Table 1.
Summary of compound properties
| Compound name | S. cerevisiae IC50, WT CXCR4 (nM)a | S. cerevisiae IC50 [EC50 for AMD3100], N1193.35A CXCR4 (nM)a | CXCL12 binding IC50, WT CXCR4 (nM)b | HIV-1 IC50 (nM)b | β-arrestin-2 IC50, WT CXCR4 (nM)a | Cytotoxicity CC50 (μM) | |
|---|---|---|---|---|---|---|---|
| CEM cells | TZM-bl cells | ||||||
| AMD3100 | 49.2 (39.1, 61.3) | [47.2 (19.7, 107)] | 12.0 ± 1.1d | 4 – 10g | 29 (16, 54) | NTj | NTj |
| B7 | 0.0551 (0.0386, 0.0785) | NRc | 28.0 ± 2.7 | 2.4 ± 0.4 | 90 (61, 130) | >50 | >50 |
| B8 | 0.0695 (0.0507, 0.0946) | 83.0 (1.87, 2430) | 18.1 ± 2.8e | 2.0 ± 0.1e | 170 (83, 590) | >50e | >50e |
| B9 | 7.18 (6.39, 8.06) | 21.0 (6.21, 75.3) | 39.7 ± 5.1f | 25.2 ± 24.9 | 700 (210, 2200000) | >50 | >50 |
| CX0298 | 0.167 (0.130, 0.213) | NRc | 27.8 ± 1.9 | 4.2 ± 0.3 | 1600 (370, NRi) | >50 | >50 |
| CX344 | 7.75 (6.87, 8.73) | 98.9 (29.6, 392) | 4.2 ± 0.4e | 0.61 ± 0.27e | 55 (31, 120) | >50e | >50e |
| IT1t | 0.198 (0.163, 0.240) | 13.7 (6.08, 32.5) | 2.1± 0.4d | 40h | NTj | NTj | NTj |
a
95% confidence intervals are provided in parentheses
b
Error is presented as standard deviation of the mean (SD)
c
NR = not reported. These compounds function as neutral antagonists against the CAM
d
As reported by Van Hout et al., 2017 (Van Hout et al., 2017), in which a fluorescently-labeled CXCL12 was used
e
As reported by Wu et al., 2015 (Wu et al., 2015b)
f
As reported by Wu et al., 2015 (Wu et al., 2015a)
g
As reported by Schols et al., 1997 (Schols et al., 1997)
h
As reported by Thoma et al., 2008 (Thoma et al., 2008)
i
NR = not reported. The upper confidence interval is not defined
j
NT = not tested