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.