Challenges of drug discovery in novel target space. The Discovery and Evaluation of PF-3893787: A Novel Histamine H4 Receptor Antagonist

Paradowski, Michael (2011) Challenges of drug discovery in novel target space. The Discovery and Evaluation of PF-3893787: A Novel Histamine H4 Receptor Antagonist. Bioorganic & Medicinal Chemistry Letters, 21. pp. 6596-6602. ISSN 0960894X

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Abstract

We describe the development of novel benzimidazoles as small molecule histamine H4 receptor (H4R) antagonists and their profiling in rat early toxicity studies. The discovery and optimisation of a second series of pyrimidine based antagonists is then described culminating in the identification of the clinical development candidate 13 (PF-3893787). The pre-clinical profile of 13 (PF-3893787) is presented including the development of a translatable biomarker. Our pragmatic approach to target selection, safety assessment, and testing for efficacy faced numerous challenges and we share a number of lessons which the team learned and which will assist us and others in future drug discovery projects.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Depositing User: Michael Paradowski
Date Deposited: 06 Feb 2012 20:27
Last Modified: 31 May 2012 16:24
URI: http://sro.sussex.ac.uk/id/eprint/25985
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