Chemokine receptor antagonist development.

Authors: Garin A, Johnson Z, Hermant A, Beltran F, Ratinaud Y, Michel A, Krohn S, Gaudet M, Carboni S, Ji H, Missotten M, Leger O, Power C and Proudfoot A.
Publisher/Year: Methods Mol Biol 1013:67-92.
Pub Med ID/Journal ID: PMID:23625494


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.