Discovery of NVP-LEQ506, a second-generation inhibitor of smoothened

ChemMedChem. 2013 Aug;8(8):1261-5. doi: 10.1002/cmdc.201300217. Epub 2013 Jul 2.
No abstract available

Keywords: antitumor agents; hedgehog signaling; medicinal chemistry; pyridazines; smoothened inhibitors.

MeSH terms

  • Animals
  • Cell Line
  • Disease Models, Animal
  • Dogs
  • Drug Evaluation, Preclinical
  • ERG1 Potassium Channel
  • Ether-A-Go-Go Potassium Channels / metabolism
  • Half-Life
  • Humans
  • Mice
  • Pyrazines / chemical synthesis
  • Pyrazines / chemistry*
  • Pyrazines / pharmacokinetics
  • Pyridazines / chemical synthesis
  • Pyridazines / chemistry*
  • Pyridazines / pharmacokinetics
  • Rats
  • Receptors, G-Protein-Coupled / antagonists & inhibitors*
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / metabolism
  • Smoothened Receptor
  • Solubility
  • Structure-Activity Relationship

Substances

  • ERG1 Potassium Channel
  • Ether-A-Go-Go Potassium Channels
  • NVP-LEQ506
  • Pyrazines
  • Pyridazines
  • Receptors, G-Protein-Coupled
  • SMO protein, human
  • Smoothened Receptor