Target family: Relaxin family peptide receptors (type: gpcr)
Target: RXFP4

Ligand: analogue 13: B7-24 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.100000381469727 pIC50
Reference (Journal): Human Insulin-like Peptide 5 (INSL5). Identification of a Simplified Version of Two-Chain Analog A13.
Published in: ACS Med Chem Lett

Ligand: compound 10d [PMID: 34855388] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.569999694824219 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: 8.800000190734863 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: compound 7a [PMID: 33730669] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.300000190734863 pEC50
Reference (Journal): Design, synthesis and pharmacological evaluation of tricyclic derivatives as selective RXFP4 agonists.
Published in: Bioorg Chem

Ligand: DC591053 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.949999809265137 pKi
Reference (Journal): Ligand recognition mechanism of the human relaxin family peptide receptor 4 (RXFP4).
Published in: Nat Commun

Ligand: ΔR3/I5 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKi
Reference (Journal): Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4.
Published in: Sci Rep

Ligand: europium-labelled INSL5 (Peptide)
Interaction type: None
Action: None
Ligand approved: no
Median affinity: 8.3 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 mouse INSL5 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.300000190734863 pKd
Reference (Journal): Structure and function relationship of murine insulin-like peptide 5 (INSL5): free C-terminus is essential for RXFP4 receptor binding and activation.
Published in: Biochemistry

Ligand: europium-labelled mouse INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKd
Reference (Journal): Minimum active structure of insulin-like peptide 5.
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: hINSL5: A8-21 (T15K) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.53000020980835 pKi
Reference (Journal): Engineering of a Novel Simplified Human Insulin-Like Peptide 5 Agonist.
Published in: J Med Chem

Ligand: hINSL5: A8-21 (T9R) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKi
Reference (Journal): Engineering of a Novel Simplified Human Insulin-Like Peptide 5 Agonist.
Published in: J Med Chem

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Signal transduction pathways activated by insulin-like peptide 5 at the relaxin family peptide RXFP4 receptor.
Published in: Br J Pharmacol

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
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: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The actions of relaxin family peptides on signal transduction pathways activated by the relaxin family peptide receptor RXFP4.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): A structural, theoretical and coordinative evaluation of the bicyclic guanidinate derived from 1,4,6-triazabicyclo[3.3.0]oct-4-ene.
Published in: Dalton Trans

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): INSL5 is a high affinity specific agonist for GPCR142 (GPR100).
Published in: J Biol Chem

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The actions of relaxin family peptides on signal transduction pathways activated by the relaxin family peptide receptor RXFP4.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Engineering of a Novel Simplified Human Insulin-Like Peptide 5 Agonist.
Published in: J Med Chem

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): INSL5 is a high affinity specific agonist for GPCR142 (GPR100).
Published in: J Biol Chem

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Engineering of a Novel Simplified Human Insulin-Like Peptide 5 Agonist.
Published in: J Med Chem

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  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: INSL5 (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: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Engineering of a Novel Simplified Human Insulin-Like Peptide 5 Agonist.
Published in: J Med Chem

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): INSL5 is a high affinity specific agonist for GPCR142 (GPR100).
Published in: J Biol Chem

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Engineering of a Novel Simplified Human Insulin-Like Peptide 5 Agonist.
Published in: J Med Chem

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Signal transduction pathways activated by insulin-like peptide 5 at the relaxin family peptide RXFP4 receptor.
Published in: Br J Pharmacol

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Minimum active structure of insulin-like peptide 5.
Published in: J Med Chem

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): INSL5 activates multiple signalling pathways and regulates GLP-1 secretion in NCI-H716 cells.
Published in: J Mol Endocrinol

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Minimum active structure of insulin-like peptide 5.
Published in: J Med Chem

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): INSL5 activates multiple signalling pathways and regulates GLP-1 secretion in NCI-H716 cells.
Published in: J Mol Endocrinol

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Minimum active structure of insulin-like peptide 5.
Published in: J Med Chem

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4.
Published in: Sci Rep

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The C-terminus of the B-chain of human insulin-like peptide 5 is critical for cognate RXFP4 receptor activity.
Published in: Amino Acids

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The C-terminus of the B-chain of human insulin-like peptide 5 is critical for cognate RXFP4 receptor activity.
Published in: Amino Acids

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4.
Published in: Sci Rep

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Identification of important residues of insulin-like peptide 5 and its receptor RXFP4 for ligand-receptor interactions.
Published in: Arch Biochem Biophys

Ligand: INSL5 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Minimum active structure of insulin-like peptide 5.
Published in: J Med Chem

Ligand: INSL5-A13NR (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): A Novel Antagonist Peptide Reveals a Physiological Role of Insulin-Like Peptide 5 in Control of Colorectal Function.
Published in: ACS Pharmacol Transl Sci

