Targeting of chemokine receptors by small molecules has been widely pursued. This review highlights recent illustrative disclosures of clinical relevance that could further shape our appreciation, and add to our understanding, of the therapeutic value of chemokine receptor targeting. Disclosures include new structures, announcements of new trials, or results of conducted trials (including setbacks). This review shows how most of the discussed disclosures seem to be concentrated on selected receptors, for example, CCR1, CCR2, CCR5, CCR9, CXCR2 and CXCR4, with a wide variety of associated ligand chemotypes and diseases. With two approved antagonist drugs and several in Phase III trials, as well as new antagonist chemotypes entering the pipeline, the chemokine receptor field proves dynamic and upcoming results will further fuel the field.© 2012 Elsevier Ltd. All rights reserved.