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Table 1 Relative potencies calculatedA from published human ERα transactivation results

From: Human-relevant potency threshold (HRPT) for ERα agonism

Chemical Mean
relative
potency
Median
relative
potency
Range Data sources
Hormones
 17β-estradiol 1.0E+00 All sources
 Estrone 3.5E−02 2.9E−02 1.0E−02 to 7.5E−02 B, K1, K2, K3, P, Y
 Estriol 1.4E−01 8.3E−02 3.3E−02 to 4E−01 B, K1, K2, K3, P
Pharmaceuticals
 17α-estradiol 2.6E−02 2.6E−02 5.3E−03 to 4.7E−02 B, Y
 17α-ethinyl estradiol 2.1E+00 1.3E+00 1.1E+00 to 5.7E+00 B, K1, K2, K3, P, Y
 Diethylstilbestrol 2.0E+00 1.4E+00 2.5E−01 to 8.0E+00 B, C, G, K1, K2, K3, L, O
 Tamoxifen 1.6E−05 8.3E−06 7.1E−07 to 4E−05 K1, K2, K3
Botanicals
 Equol 2.4E−03 3.6E−04 1.8E−04 to 1E−02 F, G, H, J, L, Q, S
 Dehydroequol NA 6.3E−05 NA Q
 Coumestrol 8.3E−03 1.0E−03 4.0E−05 to 8.0E−02 B, C, G, J, K1, K2, K3, L, P, S, U
 Genistein 1.3E−03 4.5E−04 1.2E−05 to 1.0E−02 B, C, D, E, F, H, J, K1, K2, K3, L, N1, N2, O, P, Q, S, T, U, Y
 Genistein glucuronide NA 6.7E−07 NA T
 Daidzein 1.8E−04 4.7E−05 2.7E−06 to 9.7E−04 B, C, D, E, F, H, J, N1, N2, O, P, Q, S, T
 Daidzein glucuronide NA 6.7E−08 NA T
 O-DMA (daidzein metabolite) NA 1.4E−04 NA S
 347-IF (daidzein metabolite) 6.1E-05 6.1E−05 2.8E−06 to 1.2E−04 L, S
 674-IF (daidzein metabolite) NA 6.0E−05 NA L
 Resveratrol 1.0E−04 1.0E−04 1.3E−07 to 2E−04 L, S
 Resveratrol-3-O-SO4 NA 1.4E−05 NA M
 Biochanin A 2.2E−04 1.5E−04 2.5E−06 to 6.2E−04 C, D, E, F, H, J, P, S
 Formononetin 2.4E−04 2.4E−04 9.6E−06 to 4.9E−04 D, E, F, J, S
 Zearalenol NA 7.0E−02 NA C
 Zearalenone 4.5E−01 3.4E−01 5.1E−03 to 1E+00 C, L, Y
 Enterolactone 4.7E−05 2.1E−06 1.0E−07 to 1.4E−04 S, L, V
 Enterodiol NA 3.5E−07 NA S
 Sesamol NA 2.0E−06 NA V
 Sesamin 3.3E−05 2.3E−05 2E−07 to 7.7E−05 H, J, V
 Sesamolin NA 6.7E−08 NA V
 Apigenin 9.7E−05 9.7E−05 3.4E−06 to 1.9E−04 J, S
 Naringenin 6.1E−05 2.3E−05 1.9E−06 to 2E−04 C, H, J, S, W2
 8-Prenylnaringenin (8-PN) 7.0E−02 8.6E−02 1E−02 to 1E−01 W1, W2, X1, X2
 6-(l,l-dimethylallyl)naringenin 1.3E−02 1.7E−03 1E−03 to 1E−02 W1, W2, X2
 8-PN-OH (metabolite of 8-PN) 2.1E−03 2.1E−03 1E−01 to 3.1E−03 X1, X2
 8-PN-O (metabolite of 8-PN) NA 1.4E−03 NA X1
 α-Erythroidin 1.1E−03 1.1E−03 1.0E−03 to 1.2E−03 R1, R2
 β-Erythroidin 5.0E−04 5.0E−04 5E−04 to 5E−04 R1, R2
Androgens
 Testosterone NA 7.1E−06 NA B
 Dihydrotestosterone NA 9.6E−06 NA Y
 Methyltestosterone NA 2.5E−06 NA B
 19-Nortestosterone NA 4.7E−06 NA B
Test case chemical
 D4 NA 5.0E-06 NA I
  1. Individual potency values for this table are found in electronic supplementary material
  2. AUnless provided in the publication, Relative Potencies were derived by dividing an EC% value of the primary endogenous human estrogen, 17β-estradiol, by the equivalent EC% value of each chemical. EC% values were either extracted from tables or interpolated from figures. Where necessary, concentrations were adjusted to better approximate equivalent EC% values. NA not applicable
  3. BValues derived from Table 4-1; ICCVAM 2011. [BG1Luc]
  4. CValues derived from Table 3; Jefferson et al. 2002. [BG1Luc]
  5. DValues derived from Table 2; Dornstauder et al. 2001. [YES]
  6. EValues derived from Table 3; Beck et al. 2003. [YES]
  7. FValues derived from Table 2; Pfitscher et al. 2008. [YES]
  8. GValues derived from Fig. 1; Coldham et al. 1997. [YES]
  9. HValues derived from Table 1; Breinholt and Larsen 1998. [YES]
  10. IValues taken from Fig. 4; Quinn et al. 2007. [MCF-7]
  11. JValues from Table 3; Procházková et al. 2017. [HeLa-9903]
  12. KValues from Table 2; Gutendorf and Westendorf 2001
  13. LValues from Fig. 3a RP ratios; Mueller et al. 2004. [Ishikawa EREα]
  14. MValues from Table 1; Ruotolo et al. 2013. [YES]
  15. NValues from Fig. 1; Chrzan and Bradford 2007. [N-1: MCF-7 / N-2: G-292]
  16. OValues from Table 1; Chu et al. 2009. [YES-SRC-1]
  17. PValues from Table 2; Escande et al. 2006. [HELN]
  18. QValues from Table 2; De Angelis et al. 2005. [HEC-1]
  19. RValues from Figs. 2, 3; Djiogue et al. 2014. [R-1: MVLN / R-2: U2OS]
  20. SValues from Table 1; Takeuchi et al. 2009. [CHO]
  21. TValues from Table 1; Islam et al. 2015. [U2OS]
  22. UValues from Table 2; Harris et al. 2005. [MCF-7]
  23. VValues from Pianjing et al. 2011. [TD47-KBLuc]
  24. WValues from Zierau et al. 2002. [W-1: YES / W-2: MVLN]
  25. XValues from Zierau et al. 2004. [X-1: YES / X-2: MVLN]
  26. YValues from Table 1 (PC10, PC50), Yamasaki et al. 2002b. [HeLa229]