| Sunday 26/06/2022 |
| 11:00 | Registration |
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| 13:00 | Welcome Address by NMCS NYC Co-Chairs |
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| 13:00 | |
Dr Amjad ALI (MERCK & CO. INC., Kenilworth, United States)
Prof. Robert DEVITA (ICAHN SCHOOL OF MEDICINE AT MT. SINAI, New York, NY, United States) |
| 13:15 | Session 1: Integrating Novel Chemical Modalities in Hit-to-lead: a New Paradigm for Early Drug Discovery
Session Sponsored by X-Chem |
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| 13:15 | Introduction by Session Chair |
Dr Maria-Jesus BLANCO
(ATAVISTIK BIO, Cambridge, MA, United States) |
| 13:20 | Integrating DNA-Encoded Library Technologies in Lead Discovery (IL01) |
Dr Lisa MARCAURELLE
(GSK, Cambridge, United States) |
| 13:55 | Discovery of IRAKIMiDs: Dual-Mechanism Degraders Targeting IRAK4 and IMiD Substrates for Oncology (IL02) |
Dr Lewis PENNINGTON
(KYMERA THERAPEUTICS INC., Watertown, United States) |
| 14:30 | Development and Optimization of Small Molecule RNA Degraders (IL03) |
Prof. Matthew DISNEY
(SCRIPPS RESEARCH INSTITUTE, Jupiter, United States) |
| 15:05 | Coffee Break & Exhibition |
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| 15:35 | Oral Peptides: Theory and Practice (IL04) |
Dr Lauren MONOVICH
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Cambridge, United States) |
| 16:10 | Structural Approach to Identify Lead Scaffolds for Protein-Protein Interaction Targets (IL05) |
Prof. Kyle HADDEN
(UNIVERSITY OF CONNECTICUT, Storrs, United States) |
| 16:45 | Poster Session 1 |
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| 16:45 | Poster Session (posters with odd numbers)
Chaired by |
Dr Lori FERRINS (NORTHEASTERN UNIVERSITY, Boston, MA, United States)
Prof. Andrii MONASTYRSKYI (MOFFITT CANCER CENTER & RESEARCH INSTITUTE, Tampa, United States) |
| 18:15 | Welcome Reception & Networking |
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| 20:00 | End of the Day |
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| Monday 27/06/2022 |
| 08:30 | Session 2: New Directions in Targeting DNA Damage Repair (DDR)
Session Sponsored by NuChem Sciences |
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| 08:30 | Introduction by Session Chairs |
Dr Erin DIMAURO (MERCK & CO. INC., Boston, United States)
Dr Srinivasa KARRA (AVILAR THERAPEUTICS, Waltham, United States) |
| 08:35 | M3541 and M4076: Discovery and Optimization of Potent and Selective ATM Kinase Inhibitors with Strong Anti-tumor Efficacy in Combination Therapies (IL06) |
Dr Thomas FUCHSS
(MERCK KGAA, HEALTHCARE, Darmstadt, Germany) |
| 09:10 | Discovery and Validation of in vitro and in vivo Probes for Human DNA Polymerase Theta (Polθ) (IL07) |
Dr Robert HEALD
(ARTIOS PHARMA LTD, Cambridge, United Kingdom) |
| 09:45 | The Modification of Pyrazolopyrimidinones and their Effect on WEE1 Inhibition and the DNA Damage Response (IL08) |
Prof. Phil REIGAN
(UNIVERSITY OF COLORADO, Aurora, United States) |
| 10:20 | Coffee Break & Exhibition |
|
| 10:50 | Discovery of KB-0742, a Potent, Selective, Orally Bioavailable Small Molecule Inhibitor of CDK9/cyclin T1 for MYC-dependent Cancers (IL09) |
Dr David FREEMAN
(KRONOS BIO, INC. , Massachussetts, United States) |
| 11:25 | Harnessing CDK12 Inhibition of Transcriptional Machinery to Induce Dimerization between DDB1 and CDK12-cyclinK Complex for Targeted Protein Degradation (IL10) |
Prof. Andrii MONASTYRSKYI
(MOFFITT CANCER CENTER & RESEARCH INSTITUTE, Tampa, United States) |
| 12:00 | Lunch & Exhibition until 1:15 PM
Sponsored by ACS Publications |
|
| 12:20 | Optional Schrödinger Workshop - Augmenting Medicinal Chemistry with Digital Chemistry: A CDK2 Inhibitor Design Challenge |
