Chemokines are proinflammatory mediators that primarily control leukocyte migration into selected tissues and upregulation of adhesion receptors. They also have a role in pathological conditions that require neovascularization and are implicated in the suppression of viral replication. By interaction with their respective G-protein-coupled receptor, chemokines have a profound influence over the selective recruitment of specific cell types in acute inflammatory disease and, hence, inhibition of their action should be of therapeutic benefit. Only now are small molecule inhibitors becoming available to validate this speculation. In this review, without seeking to be comprehensive, the authors provide an introduction to chemokines, their receptors and their role in certain disease processes. Also, recent disclosures claiming novel nonpeptide ligands for chemokine receptors are summarized.