1196993-69-7Relevant articles and documents
Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR)
Masood, M.Abid,Selby, Matthew D.,Bell, Andrew S.,Mansfield, Andrew C.,Gardner, Mark,Smith, Graham F.,Smith, Charlotte Lane,Kenyon-Edwards, Helen,Osborne, Rachel,Jones, Rhys M.,Liu, Wai L.,Brown, Christopher D.,Clarke, Nicholas,Perrucio, Francesca,Mowbray, Charles E.
body text, p. 6591 - 6595 (2011/12/04)
We describe the identification of a potent, selective lead series that shows antagonism against the human histamine H4 receptor from thirteen actives identified in an HTS as part of a hit to lead program. By focusing on ligand efficiency and concurrently using a diversity based approach, compounds based around 2,4-diaminopyrimidine were identified with compound 25 being quickly shown to be a good lead. It also had the highest ligand efficiency in the series.
