Table 1.
EC50 (IC50) values for non-feminizing estrogen analogues.
Reproduced from Yi et al., 2011 with permission.
| Compound | Glut (10 mM) |
Glut (20 mM) |
IAA (20 µM) |
IAA (40 µM) |
Erα Binding |
Erβ Binding |
TBARs | Compound | Glut (10 mM) |
Glut (20 mM) |
IAA (20 µM) |
IAA (40 µM) |
ERα Binding |
ERβ Binding |
TBARs |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| ZYC1 | 1.025 | 1.571 | 0.253 | 1.72 | 3.978 | 4.058 | 4.922 | ZYC41 | 11.30 | 1.573 | 1.341 | 34.27 | 105.0 | 6.291 | |
| ZYC2 | 9.021 | 10.00 | 0.006 | 8.259 | 126.75 | 165.8 | 16.075 | ZYC42 | 1.167 | 1.510 | 0.051 | 0.942 | 248.5 | 323.6 | 21.89 |
| ZYC3 | 0.159 | 0.365 | 0.216 | 10000 | 10000 | 1.126 | ZYC43 | 0.730 | 1.511 | 1.393 | 1.449 | 8729 | 7938 | 4.506 | |
| ZYC4 | 9.207 | 17.14 | 196.2 | 0.052 | 43.57 | 31.41 | 10.171 | ZYC44 | 0.363 | 0.399 | 0.051 | 0.167 | 2637.5 | 10000 | 0.408 |
| ZYC5 | 0.023 | 0.121 | 0.120 | 0.152 | 10000 | 10000 | 1.391 | ZYC45 | 0.684 | 0.975 | 0.239 | 0.446 | 800.2 | 5176 | 2.214 |
| ZYC6 | 17.61 | 13.69 | 2.708 | 8.483 | 1698 | 10000 | 17.079 | ZYC46 | 0.866 | 0.465 | 0.069 | 0.155 | 7305 | 10000 | 2.130 |
| ZYC7 | 8.582 | 14.73 | 2.405 | 1.729 | 133.5 | 242.1 | 5.332 | ZYC47 | 0.139 | 0.121 | 0.017 | 0.088 | 8831 | 10000 | 1.415 |
| ZYC9 | 1.956 | 1.315 | 5.020 | 5.296 | 480.65 | 204.2 | 29.465 | ZYC48 | 0.179 | 0.527 | 0.176 | 1.599 | 877.5 | 5208 | 3.120 |
| ZYC10 | 0.488 | 0.851 | 0.296 | 0.679 | 16.32 | 8.138 | 3.132 | ZYC49 | NP | NP | NP | NP | 10000 | 10000 | NI |
| ZYC11 | 4.627 | 7.031 | 0.296 | 0.679 | 107.0 | 64.49 | 26.115 | ZYC50 | 0.111 | 0.139 | 0.081 | 0.235 | 202.7 | 769.2 | 2.156 |
| ZYC12 | 0.548 | 1.953 | 1.290 | 4.440 | 73.96 | 53.35 | 4.763 | ZYC51 | 0.653 | 1.769 | 0.446 | 0.651 | 1649 | 4702 | 1.521 |
| ZYC13 | 0.239 | 1.173 | 0.191 | 0.129 | 25.30 | 18.70 | 9.167 | ZYC52 | 2.439 | 4.101 | 0.057 | 0.286 | 4258 | 114.3 | 16.59 |
| ZYC14 | 0.215 | 0.240 | 0.183 | 0.382 | 2263 | 2461 | 1.033 | ZYC53 | 14.68 | 143.2 | 0.072 | 0.375 | 10000 | 10000 | NI |
| ZYC15 | 0.047 | 0.803 | 0.646 | 1.200 | 1649 | 10000 | 1.495 | ZYC54 | 5.138 | 7.621 | 0.210 | 0.918 | 10000 | 10000 | 1.580 |
| ZYC16 | 0.882 | 0.860 | 2.250 | 1.912 | 10000 | 10000 | 3.648 | ZYC55 | 0.913 | 0.926 | 0.246 | 0.458 | 10000 | 10000 | 1.369 |
| ZYC17 | 0.244 | 0.270 | 0.680 | 0.828 | 10000 | 10000 | 4.913 | ZYC56 | 3.550 | 4.59 | 0.313 | 1.717 | 445.3 | 354.1 | 18.60 |
| ZYC18 | 0.568 | 0.921 | 0.264 | 1.044 | 2384.5 | 10000 | 2.307 | ZYC57 | NP | NP | 0.165 | 1.311 | 593.9 | 10000 | 20.19 |
