Ligands that interact with RXFP1

LigandBinding Affinity pKi, pKDcAMP pEC50pERK1/2 pEC50Reference
Human relaxin-1AG8.849.1Bathgate et al. (2006b)
RelaxinAG9.2410.37Hossain et al. (2008)
RelaxinAG9.759.39Bathgate et al. (2013a)
RelaxinAG9.719.60Siwek et al., unpublished
RelaxinAG16.96, 9.46Halls and Cooper (2010)
A(4–24)(B7–24)H2AG6.998.22Hossain et al. (2011)
A(4–24)(B7–24)H2AG8.368.24Siwek et al., unpublished
Relaxin-3AG7.699.36Hossain et al. (2008)
Relaxin-3AG8.68.74Shabanpoor et al. (2012)
Relaxin-3AG8.858.57Siwek et al., unpublished
INSL3AG5.68N.A.Bathgate et al. (2013a)
B−R13/17KH2PA6.296.67Hossain et al. (2010)
B−R13/17KH2 (AT-001)PA5.035.66Silvertown et al. (2007), Neschadim et al. (2014)
B−R13/17KH2PA7.598.41 (7.97 ant)Siwek et al., unpublished
A(4–24)(F23A)H2AG9.179.82Chan et al. (2012)
Minimized relaxin-3 analog 2AG<5N.A.Shabanpoor et al. (2012)
Minimized relaxin-3 analog 3<5N.D.Shabanpoor et al. (2012)
ML290AAN.A.7.03N.A.Xiao et al. (2013)
  • AA, allosteric agonist; AG, agonist; BA, biased agonist; N.A., no activity; N.D., not determined; PA, partial agonist.