Table 2. Characterization of CXCR7 β-Arrestin Antagonist 10.
| 10 | |
|---|---|
| CXCR7 Ki (nM)a | 597 (6.22 ± 0.27) |
| CXCR4 IC50 (nM) | >15,000 |
| CXCR7 β-arrestin EC50 (nM) agonist mode | >10,000 |
| CXCR7 β-arrestin IC50 (nM)aantagonist mode | 622 (6.20 ± 0.38) |
| logDb | 3.1 |
| Solubility (μg/mL)c | 98.8 |
| Papp (10–6 cm/s)d | 1.1 |
| HLM CLint (μL/min/mg)e | 109 |
| MLM CLint (μL/min/mg)f | 737 |
a
Values are reported as geometric means of at least three independent experiments with pKi or pIC50 ± SD in parentheses.
b
logD was measured by the shake flask method at pH 7.4.
c
Kinetic stability was measured at pH 6.5.
d
Passive permeability was determined using a Madin–Darby canine kidney (MDCK) cell line.
e
Microsomal stability was determined in human liver microsomes (HLM).
f
Microsomal stability was determined in mouse liver microsomes (MLM).