EFMC-ISMC 2016

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Conferences > Archives > EFMC-ISMC 2016

Programme Schedule

Sunday August 28, 2016
13:30Registration
16:00Opening Ceremony
Dr Phil JONES
(UNIVERSITY OF DUNDEE, Glasgow, United Kingdom)
16:20Science, Art and Drug Discovery, a Personal Perspective
Sir Simon CAMPBELL
(SCIENTIFIC CONSULTANT, Poole, United Kingdom)
Chair
Dr Phil JONES
(UNIVERSITY OF DUNDEE, Glasgow, United Kingdom)
17:05The European Research Council (ERC) and its Support for Medicinal Chemistry
Prof. Klaus BOCK
(UNIVERSITY OF COPENHAGEN , Copenhagen, Denmark)
Chair
Prof. Rebecca DEPREZ-POULAIN
(UNIVERSITY OF LILLE, Lille, France)
17:30Award Ceremony
Prof. Koen AUGUSTYNS
(UNIVERSITY OF ANTWERP, Antwerp, Belgium)
17:50NAUTA AWARD FOR PHARMACOCHEMISTRY
Molecular Recognition Studies with Chemical and Biological Systems: A Multi-Dimensional Approach to Support Structure-Based Drug Design
Prof. François DIEDERICH
(ETH ZURICH, Zürich, Switzerland)
Chair
Prof. Henk TIMMERMAN
(VU UNIVERSITY AMSTERDAM, Oegstgeest, The Netherlands)
18:40Late-Stage Fluorination
Prof. Tobias RITTER
(MAX-PLANCK-INSTITUT FÜR KOHLENFORSCHUNG, Mulheim, Germany)
Chair
Dr Anette GRAVEN SAMS
(H. LUNDBECK, Valby, Denmark)
19:25Welcome Reception Sponsored by Concept Life Sciences
Monday August 29, 2016
08:30UCB-EHRLICH AWARD FOR EXCELLENCE IN MEDICINAL CHEMISTRY
Traversing the Valley of Death in Anticancer Drug Discovery
Prof. Paul J. HERGENROTHER
(UNIVERSITY OF ILLINOIS, Urbana, United States)
Chair
Dr Laurent PROVINS
(UCB, Braine-l'Alleud, Belgium)
09:15Cross-Coupling Approaches to Saturated N-Heterocycles
Prof. Jeffrey BODE
(ETH ZÜRICH, Zürich, Switzerland)
Chair
Dr Karin BRINER
(NOVARTIS, Cambridge, United States)
10:00Exhibition & Coffee
1.1 Intramolecular Hydrogen Bonding and its Impact in Drug Design and Discovery (ACSMEDI Session)1.2 Drug Discovery Approaches Toward Targeting Ras1.3 New Antibacterials. An Update
10:30Session Chairs
Dr Amjad ALI (MERCK & CO. INC., Kenilworth, United States)
Dr Tanweer KHAN (MERCK, SHARP & DOHME, Kenilworth, United States)
10:30Session Chair
Dr Joachim RUDOLPH
(GENENTECH, South San Francisco, United States)
10:30Session Chair
Prof. Malcolm PAGE
(JACOBS UNIVERSITY, Bremen, Germany)
10:35The Need of Implementing Intramolecular Hydrogen Bonding (IMHB) Considerations in Drug Discovery and How to do it
Prof. Giulia CARON
(UNIVERSITY OF TORINO, Torino, Italy)
10:35Studying Ciliary Trafficking and How it Leads to RAS Drug Candidates
Prof. Alfred WITTINGHOFER
(MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany)
10:35New Antibacterial Agents in the Pipeline
Dr Eric DESARBRE
(BASILEA PHARMACEUTICA, Basel, Switzerland)
11:15Intramolecular Hydrogen Bond Expectations in Medicinal Chemistry
Dr Fabrizio GIORDANETTO
(D.E. SHAW RESEARCH LLC, New York, United States)
11:15Chemical Biological Modulation of KRas-Signaling
Prof. Herbert WALDMANN
(MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany)
11:15Mechanistic and Inhibition Studies on Metallo-Beta-Lactamases
Prof. Christopher J. SCHOFIELD
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
11:35Intramolecular Hydrogen Bonding as a Design Element in Medicinal Chemistry
