Table 2. Compound 3 Profilea.
| assay | result |
|---|---|
| CCR2 Bnd IC50 | 6.2 ± 2.7 nM |
| CCR5 Bnd IC50 | 3.6 ± 1.8 nM |
| CCR1 Bnd IC50 | >25 μM |
| CCR4 Bnd IC50 | >40 μM |
| CXCR2 Bnd IC50 | >40 μM |
| mouse CCR2 Bnd IC50 | 45 ± 22 nM |
| LM t1/2: h, m, r (min) | 146/>200/>200 |
| hERG PC %inhib @ 30 μM | 9 |
| protein binding % free h/m/r | 71/58/69 |
| PAMPA Pc pH = 5.5 (nm/s) | 19 |
| PAMPA Pc pH = 7.4 (nm/s) | 336 |
a
Liver microsomes (LM) t1/2 reported for human (h), mouse (m), rat (r). Protein binding by equilibrium dialysis with 1 μM conc at 37 °C. For additional details on assays and references see the Supporting Information.