Binding and function of estrogenic compounds toward GPER

 17β-Estradiolagonist3–6 nMB/F(Revankar et al., 2005; Thomas et al., 2005)
 17α-Estradiolunknown>10 μMB/F(Thomas et al., 2005)
 Estroneunknown>>10 μMB(Thomas et al., 2005)
 Estriolantagonist>1 μMB/F(Thomas et al., 2005; Lappano et al., 2010)
 2-Hydroxy E2antagonist0.1–1 μMB/F(Chourasia et al., 2015)
 2-Methoxy E2agonist10 nMB(Koganti et al., 2013)
 AldosteroneagonistNone detectedB/F(Gros et al., 2011; Brailoiu et al., 2013; Cheng et al., 2014)
 7β-Hydroxy-epiandrosteroneantagonist< 1 nMF(Sandra et al., 2012)
 Estradiol-17β-d-glucuronideagonist50 μM*F(Zucchetti et al., 2014)
 4-OHTagonist0.1–1 μMB/F(Revankar et al., 2005; Thomas et al., 2005; Vivacqua et al., 2006a,b)
 ICI 182,780agonist1 μM*F(Filardo et al., 2000)
 Raloxifeneagonist100 nM*F(Petrie et al., 2013)
 BT-SERMsagonists10–100 nM*F(Abdelhamid et al., 2011)
 DESunknown>1 μMB(Thomas et al., 2005; Pang et al., 2008)
 Ethynylestradiolagonistin vivo dosingF(Yates et al., 2010)
 Genisteinagonist133 nMB/F(Maggiolini et al., 2004; Thomas and Dong, 2006; Vivacqua et al., 2006a)
 Oleuropeinagonist∼200 μMF(Chimento et al., 2014a)
 Hydroxytyrosolagonist∼100 μMF(Chimento et al., 2014a)
 Resveratrolagonist∼300 μMF(Dong et al., 2013)
 Equolagonist100 nMF(Rowlands et al., 2011)
 Quercetinagonist1 μM*F(Maggiolini et al., 2004)
 Tectoridinagonist10 μM*F(Kang et al., 2009)
 Zearalenoneunknown0.8 μMB(Thomas et al., 2005; Thomas and Dong, 2006)
 Daidzeinagonist< 1 nMF(Kajta et al., 2013)
 Apigeninagonist20–50 μMF(Palmieri et al., 2012)
 Atrazineagonist>10 μMB/F(Thomas and Dong, 2006; Albanito et al., 2008)
 Bisphenol Aagonist0.6 μMB/F(Thomas and Dong, 2006; Pupo et al., 2012)
 Nonylphenolagonist0.8 μMB/F(Thomas and Dong, 2006)
 Keponeagonist1.4 μMB/F(Thomas and Dong, 2006)
p,p′-DDTunknown2.8 μMB(Thomas and Dong, 2006)
 2,2′,5′,-PCB-4-OHunknown3.8 μMB(Thomas and Dong, 2006)
o,p′-DDEagonist7.1 μMB/F(Thomas et al., 2005; Thomas and Dong, 2006)
 Methoxychlorunknown∼10 μMB(Thomas and Dong, 2006)
p,p′-DDEunknown∼10 μMB(Thomas and Dong, 2006)
o,p′-DDTunknown>>10 μMB(Thomas and Dong, 2006)
Synthetic Ligands
 G-1agonist7-11 nMB/F(Bologa et al., 2006; Dennis et al., 2009)
 G15antagonist20 nMB/F(Dennis et al., 2009)
 G36antagonist∼20 nMF(Dennis et al., 2011)
 MIBEantagonist∼5 μMB/F(Lappano et al., 2012b)
 STXagonist∼100 nMF(Lin et al., 2009)
 GPER-L1agonist100 nMB/F(Lappano et al., 2012a)
 GPER-L2agonist100 nMB/F(Lappano et al., 2012a)
 PPTagonist∼10–100 nMF(Petrie et al., 2013)
 DPNunknown>>1 μMF(Petrie et al., 2013)
  • a Reports the functional activity of the compound, where known. From studies of binding activity only, the activity is stated as unknown.

  • b Affinity/Efficacy values are based on direct (Kd) or competition (IC50) binding assays (where available) or EC50 values based on functional dose responses. In some reports, only a single dose (or limited doses) is used in functional assays, and that value (or a range for the EC50) is provided (*). Where quantitation of a dose response is not provided, the estimated value (or range) is provided (∼). None detected, indicates binding assays have been performed and no binding was detected. In vivo dosing, indicates that only functional animal studies have been carried out. >, < and > >, indicate that the half maximal response was not achieved at the indicated concentration (> indicates some effect at indicated concentration but less than 50%; > > indicates substantially less than 50% effect at stated concentration; < indicates that similar effects were observed at all doses tested and therefore it is presumed that the EC50 is below the lowest dose reported).

  • c Indicates whether the reported value is derived from a binding assay (B), functional assay (F), or has been assessed with both (B/F), with the binding constant being provided in the previous column.