Mr Wade MILLER
(SCHRÖDINGER, Cambridge, United States) |
| 13:15 | Session 3: Hot Targets from NYC Academic and Biotech Scene |
|
| 13:15 | Introduction by Session Chairs |
Dr Amjad ALI (MERCK & CO. INC., Kenilworth, United States)
Prof. Robert DEVITA (ICAHN SCHOOL OF MEDICINE AT MT. SINAI, New York, NY, United States) |
| 13:20 | Rational Design of Inhibitors of Protein-Protein Interactions (IL11) |
Prof. Paramjit ARORA
(NYU, New York, United States) |
| 13:55 | Next Generation Drug Discovery (IL12) |
Dr Steve COLLETTI
(ZYMERGEN INC., New York, United States) |
| 14:30 | Optimization of Mycobacterium Tuberculosis (Mtb) Selective Inhibitors of Lipoamide Dehydrogenase (Lpd) (IL13) |
Dr John GINN
(TRI-INSTITUTIONAL THERAPEUTICS DISCOVERY INSTITUTE, New York, United States) |
| 15:05 | Coffee Break & Exhibition |
|
| 15:35 | Therapeutic Potential of the Gut-Brain Axis (IL14) |
Dr Iyassu SEBHAT
(KALLYOPE, New Jersey, United States) |
| 16:10 | Designing and Combining Cancer's Off Switches (IL15) |
Dr Karen AKINSANYA
(SCHRODINGER, New York City, United States) |
| 16:45 | End of Session 3 |
|
| 16:50 | Optional Iktos Workshop - AI Tools for Medicinal Chemists: Novel Compound Design and Retrosynthesis Prediction |
Dr Rohit ARORA (IKTOS INC, Ashland, United States)
Dr Brian ATWOOD (IKTOS INC, Los Angeles, United States) |
| 17:15 | Poster Session 2 |
|
| 17:15 | Poster Session 2 (posters with even numbers)
Chaired by |
Dr Lori FERRINS (NORTHEASTERN UNIVERSITY, Boston, MA, United States)
Prof. Andrii MONASTYRSKYI (MOFFITT CANCER CENTER & RESEARCH INSTITUTE, Tampa, United States) |
| 18:45 | End of the Day |
|
| Tuesday 28/06/2022 |
| 08:30 | Session 4: Targeting Autophagy for Cancer, Neurodegeneration, or Autoimmune Disease |
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| 08:30 | Introduction by Session Chairs |
Dr Erin DIMAURO (MERCK & CO. INC., Boston, United States)
Dr Hongjun David ZHANG (CEREVEL THERAPEUTICS, LLC, Boston, United States) |
| 08:35 | Unraveling Autophagy in Cancer Using Chemical Genetics (IL16) |
Prof. Jeff MACKEIGAN
(MICHIGAN STATE UNIVERSITY, East Lansing, United States) |
| 09:05 | Small Molecule PINK1 Activators Rescue Parkinson’s Disease Pathology (IL17) |
Dr Nicholas HERTZ
(MITOKININ INC, San Francisco, United States) |
| 09:35 | Revolutionizing Discovery and Development of ALS Therapeutics using Transformational, AI-powered 'All-in-Human' Platforms (IL18) |
Dr Irene CHOI
(VERGE GENOMICS, South San Francisco, United States) |
| 10:05 | Coffee Break & Exhibition |
|
| 10:35 | Chasing Challenging Targets: Development of Selective Inhibitors of the Autophagy Pathway to Impact Cancer Therapy (IL19) |
Prof. Leslie ALDRICH
(UNIVERISTY OF ILLINOIS AT CHICAGO, Chicago, United States) |
| 11:05 | Chemical Activation of Chaperone-Mediated Autophagy for Protection against Neurodegeneration (IL20) |
Prof. Evripidis GAVATHIOTIS
(ALBERT EINSTEIN COLLEGE OF MEDICINE, Bronx, United States) |
| 11:35 | Necessary Complexity: The Discovery of Selective, CNS Penetrant LRRK2 Inhibitors for the Treatment of Parkinson’s Disease (IL21) |
Dr Peter FULLER
(MERCK & CO. INC., Boston, United States) |
| 12:05 | End of AM Program |
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| 13:00 | Social Activities & Free Time |
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| 17:45 | Award Session |
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| 17:45 | Award Dinner |
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| 19:15 | Award Session - Opening Address |
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| 19:29 | 2022 Division of Medicinal Chemistry Award |
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| 19:30 | Award Ceremony chaired by ACS Medi Division Chair 2022, Prof. Amanda Bryant-Friedrich (Wayne State University, United States) |
