TABLE 4

Ligands acting at RXFP4

LigandBinding Affinity pKi, pKDcAMP pEC50GTPγS pEC50Reference
hINSL5AG7.338.51Shabanpoor et al. (2012)
hINSL5AG7.598.62Belgi et al. (2013)
hINSL5AG8.668.94Zhu et al. (2008)
hINSL5AG8.88.928.89Liu et al. (2005b)
hINSL5 amideAG6.947.48Belgi et al. (2011)
mINSL5AG8.479.29Belgi et al. (2013)
mINSL5 amideAG7.076.85Belgi et al. (2011)
Relaxin-3AG8.819.01Zhu et al. (2008)
Relaxin-3AG8.839.02Kuei et al. (2007)
Relaxin-3 B-chainAG7.077.06∼7.0Liu et al. (2003b)
Relaxin-3 B-chainAG6.9Liu et al. (2005a)
R3/I5AG8.929.04Liu et al. (2005a)
R3/I5AG8.888.94Kuei et al. (2007)
Minimized hINSL5 analog 7PA6.287.40Belgi et al. (2013)
Relaxin-3AG8.94Shabanpoor et al. (2012)
Minimized relaxin-3 analog 2AG7.17.7Shabanpoor et al. (2012)
Minimized relaxin-3 analog 3ANT6.6N.A.Shabanpoor et al. (2012)
R3(BΔ23–27)R/I5ANT∼8N.D.Haugaard-Kedstrom et al. (2011)
R3(BΔ23–27)R/I5ANT8.64N.A.Kuei et al. (2007)
R3 B1–22RN.A.N.D.Haugaard-Kedstrom et al. (2011)
  • AG, agonist; ANT, antagonist; N.A., no activity; PA, partial agonist.