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. Author manuscript; available in PMC: 2013 Apr 15.
Published in final edited form as: Biochem Pharmacol. 2012 Feb 4;83(8):1112–1126. doi: 10.1016/j.bcp.2012.01.030

Table 2.

PXR antagonists

Compound Indications/Usage IC50 References
Et-743 Antineoplastic Agent 2 nM [92]
Ketoconazole And Its Analogues (Fluconazole And Enilconazol) Antifungal Agent 20 μM [239, 240]
Sulforaphane Dietary Isothiocyanate 12 μM [261]
Coumestrol Phytoestrogen 12 μM [262]
A-792611 HIV Protease Inhibitor 2 μM [263]
Polychlorinated Biphenyls Synthetic Hydrocarbon Compounds 10uM [264]
Camptothecin Antineoplastic Agent 0.58 μM [90]
Ecteinascidin-743 (ET-743) Antineoplastic Agent 3 nM [92]
Le unamide Pyrimidine Synthesis Inhibitor 6.8 μM [265]
Itraconazole Triazole Antifungal Agent 8.96 μM [265]
SPB03255 Identified By Using Ligand-Based And Structure-Based (Docking) In Silica Methods 5–25 μM [265]