
(PFIZER, Groton, United States) |
| 09:00 | Metabolism of Strained Rings: Tales of the Unexpected (PL02) |
Dr Martin HAYES
(ASTRAZENECA, Gothenburg, Sweden) |
| 09:30 | Coffee Break |
|
| 10:00 | Leveraging In Silico ADMET Profiles and Ancillary Pharmacology to Influence Prioritization of Hit Series with Higher Probability of Success (PL03) |
Dr Falgun SHAH
(MERCK & CO., West Point, United States) |
| 10:30 | Predicting ADME - Reality, Vision or Fantasy? (PL04) |
Dr Simone SCHADT
(F. HOFFMANN-LA ROCHE, Basel, Switzerland) |
| |
Dr Kenichi UMEHARA
(ROCHE PHARMACEUTICAL RESEARCH AND EARLY DEVELOPMENT, Basel, Switzerland) |
| 11:00 | Outdoor Networking Activities |
|
| 15:45 | Networking Break |
|
| 16:00 | NovAliX Workshop: DNA-Encoded Libraries, an Integrated Platform for Hit Finding and Beyond |
Dr Julien MARIN
(NOVALIX, Illkirch, France) |
| 17:00 | Session 2: Frontiers of Synthetic Chemistry |
|
| Session Chair |
Prof. Sarah E. REISMAN
(CALIFORNIA INSTITUTE OF TECHNOLOGY, Pasadena, United States) |
| 17:00 | Break-it-to-Make-it Strategies for Complex Molecule Synthesis (PL05) |
Prof. Richmond SARPONG
(UNIVERSITY OF CALIFORNIA, BERKELEY, Berkeley, United States) |
| 17:30 | New Avenues in Synthesis Enabled by Organic Photoredox Catalysis (PL06) |
Prof. David NICEWICZ
(UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, Chapel Hill, United States) |
| 18:00 | Coffee Break |
|
| 18:30 | Late-Stage Functionalizations (PL07) |
Prof. Tobias RITTER
(MAX-PLANCK-INSTITUT FÜR KOHLENFORSCHUNG, Mulheim, Germany) |
| 19:00 | A Radical Way to Abeo-Steroids (PL08) |
Prof. Philipp HERETSCH
(FREE UNIVERSITY OF BERLIN, Berlin, Germany) |
| 19:30 | Poster Session |
|
| 20:30 | End of Poster Session |
|
| 21:00 | Conference Dinner |
|
| 23:00 | End of Day 2 |
|
| Tuesday January 21, 2020 |
| 08:30 | Session 3: Structure and Biophysics - Companions for Medicinal Chemistry |
|
| Session Chair |
Dr Wolfgang JAHNKE
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland) |
| 08:30 | Membrane Proteins at the SGC – Challenges and Success Stories (PL09) |
Dr Katharina DÜRR
(UNIVERSITY OF OXFORD, Oxford, United Kingdom) |
| 09:00 | The Mechanism of Outer Membrane Protein Insertion by BamA and its Role as a Target for Novel Antibiotic (PL10) |
Prof. Sebastian HILLER
(UNIVERSITY OF BASEL, Basel, Switzerland) |
| 09:30 | Coffee Break |
|
| 10:00 | Discovery of ABL001, an Allosteric Inhibitor of BCR-ABL: Fragments, Biophysics, Structure and Chemistry (PL11) |
Dr Wolfgang JAHNKE
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland) |
| 10:30 | Discovery of Small Molecule Fascin 1 Inhibitors Using Fragment-Based Drug Discovery (OC01) |
Dr Stuart FRANCIS
(THE BEATSON INSTITUTE FOR CANCER RESEARCH, Glasgow, United Kingdom) |
| 11:00 | Outdoor Networking Activities |
|
| 15:00 | Networking Break & "Beyond-the-Science Leadership Development" Workshop |
|
| 15:00 | Beyond-the-Science Leadership Development |
|
| Session Chair |
Dr Michelle CLAFFEY
(CLAFFEY LEADERSHIP, Norwich, United States) |
| Session Chair |
|
| 17:00 | Session 4: Protein Degradation: New Rules for Drug Discovery |
|
| Session Chair |
Prof. Alessio CIULLI
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom) |
| 17:00 | Targeted Protein Degradation (PL12) |
Prof. Andy PHILLIPS
(C4 THERAPEUTICS, Watertown, United States) |
| 17:30 | Chemical Genomics Approaches to Targeted Protein Degradation (PL13) |
Dr Georg WINTER
(RESEARCH CENTER FOR MOLECULAR MEDICINE OF THE AUSTRIAN ACADEMY OF SCIENCES, Vienna, Austria) |
| 18:00 | Four E3 Ligases, One Target: Towards Novel CDK6 Protacs (OC02) |
Dr Christian STEINEBACH
(UNIVERSITY OF BONN, Bonn, Germany) |
| 18:30 | Coffee Break |
|
| 19:00 | Expanding the Druggable Genome through Cereblon-Mediated Protein Degradation (KL02) |
Dr Lawrence G. HAMANN
(BRISTOL-MYERS SQUIBB, San Francisco, United States) |
| 20:00 | End of Day 3 |
|
| Wednesday January 22, 2020 |
| 08:30 | Session 5: Innovation and Inspiration from Natural Products |
|
| Session Chair |
Prof. Thomas MAGAUER
(UNIVERSITY OF INNSBRUCK, Innsbruck, Austria) |
| 08:30 | Capturing Biological Activity in Natural Product Fragments: Success and Limitations (PL14) |
Prof. Karl GADEMANN
(UNIVERSITY OF ZÜRICH, Zürich, Switzerland) |
| 09:00 | (De)Construction of Three-Dimensional Molecular Architectures (PL15) |
Prof. Thomas MAGAUER
