Template:Absolute activities of tibolone and metabolites

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Absolute activities (nM) of tibolone and metabolites

Compound Code name PR AR ERα ERβ GR MR
Template:No selflink ORG-OD-14 123 1.05 4 105 2410* 170*
Template:No selflink ORG-OM-38 46 0.2 26 300 1760* 30*
Template:No selflink ORG-4094 2400* 135* 1.7 100 ND* 1160*
Template:No selflink ORG-30126 20000* ND* 2.4 115 ND* 3310*
Notes: Values are affinities (nM). Non-italicized values are EC50. Italicized values with an asterisk (*) are IC50. Reference ligands (EC50) were promegestone (5 nM for PR), metribolone (0.1 nM for AR), estradiol (0.018 nM for ERα, 0.08 nM for ERβ), dexamethasone (6 nM for GR), and aldosterone (0.36 nM for MR). Sources: [1]
Template documentation

References

  1. Escande A, Servant N, Rabenoelina F, Auzou G, Kloosterboer H, Cavaillès V, Balaguer P, Maudelonde T (August 2009). "Regulation of activities of steroid hormone receptors by tibolone and its primary metabolites". J. Steroid Biochem. Mol. Biol. 116 (1–2): 8–14. doi:10.1016/j.jsbmb.2009.03.008. PMID 19464167.