Table 1. Comparison of Compound 3 to Prior Lead Compounds 1 and 2^a.

	CCR2 Bnd	CCR2 CTX	CCR2 CD11b	CCR5 Bnd	CCR5 CTX	CCR5 CD11b
no.	IC50 (nM)	IC50 (nM)	IC50 (nM)	IC50 (nM)	IC50 (nM)	IC50 (nM)
1	1.1 ± 0.5	0.7 ± 0.2	NT	23.6 ± 12	NT	NT
2	2.7 ± 1.3	0.8 ± 0.5	2.6 ± 2.2	6.3 ± 1.5	1.1 ± 0.7	34.7 ± 11
3	6.2 ± 2.7	0.8 ± 0.8	4.8 ± 2.7	3.6 ± 1.8	1.1 ± 0.6	5.7 ± 2.4

^aAll assays are reported as means plus or minus standard deviation from two or more determinations. The CCR2 binding (Bnd) assay was performed in human peripheral blood mononuclear cells using labeled ¹²⁵I-CCL2 as the ligand. CCR5 binding (Bnd) and chemotaxis (CTX) assays were performed using human peripheral T cells using MIP-1β as the ligand (¹²⁵l-MIP-1β for Bnd). CCR2 chemotaxis was performed using labeled human THP-1 cells and CCL2 as the ligand. CCR2 CD11b and CCR5 CD11b upregulation assays used human whole blood with CCL2 and MIP-1β as the ligands, respectively. For additional details and references on assays, see the Supporting Information. NT = not tested.