Skip to main content
. Author manuscript; available in PMC: 2014 Dec 15.
Published in final edited form as: Anal Biochem. 2013 Sep 14;443(2):10.1016/j.ab.2013.09.009. doi: 10.1016/j.ab.2013.09.009

Table 1.

Summary of the Activity of a Panel of hPXR Ligands

Activity in This Study, Using BODIPY FL vinblastine as Probe Activity Reported, Using Fluormone PXR (SXR) Green as Probe

Chemical IC50 K i IC50a K i b
TO901317 159 nM 116 nM 44 nM [12], 52 nM [24], 90 nM[13] 22 nM, 26 nM, 45 nM
SR12813 157 nM 114 nM 42 nM [15], 49 nM [11], 69 nM [24], 140 nM [16], 710 nM[13] 21 nM, 24.5 nM, 34.5 nM 70 nM, 355 nM
Clotrimazole 1.94 μM 1.41 μM 2.0 μM [24] 1.0 μM
Rifampicin 12.7 μM 9.26 μM 14.13 μM [24] 7.06 μM
Hyperforin 147 nM 107 nM 140 nM [24], 710 nM [13] 70 nM, 355 nM
Ginkgolide A 13.7 μM 9.99 μM 54% (1000 μM) [14] NAc
Ginkgolide B 12.1 μM 8.82 μM 48% (1000 μM) [14] NA
a

Values obtained from published reports (see References)

b

Values calculated from published data by using equation 2 (see Methods)

c

NA: Not applicable