Dr Bernd KUHN
(F. HOFFMANN-LA ROCHE, Basel, Switzerland)
11:35Inhibition of Prenylated KRAS: Tools to Discover and Characterize RAS Ligands
Dr Johanna JANSEN
(NOVARTIS, Emeryville, United States)
11:35Enterobactin-Dependent Iron Uptake Pathway as a Gate for Antibiotic Trojan Horse Strategies Against Pseudomonas Aeruginosa
Dr Gaëtan MISLIN
(UNIVERSITY OF STRASBOURG, Illkirch-Graffenstaden, France)
11:55Intramolecular Hydrogen Bonds in the Design of CREBBP Bromodomain Ligands
Prof. Stuart CONWAY
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
11:55Small Molecule Binding Sites on the RAS: SOS Complex Can Be Exploited for Inhibition of RAS Activation
Dr. Jon WINTER-HOLT
(ASTRAZENECA, Macclesfield, United Kingdom)
11:55Exploring Hit-Identification Strategies for Energy-Coupling Factor Transporters, a Novel Target for the Development of Antibiotics
Ms Leticia MONJAS GOMEZ
(UNIVERSITY OF GRONINGEN, Groningen, The Netherlands)
12:15Exhibition & Lunch
12:30Flash Poster Presentations (12:30-13:10)
Session Chair
Prof. Stuart CONWAY
(UNIVERSITY OF OXFORD, Oxford, United Kingdom)
2.1 Peptides: Pushing Permeability and Bioavailability Beyond the Rule of 5 (ACSMEDI Session)2.2 Recent Progress in the Treatment of Ophthalmological Diseases2.3 Molecular Tissue Targeting
13:15Session Chairs
Dr Peter CHENG (BRISTOL-MYERS SQUIBB, New York, United States)
Dr Claudio MAPELLI (BRISTOL-MYERS SQUIBB, United States)
13:15Session Chair
Dr Yves P. AUBERSON
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland)
13:15Session Chair
Dr Malin LEMURELL
(ASTRAZENECA, Gothenburg, Sweden)
13:20Peptides and Peptidomimetics: Overcoming Problems of Activity, Selectivity and Bioavailability of Integrin Ligands
Dr Horst KESSLER
(TECHNISCHE UNIVERSITÄT MÜNCHEN, Garching, Germany)
13:20Molecular Pharmacodynamics of Visual Cycle Modulators in Protection Against Retinal Degeneration
Prof. Krzysztof PALCZEWSKI
(CASE WESTERN RESERVE UNIVERSITY, Cleveland, United States)
13:20Ligand-Targeted Therapeutic and Imaging Agents for Multiple Human Diseases
Prof. Philip S. LOW
(PURDUE UNIVERSITY, West Lafayette, United States)
14:00Discovery & Optimzation of Clips-Constrained Bicyclic Peptides (2clips) Using Pepscan Peptide Arrays
Prof. Peter TIMMERMAN
(PEPSCAN THERAPEUTICS, Lelystad, The Netherlands)
14:00The Back of The Eye: Treatment Challenges and Opportunities
Dr Muneto MOGI
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Cambridge, United States)
14:00Peptide Drugs to Target GPCR - State of the Art and Innovative Applications
14:20Phage-Encoded Combinatorial Chemical Libraries Based on Bicyclic Peptides
Prof. Christian HEINIS
(ECOLE POLYTECHNIQUE FÉDÉRALE DE LAUSANNE (EPFL), Lausanne, Switzerland)
14:20Regorafenib Eye Drops for Wet AMD – Challenges in Translatability of Preclinical Data Into Clinical Efficacy
Dr Michael BÖTTGER
(BAYER PHARMA, Wuppertal, Germany)
14:20The Development of Pyrrolobenzodiazepine in Antibody Drug Conjugates
Dr Philip HOWARD
(SPIROGEN LTD, London, United Kingdom)
14:40Attempts at Oral Delivery of a Series of Short Unnatural Peptides: Still Like Pushing a Camel Through the Eye of a Needle?
