MedChem 2012 - From Rapid Dissociation to Irreversible Inhibition
Optimisation of Drug-Target Residence Time
30/11/2012
08:00Registration
08:50Opening
09:00Looking Beyond Potency: Importance of Assessing Residence Time in Chemistry and Its Impact on Drug Discovery
Dr Yogesh SABNIS
(UCB PHARMA, Braine-l'Alleud, Belgium)
09:50Kinetics in Drug Discovery. A case for G Protein-Coupled Receptors
Prof. Ad P. IJZERMAN
(UNIVERSITY OF LEIDEN, Leiden, The Netherlands)
10:40Coffee Break
11:15Kinetics Based Early Drug Screening : a New Application for DNA-Encoded Chemical Libraries
Dr Peter BLAKSKJÆR
(VIPERGEN, Copenhagen, Denmark)
11:35A ‘Fast’ Track to Atypicality – The Discovery of JNJ37822681 for the Treatment of Schizophrenia
Dr Gregor J. MACDONALD
(JANSSEN RESEARCH & DEVELOPMENT, Beerse, Belgium)
12:25Sandwich Lunch
14:00Kinetic Screening in Drug Discovery
Prof. Andrew HOPKINS
(UNIVERSITY OF DUNDEE, Dundee, United Kingdom)
14:50How to Design Better Small Molecule Ligands: a Case of CCR2 Antagonists
Mr Maris VILUMS
(LEIDEN UNIVERSITY, Leiden, The Netherlands)
15:10A Computational Approach to Predict Inhibitor Binding Kinetics : the PNP Case
Dr Walter ROCCHIA
(FONDAZIONE ISTITUTO ITALIANO DI TECNOLOGIA, Genova, Italy)
15:30Coffee Break and Poster Session
16:05The Resurgence of Covalent Inhibitors
Dr Russell PETTER
(CELGENE AVILOMICS RESEARCH, Bedford, United States)
16:55Irreversible Inhibitors of Serine Proteases: Tools or Drugs?
Prof. Koen AUGUSTYNS
(UNIVERSITY OF ANTWERP, Antwerp, Belgium)
17:45Closing Remarks
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