Table 3.
IC50 values obtained in inhibition experimentsa.
| SK3 anti-CD4 (ng/ml) | T-1249 (nM) | T-1249-BR (nM) | BMS-378806 (nM) | HNG-105 (μM) | |
| Br | 119 (58–246) | 173 (129–230) | 195 (157–298) | 15 (9.4–23) | 3.8 (2.2–6.5) |
| BS | 79 (60–102) | 140 (113–172) | 155 (83–289) | 20 (13–31) | 1.8 (0.9–3.7) |
| Bv1v3 | 94 (55–158) | 227 (110–468) | 245 (156–387) | 8.2 (5.7–12) | 21 (12–36) |
| Bv1v2 | 22 (13–36) | 224 (174–288) | 155 (123–195) | 4.8 (3.5–6.6) | 48 (9.8–231) |
| Br(N283T) | 60 (32–114) | 166 (102–271) | 221 (148–329) | 13 (4.6–35) | 7.2 (2.2–24) |
| Spl | 5.7 (2.3–14) | 37 (19–71) | 27 (17–43) | 1.8 (1.3–2.7) | 16 (6.7–39) |
| SB | 11 (6.4–18) | 83 (53–129)b | 41 (30–56)b | 2.0 (1.2–3.5) | 25 (12–50) |
| Sv1v3 | n.d. | n.d. | n.d. | 0.9 (0.6–1.3) | n.d. |
| Sv1v2 | n.d. | n.d. | n.d. | 1.2 (0.7–2.2) | n.d. |
| Spl(T283N) | 11 (7.3–18) | n.d. | n.d. | 0.9 (0.7–1.3) | n.d. |
| DS17 | 5.4 (3.8–7.7) | 210 (160–274)b | 92 (73–116)b | 41 (29–58) | 4.1 (2.7–6.2) |
| DS17(N283T) | 5.1 (4.0–6.4) | 155 (119–202) | 104 (72–150) | 32 (24–41) | 2.6 (1.0–6.6) |
| BaL | n.d. | 102 (85–122) | 124 (103–149) | 29 (15–59) | 58 (14–241) |
| HxB | n.d. | n.d. | n.d. | 3.9 (2.8–5.4) | 1.6 (0.7–3.6) |
a Non-linear regression analysis of dose response curves generated for various viruses and inhibitors was performed with GraphPad Prism software; IC50 values are shown, with 95% confidence limits between parenthesis.
b SB and DS17 were the only Env that demonstrated statistically significant greater sensitivity to T-1249-BR than to parental T-1249 (F test, p < 0.05 and p < 0.001, respectively).
n.d., not determined.