Dr Claudio MAPELLI
(BRISTOL-MYERS SQUIBB, United States)
14:40Systemic Administration of an Allosteric GSK-3 Inhibitor Delays Photoreceptor Cell Death and Preserves Visual Function in a Retinitis Pigmentosa Mouse Model
Prof. Ana MARTINEZ
(CSIC, Madrid, Spain)
14:40Photoisomerisable Allosteric Modulators Allow a Fine Control of mGlu Receptors with Light in Vivo (EFMC-YMCS Presentation Prize)
Mr Xavier GÓMEZ-SANTACANA
(VRIJE UNIVERSITEIT AMSTERDAM, Amsterdam, The Netherlands)
15:00Exhibition & Coffee
3. First Time Disclosures
15:30Session Chair
Dr David WITTY
(CONVERGENCE PHARMACEUTICALS, United Kingdom)
15:35Discovery and Development of the Highly Potent, Highly Selective Cathepsin S Inhibitor RG7625 for the Treatment of Autoimmune Diseases
Dr Wolfgang HAAP
(F. HOFFMANN-LA ROCHE, Basel, Switzerland)
16:05First Time Disclosure of a Development Candidate to Treat Severe Acute Pancreatitis through a Drug Discovery Partnership Between GSK and the University of Edinburgh
Dr John LIDDLE
(GLAXOSMITHKLINE, Stevenage, United Kingdom)
16:35Discovery of AZD3241 is a Potent and Selective Myeloperoxidase Inhibitor for the Treatment of Neurodegenerative Disorders
Dr Jörg HOLENZ
(ASTRAZENECA NEUROSCIENCE, Collegeville, United States)
17:05Discovery of the HCV NS5A Inhibitor MK-8408 (RUZASVIR)
Dr Joe KOZLOWSKI
(MERCK, SHARP & DOHME, Rahway, United States)
17:35Poster Session (even numbers) with drinks
19:30End of the day
Tuesday August 30, 2016
08:30PROUS INSTITUTE-OVERTON AND MEYER AWARD FOR NEW TECHNOLOGIES IN DRUG DISCOVERY
Nanobody-Enabled HTS for the Discovery of GPCR Agonists
Prof. Jan STEYAERT
(VUB, Brussels, Belgium)
Chair
Dr Josep Jr. PROUS
(PROUS INSTITUTE FOR BIOMEDICAL RESEARCH, Barcelona, Spain)
09:15EFMC Prize Ceremony
Prof. Rui MOREIRA
(UNIVERSITY OF LISBON, Lisbon, Portugal)
09:20EFMC Prize for a Young Medicinal Chemist in Industry
Inhibition of the COP9 Signalosome as a Novel Approach to Treat Cancer”
Dr Jean QUANCARD
(NOVARTIS, Basel, Switzerland)
09:40EFMC Prize for a Young Medicinal Chemist in Academia
Sigma Hole Bonding in Kinase Drug Discovery
Prof. Frank BÖCKLER
(EBERHARD-KARLS UNIVERSITY TUEBINGEN, Tübingen, Germany)
10:00Exhibition & Coffee
4.1 Making Small Molecule Synthesis Simpler, General, and Automatic4.2 Hot Topics in Cardiovascular Diseases Research4.3 Neglected Diseases
10:30Session Chair
Prof. Martin D. BURKE
(UNIVERSITY OF ILLINOIS, Urbana, United States)
10:30Session Chair
Dr Susanne ROEHRIG
(BAYER HEALTHCARE, Wuppertal, Germany)
10:30Session Chair
Dr Timothy MILES
(GSK, Madrid, Spain)
10:35Towards a More Generalized and Automated Approach for Small Molecule Synthesis
Prof. Martin D. BURKE
(UNIVERSITY OF ILLINOIS, Urbana, United States)
10:35Discovery of a First-in-Class PAR4 Antagonist as a Novel Antithrombotic
Dr Scott PRIESTLEY
