Target family: Relaxin family peptide receptors (type: gpcr)
Target: RXFP3

Ligand: 135PAM1 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.119999885559082 pEC50
Reference (Journal): In vitro pharmacological characterization of RXFP3 allosterism: an example of probe dependency.
Published in: PLoS ONE

Ligand: B1-27 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.909999847412109 pKi
Reference (Journal): Development of Relaxin-3 Agonists and Antagonists Based on Grafted Disulfide-Stabilized Scaffolds.
Published in: Front Chem

Ligand: compound 10d [PMID: 34855388] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.159999847412109 pKi
Reference (Journal): Indole-Containing Amidinohydrazones as Nonpeptide, Dual RXFP3/4 Agonists: Synthesis, Structure-Activity Relationship, and Molecular Modeling Studies.
Published in: J Med Chem

Ligand: compound 10d [PMID: 34855388] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.510000228881836 pEC50
Reference (Journal): Indole-Containing Amidinohydrazones as Nonpeptide, Dual RXFP3/4 Agonists: Synthesis, Structure-Activity Relationship, and Molecular Modeling Studies.
Published in: J Med Chem

Ligand: compound 4 [PMID: 30824200] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.889999866485596 pEC50
Reference (Journal): Discovery of a small molecule RXFP3/4 agonist that increases food intake in rats upon acute central administration.
Published in: Bioorg Med Chem Lett

Ligand: DOTA/Eu relaxin-3 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKd
Reference (Journal): Site-specific DOTA/europium-labeling of recombinant human relaxin-3 for receptor-ligand interaction studies.
Published in: Amino Acids

Ligand: europium-labelled R3(B1-22R) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.550000190734863 pKd
Reference (Journal): Synthesis and pharmacological characterization of a europium-labelled single-chain antagonist for binding studies of the relaxin-3 receptor RXFP3.
Published in: Amino Acids

Ligand: europium-labelled relaxin-3-B/INSL5 A chimera (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKd
Reference (Journal): Minimization of human relaxin-3 leading to high-affinity analogues with increased selectivity for relaxin-family peptide 3 receptor (RXFP3) over RXFP1.
Published in: J Med Chem

Ligand: europium-labelled relaxin-3-B/INSL5 A chimera (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKd
Reference (Journal): Design, synthesis, and characterization of a single-chain peptide antagonist for the relaxin-3 receptor RXFP3.
Published in: J Am Chem Soc

Ligand: europium-labelled relaxin-3-B/INSL5 A chimera (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKd
Reference (Journal): Design, synthesis, and characterization of a single-chain peptide antagonist for the relaxin-3 receptor RXFP3.
Published in: J Am Chem Soc

Ligand: [G(B24)S]R3/I5 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.100000381469727 pIC50
Reference (Journal): Development of a selective agonist for relaxin family peptide receptor 3.
Published in: Sci Rep

Ligand: H3 14s18 stapled B-chain (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Intranasal administration of a stapled relaxin-3 mimetic has anxiolytic- and antidepressant-like activity in rats.
Published in: Br J Pharmacol

Ligand: H3 14s18 stapled B-chain (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pIC50
Reference (Journal): Hydrocarbon stapled B chain analogues of relaxin-3 retain biological activity.
Published in: Peptides

Ligand: H3 Ac-B10-27(13-17 HC) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pIC50
Reference (Journal): Development of a Single-Chain Peptide Agonist of the Relaxin-3 Receptor Using Hydrocarbon Stapling.
Published in: J Med Chem

Ligand: INSL5 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.010000228881836 pKi
Reference (Journal): Identification of the domains in RXFP4 (GPCR142) responsible for the high affinity binding and agonistic activity of INSL5 at RXFP4 compared to RXFP3 (GPCR135).
Published in: Eur J Pharmacol

Ligand: minimised relaxin-3 analogue 2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Minimization of human relaxin-3 leading to high-affinity analogues with increased selectivity for relaxin-family peptide 3 receptor (RXFP3) over RXFP1.
Published in: J Med Chem

