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. 2015 Feb 25;17(1):27. doi: 10.1186/s13058-015-0529-8

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© Singh et al.; licensee BioMed Central. 2015

This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.

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The lead compounds did not displace oestradiol from the hormone-binding site of oestrogen receptor-alpha. Dose–response curve (3 to 150 μM) of (A) VPC-13002, (B) VPC-16225, (C) VPC-16230 and (D) oestradiol (E2) (0.01 to 1000 nM; half-maximal inhibitory concentration: 4.2 nM) for displacement of fluorescein-labelled E2 in fluorescence polarisation assays. Data were fitted using GraphPad Prism 5 to calculate the log of the concentration of the inhibitors versus polarisation.