FSHR agonist 1 is a high affinity and allosteric follicle stimulating hormone receptor (FSHR) agonist with a pEC50 of 7.72. FSHR agonist 1 formes extensive interactions with the TMD to directly activate FSHR[1].
FSHR agonist 1 (compound 21f) 与 FSHR TMD 口袋的结合诱导 TM6 和 TM7 向内运动，这直接导致 FSHR 激活[1]。
FSHR agonist 1 (compound 21f) 可以高效激活 FSHR、LHCGR 和 TSHR，而对 FSHR 的激活效力比 LHCGR（pEC50 为 6.26）和 TSHR（pEC50 为 6.48）高 10 倍以上[1]。
[1]. Jia Duan, et al. Universal mechanism of hormone and allosteric agonist mediated activation of glycoprotein hormone receptors as revealed by structures of follicle stimulating hormone receptor. biorxiv. August 01, 2022.