FSHR agonist 1 is a high affinity and allosteric follicle stimulating hormone receptor (FSHR) agonist with a pEC 50 of 7.72. FSHR agonist 1 formes extensive interactions with the TMD to directly activate FSHR
In Vitro
The binding of FSHR agonist 1 (compound 21f) to the FSHR TMD pocket induces inward movements of TM6 and TM7, which directly results in FSHR activation. FSHR agonist 1 (compound 21f) can activate FSHR, LHCGR and TSHR with highly potency and efficacy, while the activation potency for FSHR is more than 10-fold higher than LHCGR (pEC 50 of 6.26) and TSHR (pEC 50 of 6.48). MCE has not independently confirmed the accuracy of these methods. They are for reference only.