Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.
Basic Information
ID: ALA1156992
Journal: Bioorg Med Chem Lett
Title: Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists.
Authors: Cramp S, Dyke HJ, Higgs C, Clark DE, Gill M, Savy P, Jennings N, Price S, Lockey PM, Norman D, Porres S, Wilson F, Jones A, Ramsden N, Mangano R, Leggate D, Andersson M, Hale R.
Abstract: The identification and hit-to-lead exploration of a novel, potent and selective series of histamine H(4) receptor inverse agonists is described. The initial hit, 3A (IC(50) 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 IC(50) 1 nM) as well as enhanced microsomal stability.
CiteXplore: 20299215
DOI: 10.1016/j.bmcl.2010.02.097
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