title: Chemokine receptor antagonist development.
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.
authors.affiliation: Geneva Research Centre, Division of Autoimmune and Inflammatory Diseases, Merck Serono, Geneva, Switzerland.
authors.forename: Alexandre
authors.initials: A
authors.lastname: Garin
authors.forename: Zoë
authors.initials: Z
authors.lastname: Johnson
authors.forename: Aurelie
authors.initials: A
authors.lastname: Hermant
authors.forename: Fanny
authors.initials: F
authors.lastname: Beltran
authors.forename: Yann
authors.initials: Y
authors.lastname: Ratinaud
authors.forename: Alexandra
authors.initials: A
authors.lastname: Michel
authors.forename: Sonja
authors.initials: S
authors.lastname: Krohn
authors.forename: Marilène
authors.initials: M
authors.lastname: Gaudet
authors.forename: Susanna
authors.initials: S
authors.lastname: Carboni
authors.forename: Hong
authors.initials: H
authors.lastname: Ji
authors.forename: Marc
authors.initials: M
authors.lastname: Missotten
authors.forename: Olivier
authors.initials: O
authors.lastname: Leger
authors.forename: Christine
authors.initials: C
authors.lastname: Power
authors.forename: Amanda
authors.initials: A
authors.lastname: Proudfoot
mesh_terms: D000818:Animals; D057205:Automation, Laboratory; D018929:Cell Culture Techniques; D054443:Cell Migration Assays; D002478:Cells, Cultured; D018925:Chemokines / Q000378:metabolism; D002633:Chemotaxis / Q000187:drug effects; D058266:Dielectric Spectroscopy; D004305:Dose-Response Relationship, Drug; D055808:Drug Discovery / Q000379:methods*; D004797:Enzyme-Linked Immunosorbent Assay; D057166:High-Throughput Screening Assays; D006801:Humans; D008024:Ligands; D010599:Pharmacokinetics; D011485:Protein Binding; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors* / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects
chemical_list: D018925:Chemokines; D008024:Ligands; D019707:Receptors, Chemokine