(BRISTOL-MYERS SQUIBB, Hopewell, United States)
10:35Utilization of Novel Benzoxaboroles as Drug Candidates to Treat Neglected Tropical Diseases
Dr Robert T. JACOBS
(ANACOR PHARMACEUTICALS, Palo Alto, California, United States)
11:15Robot Scientists, the Replication Crisis, and Cancer
Prof. Ross KING
(UNIVERSITY OF MANCHESTER, Manchester, United Kingdom)
11:15Discovery of Novel LPA1 Antagonist: Design and SAR Studies
Dr Masahiko TERAKADO
(ONO PHARMACEUTICAL, Osaka, Japan)
11:15The Development of DDD853651; a Potential Candidate for the Treatment of Visceral Leishmaniasis
Dr Michael THOMAS
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom)
11:35Identifying Synthetic Opportunities Using Chemplanner - How Computers Assist Chemists in Covering a Greater Synthetic Space
Dr Orr RAVITZ
(WILEY, Chichester, United Kingdom)
11:35Discovery of Clinical Candidate Ribuvaptan, a Dual Acting Vasopressin V1a/V2 Receptor Antagonist for the Treatment of Heart Failure
Dr Carsten SCHMECK
(BAYER, Wuppertal, Germany)
11:35Pharmacological Reversion of Antibiotic Resistance in Mycobacterium Tuberculosis : Design of SMART Trojan Molecules to Reprogram The Bacteria
Prof. Benoit DEPREZ
(UNIVERSITY OF LILLE 2, Lille, France)
11:55The evoSpace - A Synthesis-Driven Environment that Finds Accessible, Well-Behaved Compounds by Design
Dr Marcus GASTREICH
(BIOSOLVEIT, St. Augustin, Germany)
11:55Classification of Adamts Binding Sites: the First Step Toward Selective ADAMTS7 Inhibitors
Mrs Michaela MÜLLER
(UNIVERSITÄT ZU LÜBECK, Lübeck, Germany)
11:55The Discovery and Development of Novel Macrofilaricidal Agents for the Treatment of Onchocerciasis and Lymphatic Filariasis
Dr Thomas VON GELDERN
(ABBVIE, Chicago, United States)
12:15Exhibition & Lunch
12:15Advion Lunch Workshop: Compact Mass Spectrometry - The User's Perspective (12:15-13:45)
12:30Flash Poster Presentations (12:30-13:10)
Session Chair
Dr Sharan BAGAL
(ASTRAZENECA, Cambridge, United Kingdom)
5.1 Synthesis Driven Innovation5.2 Modulation of Protein-Protein Interactions - Novel Opportunities for Drug Discovery 5.3 Current Advances and Future Opportunities for the Treatment of Neurodegenerative Disorders
13:15Session Chair
Dr Jesus EZQUERRA
(LABORATORIOS LILLY, Alcobendas, Spain)
13:15Session Chair
Dr Christian OTTMANN
(EINDHOVEN UNIVERSITY OF TECHNOLOGY, Eindhoven, The Netherlands)
13:15Session Chair
Dr Theodora CALOGEROPOULOU
(NATIONAL HELLENIC RESEARCH FOUNDATION, Athens, Greece)
13:20Expanding the Macrocycle Chemical Space
Prof. Alexander DÖMLING
(UNIVERSITY OF GRONINGEN, Groningen, The Netherlands)
13:20Validating New Epigenetic Targets by Selective Protein Interaction Inhibitors of Bromodomains
Prof. Stefan KNAPP
(GOETHE UNIVERSITY FRANKFURT, Frankfurt am Main, Germany)
