RS 504393 is a selective CCR2 chemokine receptor antagonist (IC50 values are 98 nM and > 100 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively).

RS102895 is a potent and specific CCR2 antagonist with binding IC50 of 360 nM, no significant inhibition on CCR1 (IC50 > 17 μM).

RS102895 HCl is a potent and specific CCR2 antagonist with binding IC50 of 360 nM, no significant inhibition on CCR1 (IC50 > 17 μM).

BX471 is a potent, selective non-peptide CCR1 antagonist (Ki = 1 nM for human CCR1) and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.

NSC 5844 is a bisquinoline compound with C-C chemokine receptor type 1 (CCR1)-agonistic properties.

TAK-779 is a highly potent and selective nonpeptide CCR5 antagonist with a IC50 value of 1.4 nM in the binding assay. TAK-779 also inhibits the replication of macrophage (M)-tropic HIV-1 (Ba-L strain) in both MAGI-CCR5 cells and PBMCs with EC50 values of 1.2 and 3.7 nM, respectively.

Cenicriviroc, also known as TAK-652 and TBR-652, is an experimental drug candidate for the treatment of HIV infection. It is being developed by Takeda Pharmaceutical and Tobira Therapeutics. Cenicriviroc is an inhibitor of CCR2 and CCR5 receptors, allowing it to function as an entry inhibitor which prevents the virus from entering into a human cell. Inhibition of CCR2 may have an anti-inflammatory effect.