EFMC-ISMC 2016

XXIV EFMC International Symposium on Medicinal Chemistry

 Manchester, UK    August 28

Programme Schedule


13:30

Registration

16:00

Opening Ceremony

Dr Phil JONES
UNIVERSITY OF DUNDEE, Glasgow, United Kingdom

16:20

Science, 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

17:05

The 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

17:30

Award Ceremony

Prof. Koen AUGUSTYNS
UNIVERSITY OF ANTWERP, Antwerp, Belgium

17:50

NAUTA 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

18:40

Late-Stage Fluorination

Prof. Tobias RITTER
MAX-PLANCK-INSTITUT FÜR KOHLENFORSCHUNG, Mulheim, Germany

Chair

Dr Anette GRAVEN SAMS
H. LUNDBECK, Valby, Denmark

19:25

Welcome Reception Sponsored by Concept Life Sciences

08:30

UCB-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

09:15

Cross-Coupling Approaches to Saturated N-Heterocycles

Prof. Jeffrey BODE
ETH ZÜRICH, Zürich, Switzerland

Chair

Dr Karin BRINER
NOVARTIS, Cambridge, United States

10:00

Exhibition & Coffee

10:30

Start of sessions

1.1 Intramolecular Hydrogen Bonding and its Impact in Drug Design and Discovery (ACSMEDI Session)
1.2 Drug Discovery Approaches Toward Targeting Ras
1.3 New Antibacterials. An Update
1.1 Intramolecular Hydrogen Bonding and its Impact in Drug Design and Discovery (ACSMEDI Session)
10:30
Session Chairs
Dr Amjad ALI
MERCK & CO. INC., Kenilworth, United States
Dr Tanweer KHAN
MERCK, SHARP & DOHME, Kenilworth, United States
10:35
The Need of Implementing Intramolecular Hydrogen Bonding (IMHB) Considerations in Drug Discovery and How to do it
Prof. Giulia CARON
UNIVERSITY OF TORINO, Torino, Italy
11:15
Intramolecular Hydrogen Bond Expectations in Medicinal Chemistry
Dr Fabrizio GIORDANETTO
D.E. SHAW RESEARCH LLC, New York, United States
11:35
Intramolecular Hydrogen Bonding as a Design Element in Medicinal Chemistry
Dr Bernd KUHN
F. HOFFMANN-LA ROCHE, Basel, Switzerland
11:55
Intramolecular Hydrogen Bonds in the Design of CREBBP Bromodomain Ligands
Prof. Stuart CONWAY
UNIVERSITY OF OXFORD, Oxford, United Kingdom
1.2 Drug Discovery Approaches Toward Targeting Ras
10:30
Session Chair
Dr Joachim RUDOLPH
GENENTECH, South San Francisco, United States
10:35
Studying Ciliary Trafficking and How it Leads to RAS Drug Candidates
Prof. Alfred WITTINGHOFER
MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany
11:15
Chemical Biological Modulation of KRas-Signaling
Prof. Herbert WALDMANN
MAX PLANCK INSTITUTE OF MOLECULAR PHYSIOLOGY, Dortmund, Germany
11:35
Inhibition of Prenylated KRAS: Tools to Discover and Characterize RAS Ligands
Dr Johanna JANSEN
NOVARTIS, Emeryville, United States
11:55
Small Molecule Binding Sites on the RAS: SOS Complex Can Be Exploited for Inhibition of RAS Activation
Dr. Jon WINTER-HOLT
ASTRAZENECA, Macclesfield, United Kingdom
1.3 New Antibacterials. An Update
10:30
Session Chair
Prof. Malcolm PAGE
JACOBS UNIVERSITY, Bremen, Germany
10:35
New Antibacterial Agents in the Pipeline
Dr Eric DESARBRE
BASILEA PHARMACEUTICA, Basel, Switzerland
11:15
Mechanistic and Inhibition Studies on Metallo-Beta-Lactamases
Prof. Christopher J. SCHOFIELD
UNIVERSITY OF OXFORD, Oxford, United Kingdom
11:35
Enterobactin-Dependent Iron Uptake Pathway as a Gate for Antibiotic Trojan Horse Strategies Against Pseudomonas Aeruginosa
Dr Gaëtan MISLIN
UNIVERSITY OF STRASBOURG, Illkirch-Graffenstaden, France
11:55
Exploring 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
12:15

Exhibition & Lunch

12:30

Flash Poster Presentations (12:30-13:10)

