1228148-40-0Relevant academic research and scientific papers
Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists
Cramp, Sue,Dyke, Hazel J.,Higgs, Christopher,Clark, David E.,Gill, Matthew,Savy, Pascal,Jennings, Neil,Price, Steve,Lockey, Peter M.,Norman, Dennis,Porres, Soraya,Wilson, Francis,Jones, Alison,Ramsden, Nigel,Mangano, Raffaella,Leggate, Dan,Andersson, Marie,Hale, Richard
, p. 2516 - 2519 (2010)
The identification and hit-to-lead exploration of a novel, potent and selective series of histamine H4 receptor inverse agonists is described. The initial hit, 3A (IC50 19 nM) was identified by means of a ligand-based virtual screening approach. Subsequent medicinal chemistry exploration yielded 18I which possessed increased potency (R-enantiomer IC50 1 nM) as well as enhanced microsomal stability.
