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. 2015 Feb 25;156(5):1887–1899. doi: 10.1210/en.2014-1852

Table 1.

Specificity of ESR Agonists on Full-Length of ESR or Gal4-Ligand Binding Domain of ESR Fusion Protein in Transactivation

ESR1 Full Length on ERE
ESR2 Full Length on ERE
EC50 (M) RP (%) RE (%) ESR1/ESR2 of EC50 EC50 (M) RP (%) RE (%) ESR2/ESR1 of EC50
E2 9.66 × 10−12 100.0 100.0 0.2 5.55 × 10−11 100.0 100.0 5.7
PPT 1.67 × 10−10 5.8 128.3 0.0 1.83 × 10−7 0.0 41.5 1093.0
DPN 1.08 × 10−8 0.1 117.6 7.6 1.42 × 10−9 3.9 113.6 0.1
FERb 033 2.53 × 10−7 0.0 148.9 4.7 5.38 × 10−8 0.1 96.9 0.2
WAY 200070 1.94 × 10−7 0.0 138.9 82.8 2.35 × 10−9 2.4 79.7 0.0
ESR1 LBD-GAL4
ESR2 LBD-GAL4
EC50 (M) RP (%) RE (%) ESR1/ESR2 of EC50 EC50 (M) RP (%) RE (%) ESR2/ESR1 of EC50
E2 2.08 × 10−9 100.0 100.0 1.07 1.93 × 10−9 100.0 100.0 0.93
PPT 2.37 × 10−9 87.6 71.5 N/A N.D. N/A N.D. N/A
DPN 1.36 × 10−7 1.5 102.5 29.12 4.66 × 10−9 41.5 100.5 0.03
FERb 033 1.13 × 10−6 0.2 76.0 5.84 1.49 × 10−7 1.3 48.1 0.13
WAY 200070 6.62 × 10−7 0.3 93.8 47.17 1.40 × 10−8 13.8 83.3 0.02

RP, relative potency = (EC50 of E2/EC50 of other agonist) × 100; RE, relative efficacy = maximum response % of E2 found at any doses.