Session Chair

Prof. Stuart CONWAY
UNIVERSITY OF OXFORD, Oxford, United Kingdom

13:15

Start of sessions

2.1 Peptides: Pushing Permeability and Bioavailability Beyond the Rule of 5 (ACSMEDI Session)
2.2 Recent Progress in the Treatment of Ophthalmological Diseases
2.3 Molecular Tissue Targeting
2.1 Peptides: Pushing Permeability and Bioavailability Beyond the Rule of 5 (ACSMEDI Session)
13:15
Session Chairs
Dr Peter CHENG
BRISTOL-MYERS SQUIBB, New York, United States
Dr Claudio MAPELLI
BRISTOL-MYERS SQUIBB, United States
13:20
Peptides and Peptidomimetics: Overcoming Problems of Activity, Selectivity and Bioavailability of Integrin Ligands
Dr Horst KESSLER
TECHNISCHE UNIVERSITÄT MÜNCHEN, Garching, Germany
14:00
Discovery & Optimzation of Clips-Constrained Bicyclic Peptides (2clips) Using Pepscan Peptide Arrays
Prof. Peter TIMMERMAN
PEPSCAN THERAPEUTICS, Lelystad, The Netherlands
14:20
Phage-Encoded Combinatorial Chemical Libraries Based on Bicyclic Peptides
Prof. Christian HEINIS
ECOLE POLYTECHNIQUE FÉDÉRALE DE LAUSANNE (EPFL), Lausanne, Switzerland
14:40
Attempts 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
2.2 Recent Progress in the Treatment of Ophthalmological Diseases
13:15
Session Chair
Dr Yves P. AUBERSON
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Basel, Switzerland
13:20
Molecular Pharmacodynamics of Visual Cycle Modulators in Protection Against Retinal Degeneration
Prof. Krzysztof PALCZEWSKI
CASE WESTERN RESERVE UNIVERSITY, Cleveland, United States
14:00
The Back of The Eye: Treatment Challenges and Opportunities
Dr Muneto MOGI
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Cambridge, United States
14:20
Regorafenib Eye Drops for Wet AMD – Challenges in Translatability of Preclinical Data Into Clinical Efficacy
Dr Michael BÖTTGER
BAYER PHARMA, Wuppertal, Germany
14:40
Systemic 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
2.3 Molecular Tissue Targeting
13:15
Session Chair
Dr Malin LEMURELL
ASTRAZENECA, Gothenburg, Sweden
13:20
Ligand-Targeted Therapeutic and Imaging Agents for Multiple Human Diseases
Prof. Philip S. LOW
PURDUE UNIVERSITY, West Lafayette, United States
14:00
Peptide Drugs to Target GPCR - State of the Art and Innovative Applications
14:20
The Development of Pyrrolobenzodiazepine in Antibody Drug Conjugates
Dr Philip HOWARD
SPIROGEN LTD, London, United Kingdom
14:40
Photoisomerisable 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
15:00

Exhibition & Coffee

15:30

Start of sessions

3. First Time Disclosures
3. First Time Disclosures
15:30
Session Chair
Dr David WITTY
CONVERGENCE PHARMACEUTICALS, United Kingdom
15:35
Discovery 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
16:05
First 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
16:35
Discovery of AZD3241 is a Potent and Selective Myeloperoxidase Inhibitor for the Treatment of Neurodegenerative Disorders
Dr Jörg HOLENZ
ASTRAZENECA NEUROSCIENCE, Collegeville, United States
17:05
Discovery of the HCV NS5A Inhibitor MK-8408 (RUZASVIR)
Dr Joe KOZLOWSKI
MERCK, SHARP & DOHME, Rahway, United States
17:35

Poster Session (even numbers) with drinks

19:30

End of the day

08:30

PROUS 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

09:15

EFMC Prize Ceremony

Prof. Rui MOREIRA
UNIVERSITY OF LISBON, Lisbon, Portugal

09:20

EFMC 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

09:40

EFMC Prize for a Young Medicinal Chemist in Academia
Sigma Hole Bonding in Kinase Drug Discovery

