Irreversible covalent modulation is a crucial part of the drug discovery toolbox and is an important strategy for finding tractable equity against less druggable targets. However, understanding the binding kinetics, mechanistic PK/PD relationship and SAR of compounds is critical to success as is employing best practice in hit identification and lead optimisation.

Join us in Cambridge on 16-17 October 2024, where we will bring together established leaders and emerging investigators exploring the use of irreversible covalent modulators in drug discovery. Targeting of both cysteine and other amino acid residues will be considered as will an depth analysis of the kinetics of irreversible inhibition. Irreversible modulation as a strategy for targeted protein degradation and the identification of covalent chemical equity through proteomic approaches will also be covered.

Learning outcomes:

We expect that the meeting may serve to:

1). Build a network amongst researchers interested in irreversible modulation in drug discovery

2). Establish the framework for understanding kinetics in drug discovery for irreversible binders

3). Enable researchers to better understand and optimise chemical tools, leads and drug candidates

Session recordings will also be made available to registrants.

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