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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   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   200
PR7 4-Pregnen-3,20-dione (progesterone) 4.83 0.57 None   200
PR8 4-Pregnen-17-ol-3,20-dione 4.75 0.7 None   None
PR9 4-Pregnen-21-ol-3,20-dione (cortexone) 5.61 0.3 None   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
  1. Activities are in -log(EC50), with EC50 in molar units for the activation of human or zebrafish PXR. Efficacy is relative to 10 μM rifampicin (human PXR) or 20 μM 5α-androstan-3α-ol (zebrafish PXR) which are assigned an efficacy of 1.0. Toxicity is the lowest concentration in micromolar that produced significant toxicity in the HepG2 cells.