Prof. Frank BÖCKLER
EBERHARD-KARLS UNIVERSITY TUEBINGEN, Tübingen, Germany

10:00

Exhibition & Coffee

10:30

Start of sessions

4.1 Making Small Molecule Synthesis Simpler, General, and Automatic
4.2 Hot Topics in Cardiovascular Diseases Research
4.3 Neglected Diseases
4.1 Making Small Molecule Synthesis Simpler, General, and Automatic
10:30
Session Chair
Prof. Martin D. BURKE
UNIVERSITY OF ILLINOIS, Urbana, United States
10:35
Towards a More Generalized and Automated Approach for Small Molecule Synthesis
Prof. Martin D. BURKE
UNIVERSITY OF ILLINOIS, Urbana, United States
11:15
Robot Scientists, the Replication Crisis, and Cancer
Prof. Ross KING
UNIVERSITY OF MANCHESTER, Manchester, United Kingdom
11:35
Identifying Synthetic Opportunities Using Chemplanner - How Computers Assist Chemists in Covering a Greater Synthetic Space
Dr Orr RAVITZ
WILEY, Chichester, United Kingdom
11:55
The evoSpace - A Synthesis-Driven Environment that Finds Accessible, Well-Behaved Compounds by Design
Dr Marcus GASTREICH
BIOSOLVEIT, St. Augustin, Germany
4.2 Hot Topics in Cardiovascular Diseases Research
10:30
Session Chair
Dr Susanne ROEHRIG
BAYER HEALTHCARE, Wuppertal, Germany
10:35
Discovery of a First-in-Class PAR4 Antagonist as a Novel Antithrombotic
Dr Scott PRIESTLEY
BRISTOL-MYERS SQUIBB, Hopewell, United States
11:15
Discovery of Novel LPA1 Antagonist: Design and SAR Studies
Dr Masahiko TERAKADO
ONO PHARMACEUTICAL, Osaka, Japan
11:35
Discovery of Clinical Candidate Ribuvaptan, a Dual Acting Vasopressin V1a/V2 Receptor Antagonist for the Treatment of Heart Failure
Dr Carsten SCHMECK
BAYER, Wuppertal, Germany
11:55
Classification of Adamts Binding Sites: the First Step Toward Selective ADAMTS7 Inhibitors
Mrs Michaela MÜLLER
UNIVERSITÄT ZU LÜBECK, Lübeck, Germany
4.3 Neglected Diseases
10:30
Session Chair
Dr Timothy MILES
GSK, Madrid, Spain
10:35
Utilization of Novel Benzoxaboroles as Drug Candidates to Treat Neglected Tropical Diseases
Dr Robert T. JACOBS
ANACOR PHARMACEUTICALS, Palo Alto, California, United States
11:15
The Development of DDD853651; a Potential Candidate for the Treatment of Visceral Leishmaniasis
Dr Michael THOMAS
UNIVERSITY OF DUNDEE, Dundee, United Kingdom
11:35
Pharmacological 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
11:55
The Discovery and Development of Novel Macrofilaricidal Agents for the Treatment of Onchocerciasis and Lymphatic Filariasis
Dr Thomas VON GELDERN
ABBVIE, Chicago, United States
12:15

Exhibition & Lunch

12:15

Advion Lunch Workshop: Compact Mass Spectrometry - The User's Perspective (12:15-13:45)

12:30

Flash Poster Presentations (12:30-13:10)

