IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3291-5. doi: 10.1016/j.bmcl.2008.04.039. Epub 2008 Apr 22.

Abstract

A potent IRAK-4 inhibitor was identified through routine project cross screening. The binding mode was inferred using a combination of in silico docking into an IRAK-4 homology model, surrogate crystal structure analysis and chemical analogue SAR.

MeSH terms

  • Binding Sites
  • Crystallography, X-Ray
  • Drug Design*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Imidazoles / chemical synthesis*
  • Imidazoles / chemistry
  • Imidazoles / pharmacology*
  • Interleukin-1 Receptor-Associated Kinases / antagonists & inhibitors*
  • Models, Molecular*
  • Molecular Conformation
  • Molecular Structure
  • Pyridines / chemical synthesis*
  • Pyridines / chemistry
  • Pyridines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Imidazoles
  • Pyridines
  • Interleukin-1 Receptor-Associated Kinases