2. Academic Validation
  3. Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists

Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists

  • Bioorg Med Chem Lett. 2010 Apr 15;20(8):2516-9. doi: 10.1016/j.bmcl.2010.02.097.
Sue Cramp 1,  Hazel J Dyke,  Christopher Higgs,  David E Clark,  Matthew Gill,  Pascal Savy,  Neil Jennings,  Steve Price,  Peter M Lockey,  Dennis Norman,  Soraya Porres,  Francis Wilson,  Alison Jones,  Nigel Ramsden,  Raffaella Mangano,  Dan Leggate,  Marie Andersson,  Richard Hale
Affiliations

Affiliation

  • 1 Argenta, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, UK. Sue.cramp@argentadiscovery.com
PMID: 20299215 DOI: 10.1016/j.bmcl.2010.02.097
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.

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