Session Chair

Dr Sharan BAGAL
ASTRAZENECA, Cambridge, United Kingdom

13:15

Start of sessions

5.1 Synthesis Driven Innovation
5.2 Modulation of Protein-Protein Interactions - Novel Opportunities for Drug Discovery
5.3 Current Advances and Future Opportunities for the Treatment of Neurodegenerative Disorders
5.1 Synthesis Driven Innovation
13:15
Session Chair
Dr Jesus EZQUERRA
LABORATORIOS LILLY, Alcobendas, Spain
13:20
Expanding the Macrocycle Chemical Space
Prof. Alexander DÖMLING
UNIVERSITY OF GRONINGEN, Groningen, The Netherlands
14:00
Potent and Highly Selective Bromodomain Ligands… a Platform for Reaction Discovery
Prof. Cristina NEVADO
UNIVERSITY OF ZURICH, Zurich, Switzerland
14:20
Nucleophilic Boron for the Preparation of Highly Functionalized Small Rings
Prof. Mariola TORTOSA
AUTONOMOUS UNIVERSITY OF MADRID, Madrid, Spain
14:40
Rapid 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
5.2 Modulation of Protein-Protein Interactions - Novel Opportunities for Drug Discovery
13:15
Session Chair
Dr Christian OTTMANN
EINDHOVEN UNIVERSITY OF TECHNOLOGY, Eindhoven, The Netherlands
13:20
Validating New Epigenetic Targets by Selective Protein Interaction Inhibitors of Bromodomains
Prof. Stefan KNAPP
GOETHE UNIVERSITY FRANKFURT, Frankfurt am Main, Germany
14:00
Releasing the Brake on Apoptosis. Discovery of Bcl-2 Family Protein Inhibitors
Dr Steven ELMORE
ABBVIE, North Chicago, United States
14:20
DNA-Encoded Chemical Library for Protein-Protein Interactions
Dr Jin LI
HITGEN LTD , Chengdu, Sichuan, China
14:40
From 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
5.3 Current Advances and Future Opportunities for the Treatment of Neurodegenerative Disorders
13:15
Session Chair
Dr Theodora CALOGEROPOULOU
NATIONAL HELLENIC RESEARCH FOUNDATION, Athens, Greece
13:20
Possibilities and Pitfalls: Disease Modifying Drugs for Alzheimer's Disease
Dr Eric KARRAN
FOUNDATIONAL NEUROSCIENCE CENTER, ABBVIE, Cambridge, United States
14:00
Tackling Neurodegenerative Diseases Through Multi-Target and Theranostic Small Molecules
Prof. Maria Laura BOLOGNESI
UNIVERSITY OF BOLOGNA, Bologna, Italy
14:20
Discovery of Brain-Penetrable LpPLA2 Inhibitor for Alzheimer’s Disease
Dr Xiaomin ZHANG
GLAXOSMITHKLINE, Shanghai, China
14:40
Modulation 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
15:00

Exhibition & Coffee

15:30

Robotics, 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

16:15

Poster Session (odd numbers) with drinks

18:15

Close Poster Session

19:00

Public Lecture

21:30

End of the day

08:30

IUPAC-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

09:15

DNA-Encoded Chemical Libraries

Prof. Dario NERI
ETH ZÜRICH, Zürich, Switzerland

Chair

10:00

Exhibition & Coffee

10:30

Start of sessions

6.1 Big Data in Medicinal Chemistry
6.2 New Horizons in GPCR-targeted Medicinal Chemistry
6.3 Novel Approaches to the Treatment of Cancer
6.1 Big Data in Medicinal Chemistry
10:30
Session Chair
Prof. Andrew HOPKINS
UNIVERSITY OF DUNDEE, Dundee, United Kingdom
10:35
Big Dada in Medicinal Chemistry?
Prof. Gisbert SCHNEIDER
ETH ZÜRICH, Zürich, Switzerland
11:15
Exploiting Linked Open Data - Transporter Profiling and Beyond
Prof. Gerhard ECKER
UNIVERSITY OF VIENNA, Vienna, Austria
11:35
Mining Structural Protein-Ligand Interactions to Navigate Medicinal Chemistry Space
Dr Chris DE GRAAF
VU UNIVERSITY AMSTERDAM, Cambridge, United Kingdom
11:55
Non Coding RNA as a Small Molecule Druggable Target
Dr Graham SMITH
MERCK, SHARP & DOHME, Boston, United States
6.2 New Horizons in GPCR-targeted Medicinal Chemistry
10:30
Session Chair
Prof. Christa MÜLLER
UNIVERSITY OF BONN, Bonn, Germany
10:35
Identification of Allosteric Inhibitors of GPCRs Using SBDD
Dr Miles CONGREVE
HEPTARES, Welwyn Garden City, United Kingdom
11:15
Medicinal Chemistry of Purinergic Signalling: Targets and Drugs for the Immunotherapy of Cancer
Prof. Christa MÜLLER
UNIVERSITY OF BONN, Bonn, Germany
11:35
Targeting Long-Chain Fatty Acid Receptors FFA1 and FFA4 for Treatment of Metabolic Diseases
Prof. Trond ULVEN
UNIVERSITY OF SOUTHERN DENMARK, København Ø, Denmark
11:55
Optimising Membrane Interactions to Achieve Duration of Action for Inhaled Drug Candidates
Dr Mark HEALY
NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH, Cambridge, United States
6.3 Novel Approaches to the Treatment of Cancer
10:30
Session Chair
Dr Jonathan BENNETT
MERCK, SHARP & DOHME, Boston, United States
10:35
Small Molecule Approaches to Immune-Modulation in Cancer
Dr Ronan O'HAGAN
MERCK, SHARP & DOHME, Boston, United States
11:15
The Identification of GSK2879552, a Mechanism Based Irreversible Inhibitor of the Histone Lysine Demethylase LSD1
Dr Neil W. JOHNSON
GLAXOSMITHKLINE, Collegeville, United States
11:35
Discovery 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
11:55
Targeting the Janus-Faced Nature of IDO1 in Immuno-Oncology
Prof. Antonio MACCHIARULO
UNIVERSITY OF PERUGIA, Perugia, Italy
12:15

