Chemokine receptor antagonist development

Methods Mol Biol. 2013:1013:67-92. doi: 10.1007/978-1-62703-426-5_6.

Abstract

This chapter describes assays that focus on the characterization of compounds identified in high--throughput screening campaigns, and the subsequent medicinal chemistry programs. They cover methods to determine potency in buffer, the effect of whole blood on the compounds' activity and finally the pharmacokinetic (PK)/pharmacodynamic (PD) -relationship of the compounds in a rodent species.

MeSH terms

  • Animals
  • Automation, Laboratory
  • Cell Culture Techniques
  • Cell Migration Assays
  • Cells, Cultured
  • Chemokines / metabolism
  • Chemotaxis / drug effects
  • Dielectric Spectroscopy
  • Dose-Response Relationship, Drug
  • Drug Discovery / methods*
  • Enzyme-Linked Immunosorbent Assay
  • High-Throughput Screening Assays*
  • Humans
  • Ligands
  • Pharmacokinetics
  • Protein Binding
  • Receptors, Chemokine / antagonists & inhibitors*
  • Receptors, Chemokine / metabolism
  • Signal Transduction / drug effects

Substances

  • Chemokines
  • Ligands
  • Receptors, Chemokine