13:20Possibilities and Pitfalls: Disease Modifying Drugs for Alzheimer's Disease
Dr Eric KARRAN
(FOUNDATIONAL NEUROSCIENCE CENTER, ABBVIE, Cambridge, United States)
14:00Potent and Highly Selective Bromodomain Ligands… a Platform for Reaction Discovery
Prof. Cristina NEVADO
(UNIVERSITY OF ZURICH, Zurich, Switzerland)
14:00Releasing the Brake on Apoptosis. Discovery of Bcl-2 Family Protein Inhibitors
Dr Steven ELMORE
(ABBVIE, North Chicago, United States)
14:00Tackling Neurodegenerative Diseases Through Multi-Target and Theranostic Small Molecules
Prof. Maria Laura BOLOGNESI
(UNIVERSITY OF BOLOGNA, Bologna, Italy)
14:20Nucleophilic Boron for the Preparation of Highly Functionalized Small Rings
Prof. Mariola TORTOSA
(AUTONOMOUS UNIVERSITY OF MADRID, Madrid, Spain)
14:20DNA-Encoded Chemical Library for Protein-Protein Interactions
Dr Jin LI
(HITGEN LTD , Chengdu, Sichuan, China)
14:20Discovery of Brain-Penetrable LpPLA2 Inhibitor for Alzheimer’s Disease
Dr Xiaomin ZHANG
(GLAXOSMITHKLINE, Shanghai, China)
14:40Rapid Composition of Tricyclic Spiranoid Lactones: Access to Natural Frames and Application in Selective Silencing of the Pain Receptor TRPV1
Dr Dmitry TSVELIKHOVSKY
(THE HEBREW UNIVERSITY OF JERUSALEM, Jerusalem, Israel)
14:40From Fragment to in vivo Activity for a Challenging PPI Target: the Discovery of Potent Inhibitors of the KEAP1-NRF2 Interaction
Dr David NORTON
(ASTEX PHARMACEUTICALS, Cambridge, United Kingdom)
14:40Modulation of RS67,333: from a 5-HT4R Partial Agonist to the Identification of Several Promising Multi-Target Directed Ligands for Alzheimer's Disease
Prof. Christophe ROCHAIS
(UNIVERSITY OF CAEN, Caen, France)
15:00Exhibition & Coffee
15:30Robotics, Artificial Intelligence, and Medicinal Chemistry: A Look Into the Future
Dr Derek LOWE
(VERTEX PHARMACEUTICALS, Cambridge, United States)
Chair
Dr Matthew TOZER
(CONSULTANT, Cambridge, United Kingdom)
16:15Poster Session (odd numbers) with drinks
18:15Close Poster Session
19:00Public Lecture
21:30End of the day
Wednesday August 31, 2016
08:30IUPAC-RICHTER PRIZE
The Discovery of Sofosbuvir: A Breakthrough Curative Therapy for Hepatitis C
Dr Michael SOFIA
(ARBUTUS BIOPHARMA, Doylestown, PA, United States)
Chair
Dr Janos FISCHER
(RICHTER PLC, Budapest, Hungary)
09:15DNA-Encoded Chemical Libraries
Prof. Dario NERI
(ETH ZÜRICH, Zürich, Switzerland)
Chair
10:00Exhibition & Coffee
6.1 Big Data in Medicinal Chemistry6.2 New Horizons in GPCR-targeted Medicinal Chemistry6.3 Novel Approaches to the Treatment of Cancer
10:30Session Chair
Prof. Andrew HOPKINS
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom)
10:30Session Chair
Prof. Christa MÜLLER
(UNIVERSITY OF BONN, Bonn, Germany)
10:30Session Chair
Dr Jonathan BENNETT
(MERCK, SHARP & DOHME, Boston, United States)
10:35Big Dada in Medicinal Chemistry?
