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Table 3 Activation of human and zebrafish PXRs by xenobiotics and vitamins

From: Evolution of pharmacologic specificity in the pregnane X receptor

Cmp. #

Compound

hPXR Activity

hPXR Efficacy

zfPXR Activity

zfPXR Efficacy

Toxicity

MI1

Acetaminophen

None

 

None

 

None

MI2

3-Aminobenzoic acid

None

 

None

 

None

MI3

Benzo [a]pyren

4.75

0.55

4.00

0.06

100

MI4

n-Butyl-4-aminobenzoate

4.88

1.35

4.86

0.69

100

MI5

Butylbenzoate

None

 

None

 

None

MI6

Caffeine

None

 

None

 

None

MI7

Carbamazepine

4.20

0.37

None

 

200

MI8

Carbamazepine epoxide

4.09

0.57

None

 

200

MI9

β-Carotene

5.46

0.67

None

 

100

MI10

Chlorpyrifos

4.59

2.05

5.44

0.88

None

MI11

Chlorzoxazone

None

 

None

 

500

MI12

Cyclosporine

None

 

None

 

20

MI13

Ecdysone

None

 

None

 

None

MI14

Ethyl-2-aminobenzoate

None

 

None

 

None

MI15

Flurbiprofen

4.10

1.59

4.10

0.53

None

MI16

Folic acid

None

 

None

 

None

MI17

Guggulsterone

None

 

None

 

None

MI18

GW3965

None

 

None

 

10

MI19

Hyperforin

7.22

1.29

None

 

50

MI20

Mevastatin

5.23

0.51

None

 

15

MI21

Mycophenolic acid

None

 

None

 

None

MI22

Nifedipine

5.33

0.41

4.91

0.99

50

MI23

Oxcarbazepine

4.74

0.35

~4.70

~0.30

200

MI24

Paclitaxel

4.92

0.13

None

 

100

MI25

Phenobarbital

3.43

1.19

3.49

0.10

None

MI26

Phenytoin

4.26

0.52

None

 

200

MI27

n-Propyl-4-hydroxybenzoate

4.51

0.32

4.28

0.31

100

MI28

Provitamin D3

None

 

None

 

10

MI29

Provitamin D2

None

 

None

 

20

MI30

Reserpine

4.91

0.72

None

 

50

MI31

Retinol

5.80

0.20

None

 

50

MI32

Rifampicin

7.00

1.00

None

 

200

MI33

SR12813

6.41

0.90

None

 

10

MI34

TCDD

7.17

1.78

6.32

6.17

10

MI35

TCPOBOP

5.25

0.66

None

 

200

MI36

T-0901317

7.66

1.24

None

 

100

MI37

α-Tocopherol

~4.30

~0.25

None

 

100

MI38

β-Tocopherol

4.85

0.33

None

 

100

MI39

δ-Tocopherol

5.14

0.64

None

 

100

MI40

γ-Tocopherol

None

 

None

 

100

MI41

1α,25-Dihydroxyvitamin D3

None

 

None

 

50

MI42

1α-Hydroxyvitamin D2

None

 

None

 

50

MI43

1α-Hydroxyvitamin D3

None

 

None

 

50

MI44

Vitamin K1

4.99

0.13

None

 

100

MI45

Vitamin K2

5.04

0.80

None

 

100

MI46

Vitamin K3

~4.30

~0.15

None

 

100

  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.