Table 2.
TRE | Receptor | T3, nM (% efficacy) | QH2, nM (% efficacy) | GC-1, nM (% efficacy) |
---|---|---|---|---|
DR4 | TRα | 0.12±0.03 (100) | 737±59.0 (90) | 6.2±1.6 (88) |
TRβ | 0.51±0.05 (100) | 341±25 (98) | 2.1±0.9 (90) | |
TRβ(H435A) | 392±84 (97) | 6.43±0.57 (93) | >5000 (40) | |
| ||||
F2 | TRα | 0.25±0.08 (100) | 1596±84 (76) | n.d. |
TRβ | 0.86±0.11 (100) | 1240±122 (58) | n.d. | |
TRβ(H435A) | 774±53 (82) | 27.9±7.1 (93) | n.d. | |
| ||||
Pal | TRα | 0.12±0.04 (100) | 1439±142 (75) | n.d. |
TRβ | 0.44±0.05 (100) | 594±37 (87) | n.d. | |
TRβ (H435A) | 747±119 (90) | 22.9±5.9 (93) | n.d. |
% efficacy: maximum inducible activity compared to TR(wt) with T3. n.d.: not determined