Exhibition & Lunch

12:15

Chemical Computing Group Lunch Workshop: Stucture-Based Drug Design and Ligand Modification (12:15-13:45)

13:15

Start of sessions

7.1 Emerging Topics
7.2 Innovation in Kinase Drug Discovery
7.3 The Importance of Solute Carrier Transporters in Drug Discovery (MedChemComm Session)
7.1 Emerging Topics
13:15
Session Chair
Prof. Antonello MAI
UNIVERSITY OF ROME, Rome, Italy
13:20
Phenotypic Screening for the Discovery of Novel Molecules for Therapeutic Heart Regeneration
Dr Alleyn T. PLOWRIGHT
ASTRAZENECA, Frankfurt-Am-Main, Germany
13:45
How can Advances in Cryo-Electron Microscopy Revolutionize Medicinal Chemistry?
Dr Neil RANSON
UNIVERSITY OF LEEDS, Leeds, United Kingdom
14:10
Interaction 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
14:35
RSC 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
7.2 Innovation in Kinase Drug Discovery
13:15
Session Chair
Dr Christel MENET
CONFO THERAPEUTICS, Brussels, Belgium
13:20
Broad Multiparametric Profiling of Kinase Inhibitors
Dr Herman VAN VLIJMEN
JANSSEN, Beerse, Belgium
14:00
New Pseudokinase Drug Targets in the Human Kinome
Prof. Patrick EYERS
UNIVERSITY OF LIVERPOOL, Liverpool, United Kingdom
14:20
Switch Control Inhibitors: an Advance in Type II Kinase Inhibition
Dr Daniel FLYNN
DECIPHERA PHARMACEUTICALS, Lawrence, United States
14:40
First 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
7.3 The Importance of Solute Carrier Transporters in Drug Discovery (MedChemComm Session)
13:15
Session Chair
Dr David HEPWORTH
PFIZER MEDICINES DESIGN, Cambridge, United States
13:20
Solute Carriers, Metabolism and Drug Response: a Magic Triangle
Prof. Giulio SUPERTI-FURGA
RESEARCH CENTER FOR MOLECULAR MEDICINE (CEMM), Vienna, Austria
14:00
The Design and Evaluation of URAT1 Inhibitors for the Treatment of Hyperuricemia and Gout
Dr David HEPWORTH
PFIZER MEDICINES DESIGN, Cambridge, United States
14:20
The 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
14:40
Drug Targets in the Solute Carrier Classification (SLC)
Dr Daniela DIGLES
UNIVERSITY OF VIENNA, Vienna, Austria
15:00