Prof. Gisbert SCHNEIDER
(ETH ZÜRICH, Zürich, Switzerland)
10:35Identification of Allosteric Inhibitors of GPCRs Using SBDD
Dr Miles CONGREVE
(HEPTARES, Welwyn Garden City, United Kingdom)
10:35Small Molecule Approaches to Immune-Modulation in Cancer
Dr Ronan O'HAGAN
(MERCK, SHARP & DOHME, Boston, United States)
11:15Exploiting Linked Open Data - Transporter Profiling and Beyond
Prof. Gerhard ECKER
(UNIVERSITY OF VIENNA, Vienna, Austria)
11:15Medicinal Chemistry of Purinergic Signalling: Targets and Drugs for the Immunotherapy of Cancer
Prof. Christa MÜLLER
(UNIVERSITY OF BONN, Bonn, Germany)
11:15The Identification of GSK2879552, a Mechanism Based Irreversible Inhibitor of the Histone Lysine Demethylase LSD1
Dr Neil W. JOHNSON
(GLAXOSMITHKLINE, Collegeville, United States)
11:35Mining Structural Protein-Ligand Interactions to Navigate Medicinal Chemistry Space
Dr Chris DE GRAAF
(VU UNIVERSITY AMSTERDAM, Cambridge, United Kingdom)
11:35Targeting Long-Chain Fatty Acid Receptors FFA1 and FFA4 for Treatment of Metabolic Diseases
Prof. Trond ULVEN
(UNIVERSITY OF SOUTHERN DENMARK, København Ø, Denmark)
11:35Discovery of AG-120 – A First-in-class Inhibitor of IDH1 Mutant Enzymes for the Treatment of Cancers Harboring IDH1 Mutations
Dr Janeta POPOVICI-MULLER
(AGIOS PHARMACEUTICALS, United States)
11:55Non Coding RNA as a Small Molecule Druggable Target
Dr Graham SMITH
(MERCK, SHARP & DOHME, Boston, United States)
11:55Optimising Membrane Interactions to Achieve Duration of Action for Inhaled Drug Candidates
Dr Mark HEALY
(NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Cambridge, United States)
11:55Targeting the Janus-Faced Nature of IDO1 in Immuno-Oncology
Prof. Antonio MACCHIARULO
(UNIVERSITY OF PERUGIA, Perugia, Italy)
12:15Exhibition & Lunch
12:15Chemical Computing Group Lunch Workshop: Stucture-Based Drug Design and Ligand Modification (12:15-13:45)
7.1 Emerging Topics 7.2 Innovation in Kinase Drug Discovery7.3 The Importance of Solute Carrier Transporters in Drug Discovery (MedChemComm Session)
13:15Session Chair
Prof. Antonello MAI
(UNIVERSITY OF ROME, Rome, Italy)
13:15Session Chair
Dr Christel MENET
(CONFO THERAPEUTICS, Brussels, Belgium)
13:15Session Chair
Dr David HEPWORTH
(PFIZER MEDICINES DESIGN, Cambridge, United States)
13:20Phenotypic Screening for the Discovery of Novel Molecules for Therapeutic Heart Regeneration
Dr Alleyn T. PLOWRIGHT
(ASTRAZENECA, Frankfurt-Am-Main, Germany)
13:20Broad Multiparametric Profiling of Kinase Inhibitors
Dr Herman VAN VLIJMEN
(JANSSEN, Beerse, Belgium)
13:20Solute Carriers, Metabolism and Drug Response: a Magic Triangle
Prof. Giulio SUPERTI-FURGA
(RESEARCH CENTER FOR MOLECULAR MEDICINE (CEMM), Vienna, Austria)
13:45How can Advances in Cryo-Electron Microscopy Revolutionize Medicinal Chemistry?
