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. 2023 Feb 27;120(10):e2217804120. doi: 10.1073/pnas.2217804120

Table 1.

PXR LBD binding activities of rifampicin analogs

Compound Group PXR LBD binding [IC50 ± SD (µM)] FC*
T0901317 NA 0.004 ± 0.0003 0.0015
SR12813 NA 0.026 ± 0.003 0.0096
Rifampicin 1 2.7 ± 0.4 1
Rifamycin O 1 4.1 ± 0.4 1.5
Rifaximin 1 11.4 ± 3.3 4.2
Rifabutin 1 11.8 ± 4.4 4.4
Rifapentine 1 5.7 ± 1.6 2.1
Rifamycin 2 0.067 ± 0.009 0.025
3-Formyl Rifamycin 2 0.054 ± 0.01 0.020
Rifamycin S 2 0.054 ± 0.014 0.020
3-Bromo Rifamycin S 2 0.057 ± 0.011 0.021

*FC, fold change, calculated by dividing a compound’s IC50 value by that of rifampicin.