Chemokine receptors are involved in a broad spectrum of physiological and pathological processes that include immune responses, inflammation, viral infection, as well as development and metastasis of cancer. Targeting of chemokine receptors has become a therapeutic strategy and the selective chemokine receptor antagonists have important therapeutic implications. One of such examples is the anti-HIV effect of inhibitors of CC-chemokine receptor 5 (CCR5) and CXC chemokine receptor 4 (CXCR4). Chinese medicines (CM) have been used for the treatment of inflammatory diseases for thousands of years, however, the scientific basis for the beneficial clinical effects of CM remains to be fully understood. So far, our studies have identified a number of chemokine receptor antagonists with defined chemical structures from CM with anti-inflammatory properties. These naturally occurring compounds have in vitro activity in the blockade of binding of chemokine ligands to their receptors, and consequently inhibited the chemotactic migration of leukocytes induced by certain chemokines. Our studies indicate that the clinical efficacy of anti-inflammatory CM is at least partially attributable to their inhibitory effect on chemokine receptors. Therefore, identification of CM-derived compounds capable of targeting chemokine receptors can unveil mechanisms underlying the anti-inflammatory effect of CM, and may also lead to the development of novel therapeutic agents. This chapter summarizes and discusses some of the recent studies in this field and the relevant experimental protocols are also introduced.