Table 1 Functional and biochemical evaluation of PXR modulators

From: Chemical manipulation of an activation/inhibition switch in the nuclear receptor PXR

Compound

Bindinga IC50 (nM)

Agonismb IC50 (nM)

Antagonismc IC50 (nM)

T0901317

27 ± 3

NTd

NT

Rifampicin

NT

830 ± 40

NT

SPA70

230 ± 30

NAe

210 ± 30

SJPYT-278

23 ± 4

NA

12 ± 3

SJPYT-312f

15 ± 3

NA

7.4 ± 0.6

SJPYT-313g

23 ± 3

NA

51 ± 9

SJPYT-326

8.7 ± 0.2

15 ± 0.9

NA

SJPYT-327

21 ± 6

NA

23 ± 3

SJPYT-328

48 ± 10

7.1 ± 0.6

NA

SJPYT-330

14 ± 4

NA

34 ± 4

SJPYT-331

3.6 ± 0.8

NA

7.1 ± 0.8

  1. aPXR LBD binding assay (TR-FRET), where displacement of the fluorescence-labeled probe results in decreasing signal.
  2. bCell-based assay in agonistic mode, where agonists increase signal.
  3. cCell-based assay in antagonistic mode, where cells are incubated with rifampicin (5 μM) and antagonists reduce the rifampicin-induced signal.
  4. dNT: not tested.
  5. eNA: no IC50 value could be determined experimentally within the concentration range tested.
  6. fCorresponding to the (S)-enantiomer.
  7. gCorresponding to the (R)-enantiomer.
  8. All data were calculated from n = 3 independent experiments. Source data are provided as a Source Data file.
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