Ligands acting at RXFP3
| Ligand | Binding Affinity pKi, pKD | cAMP pEC50 | GTPγS pEC50 | pERK 1/2 pEC50 | P38 MAPK pEC50 | Reference | |
|---|---|---|---|---|---|---|---|
| Relaxin-3 | AG | 8.48 | 8.26 | Hossain et al. (2008) | |||
| Relaxin-3 | AG | 7.78 | 9.0 | Shabanpoor et al. (2012) | |||
| Relaxin-3 | AG | 9.29 | 9.48 | Zhu et al. (2008) | |||
| Relaxin-3 | AG | 8.92 | 9.17 | 9.23 | van der Westhuizen et al. (2007) | ||
| Relaxin-3 | AG | 9.13 | 9.18 | van der Westhuizen et al. (2010) | |||
| Relaxin-3 | AG | 9.93 | 8.9 | Kocan et al. (2014) | |||
| R3/I5 | AG | 9.28 | 9.35 | Liu et al. (2005a) | |||
| R3/I5 | AG | 9.31 | 9.33 | Kuei et al. (2007) | |||
| Relaxin | BA | 10.0 | 7.05 | 7.99 | van der Westhuizen et al. (2010) | ||
| Relaxin | BA, PA | 7.15 | 8.35 | Kocan et al. (2014) | |||
| INSL5 | ANT | 7.01 | N.A. | Zhu et al. (2008) | |||
| Minimized relaxin-3 analog 2 | AG | 7.87 | 8.43 | 10.4 | Shabanpoor et al. (2012) | ||
| Minimized relaxin-3 analog 3 | ANT | 7.6 | N.A. | Shabanpoor et al. (2012) | |||
| Relaxin-3 B-chain dimer | AG | 6.61 | van der Westhuizen et al. (2007) | ||||
| R3(BΔ23–27)R/I5 | ANT | 8.49 | N.A.∼8 | Haugaard-Kedstrom et al. (2011) | |||
| R3(BΔ23–27)R/I5 | ANT | 9.17 | N.A. | Kuei et al. (2007) | |||
| R3(BΔ23–27)R/I5 | ANT, PA, BA | 8.87 | 9.02 | Kocan et al. (2014) | |||
| R3 B1–22R | ANT | 7.44 | N.A. | Haugaard-Kedstrom et al. (2011) | |||
| 135PAM1 | PAM | 6.12 | Alvarez-Jaimes et al. (2012) | ||||
| Relaxin-3 B-chain | AG | 7.06 | ∼7.0 | Liu et al. (2003b) | |||
| Liu et al. (2005a) |
AA, allosteric agonist; AG, agonist; ANT, antagonist; BA, biased agonist; N.A., no activity; PA, partial agonist .