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| 19:40 | 2022 Division of Medicinal Chemistry Award Lecture
A Perspective on the Arc of Innovation in Drug Discovery over Three Decades (AL01) |
Dr Lawrence G. HAMANN
(INTERDICT BIO, San Francisco, United States) |
| 20:24 | 2022 IUPAC-Richter Prize |
|
| 20:25 | Prize Ceremony chaired by Dr Janos Eles (Gedeon Richter, Hungary) |
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| 20:35 | 2022 IUPAC-Richter Prize Lecture
Drug Discovery in Academia: Some Success Stories (AL02) |
Prof. Michael E. JUNG
(UCLA CHEMISTRY & BIOCHEMISTRY, Los Angeles, United States) |
| 21:20 | End of the Day |
|
| Wednesday 29/06/2022 |
| 08:30 | Session 5: Next Generation Therapies Shaped by Clinical Data |
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| 08:30 | Introduction by Session Chair |
Dr Steven MCKERRALL
(SEPTERNA, South San Francisco, United States) |
| 08:35 | Discovery of LPA1 antagonists for the treatment of Pulmonary Fibrotic Diseases (IL22) |
Dr Peter CHENG
(BRISTOL-MYERS SQUIBB R & D, Hopewell, United States) |
| 09:05 | Discovery of Risdiplam, a Medicine for the Treatment of Spinal Muscular Atrophy (IL23) |
Dr Luke GREEN
(HOFFMANN-LA ROCHE, Basel, Switzerland) |
| 09:35 | The Invention of MK-8262, a CETP Inhibitor for the Treatment of Coronary Heart Disease (IL24) |
Dr Petr VACHAL
(MERCK & CO. INC (MSD), Kenilworth, United States) |
| 10:05 | Coffee Break & Exhibition |
|
| 10:35 | Discovery of Inavolisib, a Highly Selective Inhibitor of PI3K-α that Induces Degradation of Mutant-p110α Protein (IL25) |
Dr Marie-Gabrielle BRAUN
(GENENTECH, South San Francisco, United States) |
| 11:05 | Discovery of PF-07081532: a Small Molecule GLP-1 Receptor Agonist Suitable for Once-daily Oral Administration (IL26) |
Dr David A. GRIFFITH
(PFIZER INC., Cambridge, United States) |
| 11:35 | Discovery of LY3154885, a Second Generation Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Drug-Drug Interaction Risk Profile (IL27) |
Dr Erik HEMBRE
(ELI LILLY & CO., Indianapolis, United States) |
| 12:05 | Lunch Break & Exhibition until 1:20PM
Sponsored by Paraza Pharma |
|
| 12:20 | Optional Aseda Sciences Workshop - Drug Discovery Platforms, the Predictive Information Gap, and How to Bridge it |
Dr Andrew BIEBERICH
(ASEDA SCIENCES, West Lafayette, United States) |
| 13:20 | Session 6: Lessons from Drug Hunters across Academia, NPOs and the Pharmaceutical Industry |
|
| 13:20 | Introduction by Session Chair |
Dr Philip KYM
(ABBVIE, North Chicago, United States) |
| 13:25 | Small Molecule Drug Discovery in Academia: DYRK1A Inhibitors as Novel beta-Cell Regenerative Drugs for Diabetes (IL28) |
Prof. Robert DEVITA
(ICAHN SCHOOL OF MEDICINE AT MT. SINAI, New York, NY, United States) |
| 14:00 | Discovery of Upadacitinib: a Tricyclic Janus Kinase 1 (JAK1) Inhibitor (IL29) |
Dr Kristine E. FRANK
(ABBVIE, North Chicago, United States) |
| 14:35 | Anticancer Drug Discovery from Pets to People, the Story of PAC-1 (IL30) |
Prof. Paul J. HERGENROTHER
(UNIVERSITY OF ILLINOIS, Urbana, United States) |
| 15:10 | Coffee Break & Exhibition |
|
| 15:40 | Discovery of Nix-TB as a Novel Regimen that Significantly Shortens Treatment of Tuberculosis (IL31) |
Dr Christopher B. COOPER
(TB ALLIANCE, GLOBAL ALLIANCE FOR TB DRUG DEVELOPMENT, New York, United States) |
| 16:15 | Adventures in Drug Hunting (IL32) |
Dr Wendy YOUNG
(MPM CAPITAL, Brisbane, CA, United States) |
| 16:50 | Closing Remarks |
Dr Amjad ALI (MERCK & CO. INC., Kenilworth, United States)
Prof. Robert DEVITA (ICAHN SCHOOL OF MEDICINE AT MT. SINAI, New York, NY, United States) |
| 17:00 | Departure |
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