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Table 2 Effects of selenophene- and thiophene-core ligand conjugates on the transcriptional activities of estrogen receptors α and β

From: Selenophene and thiophene-core estrogen receptor ligands that inhibit motility and development of parasitic stages of Haemonchus contortus

 

Agonist modea

Antagonist modeb

 

ERα

ERβ

ERα

ERβ

Cmpd

EC50 (μM)

Efficacy (%E2)

EC50 (μM)

Efficacy (%E2)

IC50 (μM)

Efficacy (%E2)c

IC50 (μM)

Eff (%E2)

WZY-2

–

-21 ± 13

–

–

–

73 ± 8

3.02

13.9 ± 5.3

MJ-22

0.47

117 ± 8

0.61

277 ± 15

–

–

–

–

MJ-17

0.045

90 ± 7

0.203

57 ± 3

–

–

–

–

  1. aLuciferase activity was measured in HEK 293 T cells transfected with 3 × estrogen response element (ERE)-driven luciferase reporter and expression vectors encoding estrogen receptor α (ERα) or ERβ and treated in triplicate with increasing doses (up to 10-5 M) of the compounds. Half maximal effective concentrations (EC50) and standard deviation (mean ± SD), shown as a percentage of 10-8 M 17β-estradiol (E2), were determined
  2. bHalf maximal inhibitory concentrations (IC50) and standard deviation (mean ± SD) were determined in the percentage of 10-8 M 17β-estradiol (E2) on ERα or ERβ
  3. cERs have considerable basal activity in HEK 293 T cells. Omitted EC50 or IC50 values were too high to be determined accurately