Excursions

20:00

Banquet

08:30

Start of sessions

8.1 Covalent Drugs Revisited (AFMC Session)
8.2 Novel Molecular Probes for in Vivo Chemistry
8.3 Recent Advances on Approaches to Treat Pain
8.1 Covalent Drugs Revisited (AFMC Session)
08:30
Session Chair
Prof. Zhengying PAN
PEKING UNIVERSITY, Shenzhen, China
08:35
Targeted Covalent Inhibitors of Bruton's Tyrosine Kinases - Design, Evaluation and Follow-up
Prof. Zhengying PAN
PEKING UNIVERSITY, Shenzhen, China
09:15
Chemical Biology Efforts in Cancer Drug Discovery
Prof. Huchen ZHOU
SHANGHAI JIAO TONG UNIVERSITY, Shanghai, China
09:35
Advances in the Development of Covalent EGFR Inhibitors: from Early Hits to Osimertinib
Dr Gail WRIGLEY
ASTRAZENECA, Macclesfield, United Kingdom
09:55
Rapid Discovery of Potent and Selective Covalent Inhibitors via Covalent Docking
Dr Nir LONDON
THE WEIZMANN INSTITUTE OF SCIENCE, Rehovot, Israel
8.2 Novel Molecular Probes for in Vivo Chemistry
08:30
Session Chair
Dr Marc ROBILLARD
TAGWORKS PHARMACEUTICALS, Eindhoven, The Netherlands
08:35
Antibody Imaging and Therapy Using in Vivo Click and Click-to-Release Strategies
Dr Marc ROBILLARD
TAGWORKS PHARMACEUTICALS, Eindhoven, The Netherlands
09:15
Novel Antibody-Tetrazine Conjugate for Breast Cancer Imaging
Mr Eduardo RUIVO
UNIVERSITY OF ANTWERP, Antwerp, Belgium
09:35
Atypical 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
09:55
RSC 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
8.3 Recent Advances on Approaches to Treat Pain
08:30
Session Chair
Dr Alan BROWN
STRATIFIED MEDICAL, Deal, United Kingdom
08:35
The Painful Reality of Drug Discovery and Development
Dr Paul BESWICK
UNIVERSITY OF SUSSEX, Brighton, United Kingdom
09:15
Challenges in the Discovery of Sigma-1 Receptor Antagonists for the Treatment of Pain
Dr Carmen ALMANSA
ESTEVE, Barcelone, Spain
09:35
Functionally Irreversible Non-Covalent Inhibitors of FAAH: a Safer Approach?
Dr Philippe NANTERMET
MERCK & CO. INC (MSD), West Point, United States
09:55
Towards 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
10:15

Exhibition & Coffee

10:45

Start of sessions

9.1 High Throughput Screening Strategies to Obtain High Quality Leads
9.2 Late Breaking News
9.3 Showcase Brazil
9.1 High Throughput Screening Strategies to Obtain High Quality Leads
10:45
Session Chair
Prof. Jonathan BAELL
MONASH UNIVERSITY, Parkville, Australia
10:50
Histone Acetyltransferase Inhibitors, from Screening to Optimization - a Tricky Track
Prof. Jonathan BAELL
MONASH UNIVERSITY, Parkville, Australia
11:30
Direct and Synergistic Inhibition of The HCV NS5A Protein
Dr Makonen BELEMA
BRISTOL-MYERS SQUIBB, Wallingford, United States
11:50
Discovery of In Vivo Active and Selective Diacylglycerol Lipase-Alpha Inhibitors
Dr Mario VAN DER STELT
LEIDEN UNIVERSITY, Leiden, The Netherlands
12:10
Anti-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
9.2 Late Breaking News
10:45
Session Chair
Dr Luc VAN HIJFTE
SCT & NOVALIX, Nijmegen, The Netherlands
10:50
Discovery of PF-06840003, a Novel IDO1 Inhibitor for Cancer Immunotherapy
Dr Stefano CROSIGNANI
ITEOS THERAPEUTICS SA, Gosselies, Belgium
11:15
Driving 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
11:40
Delivering First-in-Class In Vitro Chemical Probes Against Poly (ADP Ribose) Glycohydrolase (PARG)
Dr Allan JORDAN
CANCER RESEARCH UK MANCHESTER INSTITUTE, Manchester, United Kingdom
12:05
Discovery 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
9.3 Showcase Brazil
10:45
Session Chair
Prof. Andrei LEITÃO
UNIVERSITY OF SAO PAULO, São Carlos, Brazil
10:50
Molecular Design, Synthesis and Trypanocidal Activity of Dipeptidyl Nitriles as Cruzain Inhibitors
Prof. Carlos MONTANARI
UNIVERSITY OF SAO PAULO, Sao Paulo, Brazil
11:30
Research, Development & Innovation at Aché Laboratórios Farmacêuticos
Dr Cristiano GUIMARAES
ACHÉ PHARMACEUTICAL, Brazil
11:50
Effects 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
12:10
Antiplatelet and Antithrombotic Activity of 1,2,5-Oxadiazole-2-N-Oxide Derivatives
Mr Luiz Antonio DUTRA
STATE UNIVERSITY OF SAO PAULO - UNESP, Araraquara, Brazil
12:30

Heterocycles and Medicinal Chemistry: The Importance of Innovative Synthesis 

Dr Anthony WOOD
PFIZER, Waltham, United States

Chair

Dr Franz VON NUSSBAUM
BAYER PHARMA, Berlin, Germany

13:15

Closing Remarks, Poster Prizes and Welcome to EFMC-ISMC 2018

Prof. Marko ANDERLUH
UNIVERSITY OF LJUBLJANA, Ljubljana, Slovenia