| ZYC19 | 0.184 | 0.272 | 0.099 | 0.302 | 784.1 | 10000 | 2.488 | ZYC58 | 1.655 | 2.922 | 0.163 | 0.829 | 10000 | 10000 | 2.564 |
| ZYC20 | 0.132 | 0.273 | 0.908 | 1.134 | 5089 | 10000 | 1.905 | ZYC59 | 0.765 | 0.924 | 0.162 | 0.337 | 752.6 | 263.9 | 7.398 |
| ZYC21 | 0.122 | 0.245 | 0.108 | 0.282 | 2855 | 4456 | 1.264 | αE2 | 3.102 | 5.739 | 3.375 | 161.7 | 16.46 | 83.75 | |
| ZYC22 | 0.030 | .030 | 0.084 | 0.358 | 10000 | 10000 | 1.827 | βE2 | 1.364 | 1.978 | 2.902 | 4.704 | 3.041 | 4.512 | 19.83 |
| ZYC23 | NP | NP | NP | NP | 10000 | 10000 | NI | DES | 3.772 | 14.10 | 0.769 | 3.802 | 2.615 | 1.84 | 6.882 |
| ZYC24 | 0.665 | 0.768 | 1.132 | 3.928 | 209.45 | 259.95 | 7.028 | E1 | 3.029 | 8.920 | 2.092 | 1609.2 | 13.35 | 30.92 | 80.79 |
| ZYC25 | 0.238 | 0.147 | 0.159 | 0.359 | 10000 | 10000 | 1.375 | E1-quinol | 10000 | 10000 | |||||
| ZYC26 | 0.012 | 0.037 | 0.164 | 0.280 | 10000 | 10000 | 0.708 | EntE2 | 0.936 | 1.166 | 7.110 | 35.01 | 24.65 | 5.635 | 23.95 |
| ZYC27 | 0.992 | 1.195 | 0.541 | 1.932 | 14.28 | 11.97 | 3.279 | E380 | 1.277 | 1.980 | 0.159 | 1.230 | 5.912 | 2.372 | 6.725 |
| ZYC28 | 0.497 | 0.568 | 0.458 | 1.268 | 61.12 | 533.9 | 7.88 | E400 | 1.651 | 1.866 | 0.126 | 1.245 | 117.5 | 52.37 | 20.88 |
| ZYC29 | 6.730 | 8.252 | 1.576 | 7.525 | 10.97 | 17.42 | 10.47 | E430 | NP | NP | 7.923 | 33.47 | 1880 | 10000 | NI |
| ZYC30 | 8.290 | 9.033 | 0.591 | 8.814 | 26.95 | 16.84 | 14.89 | E1240 | NP | NP | NP | NP | 785.5 | 1197 | NI |
| ZYC33 | 0.0938 | 0.1273 | 0.046 | 0.086 | 10000 | 10000 | 1.208 | E2540 | NP | NP | NP | NP | NI | ||
| ZYC34 | 0.121 | 0.19 | 0.046 | 0.219 | 1460 | 88.01 | 0.664 | E2550 | NP | NP | NP | NP | 953.4 | 260.3 | NI |
| ZYC35 | 3.203 | 3.896 | 1.021 | 1.623 | 5.53 | 14.31 | 7.806 | E2555 | NP | NP | NP | NP | 1513 | 10000 | NI |
| ZYC36 | 6.883 | 6.627 | 1.195 | N/A | 5.55 | 2.64 | 17.445 | E2560 | NP | NP | NP | NP | 33.06 | 261.7 | NI |
| ZYC37 | 11.75 | 8.228 | 1.836 | 4.25 | 4.88 | 7.48 | 11.024 | PS1 | 13.08 | 13.84 | 17.45 | 2.547 | 29.04 | 12.22 | 9.701 |
| ZYC38 | 0.133 | 0.213 | 0.021 | 0.035 | 296.4 | 10000 | 0.895 | PS2 | 10.15 | 16.21 | 278.7 | 1662 | 27.65 | 33.09 | 8.951 |
| ZYC39 | 0.180 | 0.368 | 0.049 | 0.282 | 633.2 | 10000 | 1.577 | PS3 | NP | NP | NP | NP | 692.2 | 615.4 | NI |
| NYC40 | 0.524 | 0.443 | 1.901 | PS4 | NP | NP | NP | NP | 2862 | 10000 | NI |
NP (no protection); NI (no inhibition); 10000 (over 10 µM required for binding or no binding activity).