Synonyms: Z-norendoxifen
Compound class:
Synthetic organic
Comment: Norendoxifen is an active metabolite of tamoxifen. In addition to acting as an estrogen receptor modulator, norendoxifen also inhibits aromatase enzyme activity (i.e. inhibits estrogen biosynthesis) [1-2]. We show the Z isomer here as it is more potent in terms of ER modulation and in vivo activity compared to the E isomer.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Lu WJ, Xu C, Pei Z, Mayhoub AS, Cushman M, Flockhart DA. (2012)
The tamoxifen metabolite norendoxifen is a potent and selective inhibitor of aromatase (CYP19) and a potential lead compound for novel therapeutic agents. Breast Cancer Res Treat, 133 (1): 99-109. [PMID:21814747] |
2. Lv W, Liu J, Lu D, Flockhart DA, Cushman M. (2013)
Synthesis of mixed (E,Z)-, (E)-, and (Z)-norendoxifen with dual aromatase inhibitory and estrogen receptor modulatory activities. J Med Chem, 56 (11): 4611-8. [PMID:23731360] |