Course Identification

Introduction drug discovery

Guidelines for assays, screening methods

General concepts for biochemical and cell-based assays.

Target identification

Phenotypic vs targeted drug discovery

Lab exercises for proteases and viability screening

Structure-guided hit optimization

Basic medicinal chemistry

Emerging strategies in drug discovery

Covalent targeting

Degraders

Molecular glues

Methods for confirming target engagement by small moecules

ADME-Tox assays (e.g. cell viability, apoptosis, cardiotoxicity and mitochondrial toxicity).

Practical Training Sessions

Discovery team exercise

Project proposal

Participants will experience hands-on training sessions using experimental methods to provide a foundation for applying in-vitro approaches in drug discovery.

The course takes place at the INCPM, drug discovery facility.

During the course, students will learn about principles, methods and goals of drug discovery as it pertains to driving academic research towards applications relevant to the clinic. The scope of the course will be limited to small molecules and their use as chemical probes or leads to novel drugs. Students will perform different types of the experiments demonstrating assay development and screening methods, and will practice interpreting their data. Lectures will provide background for lab experiments and broader knowledge of strategies such as phenotypic screening, degraders, covalent targeting, pre-clinical pharmokinetics and pharmacology. Data sharing and multidisciplinary team-work is central to drug discovery, so students will perform a team-based exercise using open-source data from an antiviral discovery campaign. Finally, students will present project proposals for review in a group exercise.