(UNIVERSITY OF INNSBRUCK, Innsbruck, Austria) |
| 09:30 | Coffee Break |
|
| 10:00 | Synthesis of Complex Antiplasmodial Isocyanoterpenes (PL16) |
Prof. Christopher VANDERWAL
(UNIVERSITY OF CALIFORNIA, Irvine, United States) |
| 10:30 | Total Synthesis of Chivosazole F (OC03) |
Dr Simon WILLIAMS
(SYNGENTA, Stein AG, Switzerland) |
| 11:00 | Outdoor Networking Activities |
|
| 15:45 | Networking Break & "Panel Discussion on Protein Degradation" |
|
| Panel Discussion on Protein Degradation |
|
| Session Chair |
Dr Klemens HOEGENAUER
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland) |
| |
Prof. Alessio CIULLI
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom) |
| |
Prof. Andy PHILLIPS
(C4 THERAPEUTICS, Watertown, United States) |
| |
Dr Christian STEINEBACH
(UNIVERSITY OF BONN, Bonn, Germany) |
| |
Dr Georg WINTER
(RESEARCH CENTER FOR MOLECULAR MEDICINE OF THE AUSTRIAN ACADEMY OF SCIENCES, Vienna, Austria) |
| 17:00 | Session 6: Accelerating Drug Discovery by Intelligence Augmentation |
|
| Session Chair |
Dr Thomas TRIESELMANN
(BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG, Biberach an der Riss, Germany) |
| 17:00 | Organic Synthesis on a Computer: Should Medicinal Chemists Care? (PL17) |
Prof. Bartosz A. GRZYBOWSKI
(ULSAN NATIONAL INSTITUTE OF SCIENCE & TECHNOLOGY, Ulsan, Korea, South) |
| 17:30 | Exploring an Interface of Synthesis and Data Science (PL18) |
Prof. Timothy CERNAK
(UNIVERSITY OF MICHIGAN, Ann Arbor, United States) |
| 18:00 | Accelerating R&D with Augmented Intelligence (PL19) |
Dr Matthias ZENTGRAF
(BOEHRINGER INGELHEIM, Biberach an der Riss, Germany) |
| 18:30 | Coffee Break |
|
| Session 7: Targeted Delivery - Strategies to Help your Drug Substances get to the Right Place |
|
| Session Chair |
Dr Philippe NANTERMET
(MERCK & CO. INC (MSD), West Point, United States) |
| 19:00 | Using Small Molecules to Engineer and Explore Human Immunity (PL20) |
(BIOIBÉRICA)
Prof. David SPIEGEL (YALE UNIVERSITY, New Haven, United States) |
| 19:30 | Poster Session |
|
| 20:30 | End of Day 4 |
|
| Thursday January 23, 2020 |
| 08:30 | Session 7: Targeted Delivery - Strategies to Help your Drug Substances get to the Right Place |
|
| Session Chair |
Dr Philippe NANTERMET
(MERCK & CO. INC (MSD), West Point, United States) |
| 08:30 | Discovery of Tumor-Targeted TLR7/8 Immune-Stimulating Antibody Conjugates (ISAC): A New Class of Immuno-Oncology Therapeutics (PL21) |
Dr Brian SAFINA
(BOLT BIOTHERAPEUTICS, Redwood City, United States) |
| 09:00 | Intracellular and Tissue Specific Targeting of Therapeutic Modalities (PL22) |
Dr Vadim DUDKIN
(JANSSEN DISCOVERY SCIENCES, Lansdale, United States) |
| 09:30 | Coffee Break |
|
| 10:00 | SBT6050, a HER2-Directed TLR8 Immunotac™ Therapeutic, is a Potent Human Myeloid Cell Agonist with Tumor-Localized Activity (PL23) |
Dr Valerie ODEGARD
(SILVERBACK THERAPEUTICS, Seattle, United States) |
| 10:30 | Outdoor Networking Activities |
|
| 15:45 | Networking Break |
|
| Session 8: Drug Discovery Tales |
|
| Session Chair |
Dr Lena RIPA
(ASTRAZENECA, Sweden) |
| 16:00 | Discovery of GDC-0334: a potent and orally bioavailable clinical candidate for the inhibition of TRPA1 (OC04) |
Dr Vishal VERMA
(GENENTECH, South San Francisco, United States) |
| 16:30 | Investigating the Chameleonic Properties of RGD Integrin Antagonists for the Treatment of IPF (OC05) |
Dr James THOMPSON
(GLAXOSMITHKLINE/UNIVERSITY OF STRATHCLYDE, Stevenage, United Kingdom) |
| 17:00 | Discovery of AZD3458 a Highly Selective PI3Ky Inhibitor: Combining Structure, HDX-MS and Binding Kinetics to Understand the Mode of Action (OC06) |
Dr Nils PEMBERTON
(ASTRAZENECA, Mölndal, Sweden) |
| 17:30 | The Discovery of a Potent and Orally Bioavailable Macrocyclic Cyclophilin Inhibitor Based on The Structural Simplification of Sanglifehrin A (OC07) |
Dr Vicky STEADMAN
(EUROFINS DISCOVERY, Essex, United Kingdom) |
| 18:00 | Coffee Break |
|
| 18:30 | The Big Impact of Small Changes : Towards Best-in-Class EZH2 and LSD1 Inhibitors (OC08) |
Dr Julian LEVELL
(CONSTELLATION PHARMACEUTICALS, Cambridge, United States) |
| 19:00 | Controlling the Fate and Function of Proteins with Photopharmacology (KL03) |
Prof. Dirk TRAUNER
(NEW YORK UNIVERSITY, New York, United States) |
| 20:00 | Closing Remarks |
|
| 20:30 | End of Symposium |
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