Lead optimisation: what you should know!

Ward, Simon E. ORCID: https://orcid.org/0000-0002-8745-8377 and Davis, Andrew M. 2023. Lead optimisation: what you should know! Ward, Simon E. and Davis, Andrew, eds. The Handbook of Medicinal Chemistry: Principles and Practice, The Royal Society of Chemistry, pp. 720-768. (10.1039/9781788018982-00720)

Full text not available from this repository.

Abstract

Lead Optimisation (LO) is a critical part of the drug discovery process as it is the part where all efforts that go into earlier parts of the process (Target Identification, HTS, Hit-to-Lead, Lead Identification) are crystallised into a single compound, the candidate drug. The optimisation phase is like a treasure hunt, and discovery projects can take many paths to discover their treasured molecule. In this chapter we have chosen to focus on the practicalities of how the LO project can be organised, and what different property issues the project may face as it attempts to find an efficient path forward to find a suitable candidate drug for development. This multiparameter optimisation dance can have many issues, often interconnected. We discuss approaches to many of these problems and offer advice on how project members should think about tackling issues in a holistic way. In this way we hope to support projects in understanding the right issues to tackle at the right time. We offer some tips, and examples, of successes, and suggest that identifying the issue to tackle is key to establishing robust hypotheses to test and so drive projects forward. Our goal in this chapter is to aid project thinking about the best way forward.

Item Type:	Book Section
Date Type:	Publication
Status:	Published
Schools:	Medicine
Publisher:	The Royal Society of Chemistry
ISBN:	9781788018982
Last Modified:	21 Oct 2024 08:00
URI:	https://orca.cardiff.ac.uk/id/eprint/173147

Actions (repository staff only)

Edit Item