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. 2020 Jun 29;10:10579. doi: 10.1038/s41598-020-67473-w

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© The Author(s) 2020

Open Access This article is licensed under a Creative Commons Attribution 4.0 International License, which permits use, sharing, adaptation, distribution and reproduction in any medium or format, as long as you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in a credit line to the material. If material is not included in the article’s Creative Commons license and your intended use is not permitted by statutory regulation or exceeds the permitted use, you will need to obtain permission directly from the copyright holder. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/.

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GnRHR pharmacoperone assay principle. (A) The GnRHR agonist, GnRH, stimulates the GPCR, activating the Gq subunit to stimulate IP3 to cause a release of intracellular calcium. The fluorescence of the Ca²⁺-sensitive dye Fluo2 is measured in the FLIPR kinetically, with pharmacoperones such as SR-01000435409 causing an increase in RFU signal over time compared to no pharmacoperone. (B) The IP-One TR-FRET assay utilizes the same pathway but, detects the binding of IP1 to the tagged antibody. The increase in IP1 present from the activation of Gq by GnRH, with the activity of the pharmacoperone, based on competition for the TR-FRET Ab, results in a decrease the overall TR-FRET signal.