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Challenges of drug discovery in novel target space. The Discovery and Evaluation of PF-3893787: A Novel Histamine H4 Receptor Antagonist
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posted on 2023-06-08, 06:19 authored by Michael ParadowskiWe 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.
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Publication status
- Published
Journal
Bioorganic and Medicinal Chemistry LettersISSN
0960894XPublisher
ElsevierVolume
21Page range
6596-6602Department affiliated with
- Chemistry Publications
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- No
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- Yes
Legacy Posted Date
2012-02-06Usage metrics
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