Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists
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.
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
scheme or table
p. 2516 - 2519
(2010/06/20)
Syntheses of 2,4 dicyanophenoxyacetic acid and its analogues
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Hatano,Matsui
p. 2917 - 2919
(2007/10/12)
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