Chemokine receptor-5 (CCR5) serves as a co-receptor necessary for the binding of HIV-1 to the host cells, the defective CCR5 function and the blocking of CCR5 sites by CCR5 antagonists will suppress the entry of HIV-1 to target cells. To acquire the peptide antagonists specifically binding CCR5, CHO cells stably expressing human CCR5 (CHO/CCR5) were used to select CCR5-binding peptides from a phage displayed 12-mer peptide library. After four rounds of selection, eleven out of the 20-phage clones shared the amino acid motif AFDWTFVPSLIL. The motif-containing phages could competitively bind to CHO/CCR5 cells with anti-human CCR5 mAb, and the synthetic peptide AFDWTFVPSLIL could inhibit RANTES binding to CHO/CCR5. These results suggest that the peptide could specifically bind CCR5 molecules.