From: Evolution of pharmacologic specificity in the pregnane X receptor
Cmp. # | Compound | hPXR Activity | hPXR Efficacy | zfPXR Activity | zfPXR Efficacy | Toxicity |
---|---|---|---|---|---|---|
 | ANDROSTANES |  |  |  |  |  |
AN1 | 5α-Androstan-3α,17β-diol | 5.38 | 0.68 | 5.19 | 0.84 | None |
AN2 | 5α-Androstan-3,17-dione (androstanedione) | 4.90 | 0.87 | 5.50 | 0.86 | None |
AN3 | 5α-Androstan-3α-ol (androstanol) | 5.20 | 0.5 | 5.34 | 1.00 | None |
AN4 | 5α-Androstan-3α-ol-17-one (androsterone) | 4.73 | 0.93 | 5.60 | 0.87 | None |
AN5 | 5α-Androstan-17β-ol-3-one (dihydrotestosterone) | 4.94 | 0.39 | 5.21 | 0.59 | None |
AN6 | 5β-Androstan-3α-ol-17-one (etiocholanolone) | 5.24 | 0.54 | 5.47 | 0.88 | 200 |
AN7 | 4-Androsten-3,17-dione (androstenedione) | 4.69 | 0.59 | 5.44 | 0.14 | None |
AN8 | 4-Androsten-17β-ol-3-one (testosterone) | 4.14 | 0.22 | 5.61 | 0.12 | None |
AN9 | 5-Androsten-3β-ol-17-one (DHEA) | 4.49 | 0.52 | 4.89 | 0.35 | None |
AN10 | 5α-Androst-16-en-3α-ol (androstenol) | 5.26 | 0.7 | 5.44 | 1.02 | None |
AN11 | 5β-Androstan-3α,11β-diol-17-one | 4.72 | 0.51 | 4.52 | 1.04 | None |
AN12 | 5-Androsten-3β-sulfate-17-one (DHEA sulfate) | 4.32 | 0.22 | None |  | None |
AN13 | 5β-Androstan-3α-ol-17-one (epiandrosterone) | 5.31 | 0.7 | 5.02 | 0.43 | None |
AN14 | 5β-Androstan-3α-ol-11,17-dione | 4.39 | 0.15 | 5.01 | 0.49 | None |
AN15 | 4-Androsten-17α-ol-3-one (epitestosterone) | 4.17 | 0.9 | None |  | None |
AN16 | 4-Androsten-17α-glucosiduronate-3-one (epitestosterone glucuronide) | 4.86 | 0.69 | None |  | None |
AN17 | 4-Androsten-17α-sulfate-3-one (epitestosterone sulfate) | 5.47 | 0.67 | None |  | None |
AN18 | 5β-Androstan-3α-glucosiduronate-17-one (etiocholanolone glucuronide) | None |  | None |  | None |
AN19 | 5α-Androstane | None |  | None |  | 100 |
AN20 | 5α-Androstan-3β-ol | 6.10 | 0.43 | 5.57 | 1.66 | 50 |
AN21 | 5α-Androst-16-en-3β-ol | 5.32 | 1.01 | 5.48 | 2.11 | 50 |
AN22 | 5α-Androst-16-en-3-one | 5.52 | 0.96 | 5.58 | 0.68 | 100 |
AN23 | 5β-Androstan-3α-ol | 5.85 | 1.12 | 5.59 | 0.33 | None |
AN24 | Androst-4,16-dien-3-one | 5.15 | 0.64 | 5.96 | 0.17 | 100 |
AN25 | Androst-5,16-dien-3β-ol | None |  | 5.60 | 1.50 | 100 |
 | ESTRANES |  |  |  |  |  |
ES1 | 1,3,5(10)-Estratrien-3,17β-diol (estradiol) | 4.80 | 0.34 | None |  | 200 |
ES2 | 1,3,5(10)-Estratrien-3-ol-17-one (estrone) | 4.42 | 0.47 | None | Â | 200 |
ES3 | 1,3,5(10)-Estratrien-3,16α,17β-triol (estriol) | None |  | None |  | 200 |
ES4 | 1,3,5(10)-Estratrien-3,16α-diol-17-one (16α-hydroxyestrone) | 5.60 | 0.42 | 5.70 | 0.17 | None |
ES5 | 1,3,5(10)-Estratrien-3-ol-4-methoxy-17-one (4-methoxyestrone) | 5.40 | 0.93 | 5.62 | 0.19 | None |
ES6 | 1,3,5(10)-Estratrien-3,15α,16α,17β-tetrol (estetrol) | 5.67 | 0.29 | None |  | 200 |
ES7 | 1,3,5(10)-Estratrien-2,3-diol-17-one (2-hydroxyestrone) | 5.44 | 0.93 | 5.74 | 0.19 | None |
ES8 | 1,3,5(10)-Estratrien-17-one-3-sulfate (estrone sulfate) | 5.47 | 0.43 | None | Â | None |
ES9 | 1,3,5(10)-Estratrien-17β-ol-3-glucosiduronate (estradiol glucuronide) | None |  | None |  | None |
ES10 | 1,3,5(10)-Estratrien-17β-ol-3-sulfate (estradiol sulfate) | 6.05 | 0.6 | None |  | 200 |
ES11 | 1,3,5(10)-Estratrien-17α-ethinyl-3,17β-diol (ethinyl estradiol) | 5.72 | 0.68 | None |  | 200 |