Ligand: minimised relaxin-3 analogue 2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.869999885559082 pKi
Reference (Journal): Minimization of human relaxin-3 leading to high-affinity analogues with increased selectivity for relaxin-family peptide 3 receptor (RXFP3) over RXFP1.
Published in: J Med Chem

Ligand: minimised relaxin-3 analogue 2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.869999885559082 pKi
Reference (Journal): Differential effects of relaxin-3 and a selective relaxin-3 receptor agonist on food and water intake and hypothalamic neuronal activity in rats.
Published in: Behav Brain Res

Ligand: minimised relaxin-3 analogue 3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.599999904632568 pKi
Reference (Journal): Minimization of human relaxin-3 leading to high-affinity analogues with increased selectivity for relaxin-family peptide 3 receptor (RXFP3) over RXFP1.
Published in: J Med Chem

Ligand: NanoLuc R3/I5 chimera (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Exploring receptor selectivity of the chimeric relaxin family peptide R3/I5 by incorporating unnatural amino acids.
Published in: Biochimie

Ligand: NanoLuc R3/I5 chimera (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Rapid preparation of bioluminescent tracers for relaxin family peptides using sortase-catalysed ligation.
Published in: Amino Acids

Ligand: R3 B1-22R (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.440000057220459 pKi
Reference (Journal): Design, synthesis, and characterization of a single-chain peptide antagonist for the relaxin-3 receptor RXFP3.
Published in: J Am Chem Soc

Ligand: R3 B1-22R (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.690000057220459 pKi
Reference (Journal): Synthesis and pharmacological characterization of a europium-labelled single-chain antagonist for binding studies of the relaxin-3 receptor RXFP3.
Published in: Amino Acids

Ligand: R3(BΔ23-27)R/I5 chimeric peptide (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 10.100000381469727 pIC50
Reference (Journal): Partial agonist activity of R3(BΔ23-27)R/I5 at RXFP3--investigation of in vivo and in vitro pharmacology.
Published in: Eur J Pharmacol

Ligand: R3(BΔ23-27)R/I5 chimeric peptide (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pIC50
Reference (Journal): Partial agonist activity of R3(BΔ23-27)R/I5 at RXFP3--investigation of in vivo and in vitro pharmacology.
Published in: Eur J Pharmacol

Ligand: R3(BΔ23-27)R/I5 chimeric peptide (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Partial agonist activity of R3(BΔ23-27)R/I5 at RXFP3--investigation of in vivo and in vitro pharmacology.
Published in: Eur J Pharmacol

Ligand: R3(BΔ23-27)R/I5 chimeric peptide (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.489999771118164 pKi
Reference (Journal): Design, synthesis, and characterization of a single-chain peptide antagonist for the relaxin-3 receptor RXFP3.
Published in: J Am Chem Soc

Ligand: R3(BΔ23-27)R/I5 chimeric peptide (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Signalling profiles of H3 relaxin, H2 relaxin and R3(BΔ23-27)R/I5 acting at the relaxin family peptide receptor 3 (RXFP3).
Published in: Br J Pharmacol

Ligand: R3(BΔ23-27)R/I5 chimeric peptide (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pIC50
Reference (Journal): Partial agonist activity of R3(BΔ23-27)R/I5 at RXFP3--investigation of in vivo and in vitro pharmacology.
Published in: Eur J Pharmacol

Ligand: R3(BΔ23-27)R/I5 chimeric peptide (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pIC50
Reference (Journal): R3(BDelta23 27)R/I5 chimeric peptide, a selective antagonist for GPCR135 and GPCR142 over relaxin receptor LGR7: in vitro and in vivo characterization.
Published in: J Biol Chem

Ligand: R3/I5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Modulation of feeding by chronic rAAV expression of a relaxin-3 peptide agonist in rat hypothalamus.
Published in: Gene Ther

Ligand: R3/I5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pIC50
Reference (Journal): Relaxin-3/insulin-like peptide 5 chimeric peptide, a selective ligand for G protein-coupled receptor (GPCR)135 and GPCR142 over leucine-rich repeat-containing G protein-coupled receptor 7.
Published in: Mol Pharmacol

