TABLE 1.
First inhibitor | Target | IC50 (nM) | IC90 (nM) | Second inhibitor | CI50 | P value | CI90 | P value |
---|---|---|---|---|---|---|---|---|
PRO 140 | CCR5 | 2.5 | 8.6 | PRO 140 | 0.97 ± 0.07 | 0.13 | 0.96 ± 0.14 | 0.37 |
Maraviroc | CCR5 | 5.3 | 27 | PRO 140 | 0.61 ± 0.05 | <0.0001 | 0.40 ± 0.06 | <0.0001 |
Vicriviroc | CCR5 | 3.2 | 16 | PRO 140 | 0.51 ± 0.05 | <0.0001 | 0.36 ± 0.06 | <0.0001 |
TAK-779 | CCR5 | 11 | >200 | PRO 140 | 0.38 ± 0.08 | <0.0001 | NA | NA |
RANTES | CCR5 | 2.4 | 38 | PRO 140 | 0.59 ± 0.08 | 0.0022 | 0.43 ± 0.05 | 0.0002 |
RANTES | CCR5 | 2.4 | 38 | Maraviroc | 0.48 ± 0.03 | 0.0017 | 0.18 ± 0.01 | <0.0001 |
Vicriviroc | CCR5 | 3.2 | 16 | Maraviroc | 0.86 ± 0.03 | 0.016 | 0.75 ± 0.02 | 0.0033 |
Vicriviroc | CCR5 | 3.2 | 16 | TAK-779 | 1.3 ± 0.18 | 0.12 | NA | NA |
2D7 | CCR5 | 3.7 | 58 | PRO 140 | 1.0 ± 0.14 | 0.61 | 1.9 ± 0.61 | 0.024 |
Enfuvirtide | gp41 | 8.6 | 66 | PRO 140 | 0.84 ± 0.16 | 0.040 | 0.89 ± 0.20 | 0.19 |
PRO 542 | gp120 | 8.9 | 91 | PRO 140 | 0.96 ± 0.17 | 0.56 | 0.94 ± 0.19 | 0.45 |
BMS-378806 | gp120 | 5.2 | 20 | PRO 140 | 1.3 ± 0.19 | 0.0015 | 1.1 ± 0.22 | 0.19 |
Statistically significant results (P < 0.0023 after application of the Bonferroni correction for multiple comparisons) are indicated in italicized bold text. IC50 and IC90 denote values for the first inhibitor. NA, not applicable. TAK-779 did not consistently achieve 90% inhibition in the assay. CI values represent the means and standard deviations of 4 to 12 independent assays.