Dr Neil RANSON
(UNIVERSITY OF LEEDS, Leeds, United Kingdom)
14:00New Pseudokinase Drug Targets in the Human Kinome
Prof. Patrick EYERS
(UNIVERSITY OF LIVERPOOL, Liverpool, United Kingdom)
14:00The Design and Evaluation of URAT1 Inhibitors for the Treatment of Hyperuricemia and Gout
Dr David HEPWORTH
(PFIZER MEDICINES DESIGN, Cambridge, United States)
14:10Interaction of 4,5,6,7-Tetrahydrobenzo[1,2-D]Thiazoles with the Cellular Chaperone HSP90 as a Potential Pathway to Inhibit Hepatitis C Virus Replication
Dr Tihomir TOMASIC
(UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia)
14:20Switch Control Inhibitors: an Advance in Type II Kinase Inhibition
Dr Daniel FLYNN
(DECIPHERA PHARMACEUTICALS, Lawrence, United States)
14:20The Cellular Uptake of Pharmaceutical Drugs is Transporter-Mediated - A Problem not of Biophysics but of Systems Biology
Prof. Douglas KELL
(UNIVERSITY OF MANCHESTER, Manchester, United Kingdom)
14:35RSC Prize Lecture:
Advanced Chemical Genetics for Epigenetics: Bump and Hole and PROTACs (2016 MedChemComm Emerging Investigator Lectureship)
Prof. Alessio CIULLI
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom)
14:40First Disclosure of CDZ173 - Discovery of a New Generation of Potent and Selective PI3K Delta Inhibitors for Autoimmune and Inflammatory Diseases
Dr Nicolas SOLDERMANN
(NOVARTIS, Basel, Switzerland)
14:40Drug Targets in the Solute Carrier Classification (SLC)
Dr Daniela DIGLES
(UNIVERSITY OF VIENNA, Vienna, Austria)
15:00Excursions
20:00Banquet
Thursday September 1, 2016
8.1 Covalent Drugs Revisited (AFMC Session) 8.2 Novel Molecular Probes for in Vivo Chemistry8.3 Recent Advances on Approaches to Treat Pain
08:30Session Chair
Prof. Zhengying PAN
(PEKING UNIVERSITY, Shenzhen, China)
08:30Session Chair
Dr Marc ROBILLARD
(TAGWORKS PHARMACEUTICALS, Eindhoven, The Netherlands)
08:30Session Chair
Dr Alan BROWN
(STRATIFIED MEDICAL, Deal, United Kingdom)
08:35Targeted Covalent Inhibitors of Bruton's Tyrosine Kinases - Design, Evaluation and Follow-up
Prof. Zhengying PAN
(PEKING UNIVERSITY, Shenzhen, China)
08:35Antibody Imaging and Therapy Using in Vivo Click and Click-to-Release Strategies
Dr Marc ROBILLARD
(TAGWORKS PHARMACEUTICALS, Eindhoven, The Netherlands)
08:35The Painful Reality of Drug Discovery and Development
Dr Paul BESWICK
(UNIVERSITY OF SUSSEX, Brighton, United Kingdom)
09:15Chemical Biology Efforts in Cancer Drug Discovery
Prof. Huchen ZHOU
(SHANGHAI JIAO TONG UNIVERSITY, Shanghai, China)
09:15Novel Antibody-Tetrazine Conjugate for Breast Cancer Imaging
Mr Eduardo RUIVO
(UNIVERSITY OF ANTWERP, Antwerp, Belgium)
09:15Challenges in the Discovery of Sigma-1 Receptor Antagonists for the Treatment of Pain
Dr Carmen ALMANSA
(ESTEVE, Barcelone, Spain)
09:35Advances in the Development of Covalent EGFR Inhibitors: from Early Hits to Osimertinib
Dr Gail WRIGLEY
(ASTRAZENECA, Macclesfield, United Kingdom)
09:35Atypical Bile Acids as Chemical Probes for Diagnosis and Therapy Monitoring of Progressive Cholestatic Liver Disease in HSD3B7 Patients
Prof. Antimo GIOIELLO
(UNIVERSITY OF PERUGIA, Perugia, Italy)
09:35Functionally Irreversible Non-Covalent Inhibitors of FAAH: a Safer Approach?