Ligand: R3/I5- SmBiT (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.199999809265137 pKd
Reference (Journal): Development of a novel ligand binding assay for relaxin family peptide receptor 3 and 4 using NanoLuc complementation.
Published in: Amino Acids

Ligand: relaxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10 pKd
Reference (Journal): H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3).
Published in: Mol Pharmacol

Ligand: relaxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3).
Published in: Mol Pharmacol

Ligand: relaxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Signalling profiles of H3 relaxin, H2 relaxin and R3(BΔ23-27)R/I5 acting at the relaxin family peptide receptor 3 (RXFP3).
Published in: Br J Pharmacol

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Signalling profiles of H3 relaxin, H2 relaxin and R3(BΔ23-27)R/I5 acting at the relaxin family peptide receptor 3 (RXFP3).
Published in: Br J Pharmacol

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The A-chain of human relaxin family peptides has distinct roles in the binding and activation of the different relaxin family peptide receptors.
Published in: J Biol Chem

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacological characterization of relaxin-3/INSL7 receptors GPCR135 and GPCR142 from different mammalian species.
Published in: J Pharmacol Exp Ther

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The A-chain of human relaxin family peptides has distinct roles in the binding and activation of the different relaxin family peptide receptors.
Published in: J Biol Chem

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8 pIC50
Reference (Journal): Chemical synthesis and orexigenic activity of rat/mouse relaxin-3.
Published in: Amino Acids

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Identification of relaxin-3/INSL7 as an endogenous ligand for the orphan G-protein-coupled receptor GPCR135.
Published in: J Biol Chem

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Minimization of human relaxin-3 leading to high-affinity analogues with increased selectivity for relaxin-family peptide 3 receptor (RXFP3) over RXFP1.
Published in: J Med Chem

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Minimization of human relaxin-3 leading to high-affinity analogues with increased selectivity for relaxin-family peptide 3 receptor (RXFP3) over RXFP1.
Published in: J Med Chem

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): H2 relaxin is a biased ligand relative to H3 relaxin at the relaxin family peptide receptor 3 (RXFP3).
Published in: Mol Pharmacol

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanism.
Published in: Mol Pharmacol

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanism.
Published in: Mol Pharmacol

Ligand: relaxin-3 (B chain) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.9 pIC50
Reference (Journal): Identification of relaxin-3/INSL7 as an endogenous ligand for the orphan G-protein-coupled receptor GPCR135.
Published in: J Biol Chem

Ligand: relaxin-3 B chain dimer (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.610000133514404 pKi
Reference (Journal): The relaxin family peptide receptor 3 activates extracellular signal-regulated kinase 1/2 through a protein kinase C-dependent mechanism.
Published in: Mol Pharmacol

Ligand: RLX-33 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.630000114440918 pIC50
Reference (Journal): Discovery and Characterization of the First Nonpeptide Antagonists for the Relaxin-3/RXFP3 System.
Published in: J Med Chem

Ligand: [125I]relaxin-3-B/INSL5 A chimera (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 9.3 pKd
Reference (Journal): Relaxin-3/insulin-like peptide 5 chimeric peptide, a selective ligand for G protein-coupled receptor (GPCR)135 and GPCR142 over leucine-rich repeat-containing G protein-coupled receptor 7.
Published in: Mol Pharmacol

Ligand: [125I]relaxin-3 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pKd
Reference (Journal): Identification of relaxin-3/INSL7 as an endogenous ligand for the orphan G-protein-coupled receptor GPCR135.
Published in: J Biol Chem

Ligand: [125I]relaxin-3 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.5 pKd
Reference (Journal): Identification of relaxin-3/INSL7 as an endogenous ligand for the orphan G-protein-coupled receptor GPCR135.
Published in: J Biol Chem

Ligand: WNN0109-C011 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.599999904632568 pEC50
Reference (Journal): High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist.
Published in: Molecules