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Table 4 Activation of mouse, rat, rabbit, and chicken PXRs

From: Evolution of pharmacologic specificity in the pregnane X receptor

Cmp # Compound Mouse PXR Activity (efficacy, ε, in parentheses) Rat PXR Activity (efficacy, ε, in parentheses) Rabbit PXR Activity (efficacy, ε, in parentheses) Chicken PXR Activity (efficacy, ε, in parentheses)
BI004 Murideoxycholic acid 5.09 (ε = 0.76) 4.80 (ε = 0.22) 4.52 (ε = 1.86) No effect
BI005 Chenodeoxycholic acid No effect No effect 4.70 (ε = 0.42) 4.70 (ε = 0.36)
BI008 Deoxycholic acid No effect 5.00 (ε = 0.32) 4.44 (ε = 0.37) No effect
BI011 Lithocholic acid 4.86 (ε = 0.48) 4.78 (ε = 0.42) 4.80 (ε = 0.70) 5.09 (ε = 0.17)
BI020 Cholic acid No effect 4.82 (ε = 0.42) 4.02 (ε = 0.67) 4.47 (ε = 0.36)
BI023 5β-Cholestan-3α,7α,12α-triol 5.85 (ε = 1.23) 5.65 (ε = 0.72) 5.41 (ε = 0.37) 5.89 (ε = 0.27)
BI034 5β-Scymnol sulfate 4.44 (ε = 0.85) 4.40 (ε = 0.85) 4.09 (ε = 1.93) 4.37 (ε = 0.88)
BI036 5α-Cyprinol sulfate 4.78 (ε = 0.29) 4.50 (ε = 0.28) 4.09 (ε = 0.43) 4.51 (ε = 0.61)
BI038 3α,7α,12αtTrihydroxy-5β-cholestan-27-oic acid, taurine conjugated No effect No effect No effect No effect
BI046 Tauro-β-muricholic acid No effect No effect No effect No effect
BI047 7α-Hydroxycholesterol No effect No effect No effect No effect
PR2 5β-Pregnane-3,20-dione 5.36 (ε = 0.84) 5.24 (ε = 1.01) 4.90 (ε = 1.0) 5.59 (ε = 0.81)
MI3 Benzo [a]pyren 4.86 (ε = 0.94) 4.85 (ε = 0.45) No effect 4.40 (ε = 0.50)
MI4 n -Butyl- p -aminobenzoate No effect < 4 < 4 > 100
MI22 Nifedipine 4.64 (ε = 0.51) 5.26 (ε = 0.68) 4.61 (ε = 0.29) 6.14 (ε = 1.00)
MI34 TCDD (2,3,7,8-tetrachlorodienzo- p -dioxin) 7.00 (ε = 1.60) 6.70 (ε = 0.83) No effect 7.04 (ε = 0.06)
AN1 5α-Androstan-3α-,17β-diol     5.07 (ε = 2.28)
AN3 5α-Androstan-3α-ol     5.38 (ε = 0.85)
AN21 5α-Androst-16-en-3β-ol     5.14 (ε = 2.99)
AN22 5α-Androst-16-en-3-one     4.99 (ε = 0.77)
BI031 Allocholic acid     No effect
BI006 Glycochenodeoxycholic acid     4.60 (ε = 0.41)
BI007 Taurochenodeoxycholic acid     No effect
BI009 Glycodeoxycholic acid    4.81 (ε = 0.40)  
BI010 Taurodeoxycholic acid    4.84 (ε = 0.15)  
BI017 ω-Muricholic acid No effect No effect   
BI018 α-Muricholic acid 4.59 (ε = 2.63) 3.95 (ε = 1.31)   
BI019 β-Muricholic acid No effect No effect   
BI021 Glycocholic acid No effect No effect   No effect
BI022 Taurocholic acid 4.07 (ε = 0.93) No effect   No effect
BI042 7-Ketodeoxycholic acid    4.31 (ε = 1.55)  
PR13 Pregenolone 16α-carbonitrile 6.41 (ε = 1.0) 6.20 (ε = 1.0)   
  1. Activities are in -log(EC50), with EC50 in molar units for the activation of mouse, rat, rabbit, or chicken PXRs. Efficacy is relative to 20 μM pregnenolone 16α-carbonitrile (mouse and rat PXRs), 50 μM 5α-pregnan-3,20-dione (rabbit PXR), or 20 μM nifedipine (chicken PXR) which are assigned an efficacy of 1.0. The training set consists of the 16 compounds highlighted in bold font.