Chemokines are a family of small proteins inducing directed cell migration via specific chemokine receptors, which play important roles in a variety of biological and pathological processes, such as immune surveillance, development, wound healing, bacterial infection, inflammatory reaction, tumor progression and metastasis, etc. Therapeutic strategies based on modulation of chemokine receptor pathways were reported to be promising clinical strategies in the treatment of inflammatory diseases, such as multiple sclerosis and atherosclerosis, psoriasis, inflammatory skin diseases and atopic dermatitis, as well as viral infections, including HIV. Approximately 20 chemokine receptors and 50 chemokines have been identified in humans. Chemokines and their receptors are divided into four families based on the pattern of cysteine residues: CXC, CC, CX3C and XC, where C represents the cysteine and X represents non-cysteine amino acids. Chemokine receptors are seven transmembrane spanning proteins coupled to G-protein-coupled-receptors (GPCRs). These receptors are named based on the chemokine ligands to which they bind. For example, CXC receptors (CXCR1, 2, 3, 4 and 5) bind CXC chemokines, CC receptors (CCR1, 2, 3, 4, 5, 6, 7, 8, 9) bind CC chemokines; CX3C receptor binds CX3C chemokine and lastly, the XC receptor binds the C chemokine. Advances in basic chemokine research have indicated that chemokines and their receptors are the highly promising drug targets for inflammatory and immunological diseases. Antagonizing the chemokine receptor interaction is considered to be beneficial in inflammatory disorders. Currently various chemokine receptor blockers range from monoclonal antibodies, modified chemokines, and low molecular weight receptor antagonists.

TargetMol collects 59 compounds targeting chemokines or chemokine receptors as Chemokine Inhibitor Library, which can be used for research in immune-mediated diseases, and drug screening.