Dr Philippe NANTERMET
(MERCK & CO. INC (MSD), West Point, United States)
09:55Rapid Discovery of Potent and Selective Covalent Inhibitors via Covalent Docking
Dr Nir LONDON
(THE WEIZMANN INSTITUTE OF SCIENCE, Rehovot, Israel)
09:55RSC Prize Lecture:
Chemical Pharmacology of Protein Conjugates and Natural Products (2016 Chem Soc Rev Emerging Investigator Lectureship)
Dr Goncalo BERNARDES
(INSTITUTO DE MEDICINA MOLECULAR, PORTUGAL & UNIVERSITY OF CAMBRIDGE, Cambridge, United Kingdom)
09:55Towards Low-Risk Painkillers: Human Dipeptidyl Peptidase III (hDPPIII) as a Novel Target for Therapeutic Pain Intervention
Ms Shalinee JHA
(GRAZ UNIVERSITY OF TECHNOLOGY, Graz, Austria)
10:15Exhibition & Coffee
9.1 High Throughput Screening Strategies to Obtain High Quality Leads9.2 Late Breaking News9.3 Showcase Brazil
10:45Session Chair
Prof. Jonathan BAELL
(MONASH UNIVERSITY, Parkville, Australia)
10:45Session Chair
Dr Luc VAN HIJFTE
(SCT & NOVALIX, Nijmegen, The Netherlands)
10:45Session Chair
Prof. Andrei LEITÃO
(UNIVERSITY OF SAO PAULO, São Carlos, Brazil)
10:50Histone Acetyltransferase Inhibitors, from Screening to Optimization - a Tricky Track
Prof. Jonathan BAELL
(MONASH UNIVERSITY, Parkville, Australia)
10:50Discovery of PF-06840003, a Novel IDO1 Inhibitor for Cancer Immunotherapy
Dr Stefano CROSIGNANI
(ITEOS THERAPEUTICS SA, Gosselies, Belgium)
10:50Molecular Design, Synthesis and Trypanocidal Activity of Dipeptidyl Nitriles as Cruzain Inhibitors
Prof. Carlos MONTANARI
(UNIVERSITY OF SAO PAULO, Sao Paulo, Brazil)
11:30Direct and Synergistic Inhibition of The HCV NS5A Protein
Dr Makonen BELEMA
(BRISTOL-MYERS SQUIBB, Wallingford, United States)
11:15Driving Tumors into Mitotic Catastrophe - Lead Generation of MPS1 Inhibitors Leading to Two Clinical Candidates BAY 1161909 and BAY 1217389
Dr Volker K. SCHULZE
(BAYER PHARMA AG, Berlin, Germany)
11:30Research, Development & Innovation at Aché Laboratórios Farmacêuticos
Dr Cristiano GUIMARAES
(ACHÉ PHARMACEUTICAL, Brazil)
11:50Discovery of In Vivo Active and Selective Diacylglycerol Lipase-Alpha Inhibitors
Dr Mario VAN DER STELT
(LEIDEN UNIVERSITY, Leiden, The Netherlands)
11:40Delivering First-in-Class In Vitro Chemical Probes Against Poly (ADP Ribose) Glycohydrolase (PARG)
Dr Allan JORDAN
(CANCER RESEARCH UK MANCHESTER INSTITUTE, Manchester, United Kingdom)
11:50Effects of Novel Acylhydrazones Derived From 4-Quinolone on the Acetylcholinesterase Activity and Aβ42 Peptide Fibrils Formation
Mrs Gisele SILVESTRE DA SILVA
(UNICAMP, São Paulo, Brazil)
12:10Anti-Wolbachia (A·WOL) Drug Discovery: Novel Hit Finding Via Ligand Based Virtual Screening Combined With HTS
Dr Neil G BERRY
(UNIVERSITY OF LIVERPOOL, Liverpool, United Kingdom)
12:05Discovery of Ubrogepant (MK-1602): a Potent, Selective and Orally Bioavailable CGRP Receptor Antagonist for the Acute Treatment of Migraine
Dr Mark FRALEY
(MERCK, SHARP & DOHME, West Point, United States)
12:10Antiplatelet and Antithrombotic Activity of 1,2,5-Oxadiazole-2-N-Oxide Derivatives
Mr Luiz Antonio DUTRA
(STATE UNIVERSITY OF SAO PAULO - UNESP, Araraquara, Brazil)
12:30Heterocycles and Medicinal Chemistry: The Importance of Innovative Synthesis 
Dr Anthony WOOD
(PFIZER, Waltham, United States)
Chair
Dr Franz VON NUSSBAUM
(BAYER PHARMA, Berlin, Germany)
13:15Closing Remarks, Poster Prizes and Welcome to EFMC-ISMC 2018
Prof. Marko ANDERLUH
(UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia)

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