Ligands that interact with RXFP1
| Ligand | Binding Affinity pKi, pKD | cAMP pEC50 | pERK1/2 pEC50 | Reference | |
|---|---|---|---|---|---|
| Human relaxin-1 | AG | 8.84 | 9.1 | Bathgate et al. (2006b) | |
| Relaxin | AG | 9.24 | 10.37 | Hossain et al. (2008) | |
| Relaxin | AG | 9.75 | 9.39 | Bathgate et al. (2013a) | |
| Relaxin | AG | 9.71 | 9.60 | Siwek et al., unpublished | |
| Relaxin | AG | 16.96, 9.46 | Halls and Cooper (2010) | ||
| A(4–24)(B7–24)H2 | AG | 6.99 | 8.22 | Hossain et al. (2011) | |
| A(4–24)(B7–24)H2 | AG | 8.36 | 8.24 | Siwek et al., unpublished | |
| Relaxin-3 | AG | 7.69 | 9.36 | Hossain et al. (2008) | |
| Relaxin-3 | AG | 8.6 | 8.74 | Shabanpoor et al. (2012) | |
| Relaxin-3 | AG | 8.85 | 8.57 | Siwek et al., unpublished | |
| INSL3 | AG | 5.68 | N.A. | Bathgate et al. (2013a) | |
| B−R13/17KH2 | PA | 6.29 | 6.67 | Hossain et al. (2010) | |
| B−R13/17KH2 (AT-001) | PA | 5.03 | 5.66 | Silvertown et al. (2007), Neschadim et al. (2014) | |
| B−R13/17KH2 | PA | 7.59 | 8.41 (7.97 ant) | Siwek et al., unpublished | |
| A(4–24)(F23A)H2 | AG | 9.17 | 9.82 | Chan et al. (2012) | |
| Minimized relaxin-3 analog 2 | AG | <5 | N.A. | Shabanpoor et al. (2012) | |
| Minimized relaxin-3 analog 3 | <5 | N.D. | Shabanpoor et al. (2012) | ||
| ML290 | AA | N.A. | 7.03 | N.A. | Xiao et al. (2013) |
AA, allosteric agonist; AG, agonist; BA, biased agonist; N.A., no activity; N.D., not determined; PA, partial agonist.