Table 2 Activation of human and zebrafish PXRs by pregnane steroids and related compounds
From: Evolution of pharmacologic specificity in the pregnane X receptor
Cmp. # | Compound | hPXR Activity | hPXR Efficacy | zfPXR Activity | zfPXR Efficacy | Toxicity |
|---|---|---|---|---|---|---|
PR1 | 5β-Pregnan-3α,20α-diol (5β-pregnanediol) | 5.29 | 0.34 | None |  | 100 |
PR2 | 5β-Pregnan-3,20-dione (5β-pregnanedione) | 5.59 | 0.97 | 6.08 | 0.85 | None |
PR3 | 4-Pregnen-11β,21-diol-3,20-dione (corticosterone) | 5.00 | 0.54 | None |  | None |
PR4 | 4-Pregnen-17,21-diol-3,20-dione (cortexolone) | 4.64 | 0.49 | None | Â | None |
PR5 | 4-Pregnen-11β,21-diol-3,18,20-trione (aldosterone) | 4.26 | 0.21 | None |  | None |
PR6 | 4-Pregnen-17,21-diol-3,11,20-trione (cortisone) | 4.16 | 0.28 | None | Â | 200 |
PR7 | 4-Pregnen-3,20-dione (progesterone) | 4.83 | 0.57 | None | Â | 200 |
PR8 | 4-Pregnen-17-ol-3,20-dione | 4.75 | 0.7 | None | Â | None |
PR9 | 4-Pregnen-21-ol-3,20-dione (cortexone) | 5.61 | 0.3 | None | Â | 200 |
PR10 | 4-Pregnen-3β,17,21-triol-3,20-dione (cortisol) | 4.32 | 0.66 | None |  | None |
PR11 | 5-Pregnen-3β,17-diol-20-one | 4.47 | 0.36 | None |  | None |
PR12 | 5-Pregnen-3β-diol-20-one (pregnenolone) | 5.64 | 1.26 | 6.32 | 2.05 | None |
PR13 | 5-Pregnen-16α-cyano-3β-ol-20-one | None |  | None |  | None |
PR14 | 5α-Pregnan-3α-ol-20-one (allopregnanolone) | 5.38 | 0.46 | 5.40 | 0.30 | None |
PR15 | 5α-Pregnan-3α,20α-diol (allopregnanediol) | 4.28 | 0.16 | 4.58 | 0.29 | None |
PR16 | 5β-Pregnan-3α,20α-diol-3-glucosiduronate (pregnanediol glucuconide) | 4.26 | 0.17 | 4.78 | 1.42 | None |
PR17 | 5β-Pregnan-3α,11β,17,20α-21-pentol (cortol) | 4.33 | 0.83 | 3.95 | 0.98 | 200 |
PR18 | 5β-Pregnan-3α,17,20α-21-tetrol-11-one (cortolone) | 4.35 | 0.72 | 4.34 | 0.25 | 200 |
PR19 | 5β-Pregnan-3α,17,21-triol-11,20-dione | 4.28 | 0.8 | 4.43 | 0.33 | None |
PR20 | 5α-Pregnan-3α,11β,21-triol-20-one | 4.90 | 0.26 | None |  | None |
PR21 | 4-Pregnen-17α,20β-diol-3,20-dione | None |  | None |  | 200 |
PR22 | 4-Pregnen-20β-ol-3,20-dione-17α-sulfate | 5.73 | 0.66 | None |  | None |
PR23 | 5β-Pregnan-3α,20β-diol | 5.42 | 0.49 | 5.95 | 0.25 | None |
PR24 | 5β-Pregnan-3α,11β,17,21-tetrol-20-one | 4.33 | 0.73 | 3.94 | 0.11 | None |
PR25 | 5β-Pregnan-3α-ol-20-one | 4.98 | 0.55 | 6.64 | 1.22 | 100 |
PR26 | 5-Pregnen-20-one-3β-sulfate | None |  | 4.95 | 0.23 | None |
PR27 | 4-Estren-17α-ethynyl-18-homo-17β-ol-3-one (levonorgestrel) | 5.37 | 0.35 | 6.00 | 0.86 | None |
PR28 | 4-Estren-17α-ethynyl-17β-ol-3-one (norethindrone) | 4.59 | 0.32 | 5.85 | 0.40 | None |
PR29 | 1,4-Pregnadien-9α-fluoro-16α-methyl-11β,17,21-triol-3,20-dione (dexamethasone) | 4.39 | 0.83 | None |  | None |