TABLE 4

CCR5 selectivity: CCL3L1-mediated CCR5 internalization versus HOS and PBMC HIV-1 entry

Table shows mean difference in pIC50 values, with variance and degrees of freedom, for CCR5 CCL3L1-mediated internalization vs HOS and vs PBMC HIV-entry inhibition. The S.E.M. is calculated using the residual variance estimate pooled across compounds. Selectivity is estimated as 10 to the power of the difference between the mean pIC50 for HOS or PBMC HIV-1 entry and mean pIC50 for internalization. Also shown are the 95% lower and upper confidence limits for selectivity, which is calculated using critical values from the t-distribution, with degrees of freedom approximated using Satterthwaite's method (Stell et al, 1997).

Compound
Log diff
Variance
df
Selectivity
HOS
    Aplaviroc −0.241 0.00534 64.2 0.574
0.42-0.8
    TAK652 1.074 0.02537 354.1 11.865
5.76-24.4
    Maraviroc −0.135 0.01206 90.8 0.732
0.44-1.2
    TAK779 −0.281 0.0133 110.1 0.524
0.31-0.89
    Vicriviroc 0.039 0.0079 94.4 1.094
0.73-1.64
    Sch-C −0.689 0.02192 59.8 0.205
0.1-0.4
PBMC
    Aplaviroc −0.237 0.00615 84.7 0.5
0.4-0.83
    TAK652 1.105 0.02657 380.8 12.7
6-26.6
    Maraviroc −0.397 0.01268 100.2 0.401
0.24-0.67
    TAK779 −0.445 0.01426 207.3 0.067
0.036-0.126
    Vicriviroc −0.445 0.01426 263.5 0.36
0.21-0.62
    Sch-C −1.35 0.02666 88 0.045
0.02-0.09