Ligand: INSL5 amide (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The C-terminus of the B-chain of human insulin-like peptide 5 is critical for cognate RXFP4 receptor activity.
Published in: Amino Acids

Ligand: INSL5 amide (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.480000019073486 pIC50
Reference (Journal): Structure and function relationship of murine insulin-like peptide 5 (INSL5): free C-terminus is essential for RXFP4 receptor binding and activation.
Published in: Biochemistry

Ligand: INSL5 amide (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Structure and function relationship of murine insulin-like peptide 5 (INSL5): free C-terminus is essential for RXFP4 receptor binding and activation.
Published in: Biochemistry

Ligand: INSL5 amide (mouse) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.070000171661377 pKi
Reference (Journal): Structure and function relationship of murine insulin-like peptide 5 (INSL5): free C-terminus is essential for RXFP4 receptor binding and activation.
Published in: Biochemistry

Ligand: INSL5 amide (mouse) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.849999904632568 pIC50
Reference (Journal): Structure and function relationship of murine insulin-like peptide 5 (INSL5): free C-terminus is essential for RXFP4 receptor binding and activation.
Published in: Biochemistry

Ligand: INSL5 analogue 13 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKi
Reference (Journal): Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4.
Published in: Sci Rep

Ligand: INSL5 analogue 13 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4.
Published in: Sci Rep

Ligand: JK1 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.579999923706055 pEC50
Reference (Journal): High-throughput screening campaign identifies a small molecule agonist of the relaxin family peptide receptor 4.
Published in: Acta Pharmacol Sin

Ligand: minimised INSL5 analogue 7 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 6.28000020980835 pKi
Reference (Journal): Minimum active structure of insulin-like peptide 5.
Published in: J Med Chem

Ligand: minimised INSL5 analogue 7 (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7.400000095367432 pIC50
Reference (Journal): Minimum active structure of insulin-like peptide 5.
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: 7.699999809265137 pIC50
Reference (Journal): Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4.
Published in: Sci Rep

Ligand: minimised relaxin-3 analogue 2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pKi
Reference (Journal): Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4.
Published in: Sci Rep

Ligand: minimised relaxin-3 analogue 2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
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: 7.099999904632568 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 3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pIC50
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): Development of a novel ligand binding assay for relaxin family peptide receptor 3 and 4 using NanoLuc complementation.
Published in: Amino Acids

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: R3(BΔ23-27)R/I5 chimeric peptide (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
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:  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: 8.9399995803833 pEC50
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: 8.880000114440918 pKi
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: 8.880000114440918 pKi
Reference (Journal): Functionality of an absolutely conserved glycine residue in the chimeric relaxin family peptide R3/I5.
Published in: Amino Acids

Ligand: R3/I5 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.5 pIC50
Reference (Journal): Functionality of an absolutely conserved glycine residue in the chimeric relaxin family peptide R3/I5.
Published in: Amino Acids

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): Identification of relaxin-3/INSL7 as a ligand for GPCR142.
Published in: J Biol Chem

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  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: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
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: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): The actions of relaxin family peptides on signal transduction pathways activated by the relaxin family peptide receptor RXFP4.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The actions of relaxin family peptides on signal transduction pathways activated by the relaxin family peptide receptor RXFP4.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  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: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
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: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4.
Published in: Sci Rep

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKi
Reference (Journal): Engineering of chimeric peptides as antagonists for the G protein-coupled receptor, RXFP4.
Published in: Sci Rep

Ligand: relaxin-3 (B chain) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Identification of relaxin-3/INSL7 as a ligand for GPCR142.
Published in: J Biol Chem

Ligand: relaxin-3 (B chain) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): INSL5 is a high affinity specific agonist for GPCR142 (GPR100).
Published in: J Biol Chem

Ligand: relaxin-3 (B chain) (Peptide)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7 pEC50
Reference (Journal): Identification of relaxin-3/INSL7 as a ligand for GPCR142.
Published in: J Biol Chem

Ligand: [125I]INSL5 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKd
Reference (Journal): INSL5 is a high affinity specific agonist for GPCR142 (GPR100).
Published in: J Biol Chem

Ligand: [125I]relaxin-3-B/INSL5 A chimera (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.9 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:  pKd
Reference (Journal): Identification of relaxin-3/INSL7 as a ligand for GPCR142.
Published in: J Biol Chem

Ligand: WNN0109-C011 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 4.46999979019165 pEC50
Reference (Journal): High-Throughput Screening Campaign Identified a Potential Small Molecule RXFP3/4 Agonist.
Published in: Molecules

Ligand: hINSL5: A8-21 (T9R) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.699999809265137 pIC50
Reference (Journal): Engineering of a Novel Simplified Human Insulin-Like Peptide 5 Agonist.
Published in: J Med Chem