Target family: Relaxin family peptide receptors (type: gpcr)
Target: RXFP2

Ligand: A(10-24)INSL3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.670000076293945 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: A(4-24)(B7-24)H2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pEC50
Reference (Journal): The minimal active structure of human relaxin-2.
Published in: J Biol Chem

Ligand: A(4-24)(B7-24)H2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 pKi
Reference (Journal): The minimal active structure of human relaxin-2.
Published in: J Biol Chem

Ligand: A(9-26)INSL3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.140000343322754 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: A(C10/15S)INSL3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.59000015258789 pKi
Reference (Journal): Role of the intra-A-chain disulfide bond of insulin-like peptide 3 in binding and activation of its receptor, RXFP2.
Published in: Peptides

Ligand: A(Δ10/15C)INSL3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.319999694824219 pKi
Reference (Journal): Role of the intra-A-chain disulfide bond of insulin-like peptide 3 in binding and activation of its receptor, RXFP2.
Published in: Peptides

Ligand: compound 6641 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.420000076293945 pEC50
Reference (Journal): Discovery of small molecule agonists of the Relaxin Family Peptide Receptor 2.
Published in: Commun Biol

Ligand: cyclic INSL3 B-chain analogue 6 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.650000095367432 pKi
Reference (Journal): Design, synthesis and pharmacological evaluation of cyclic mimetics of the insulin-like peptide 3 (INSL3) B-chain.
Published in: J Pept Sci

Ligand: (des 1-8) A-chain INSL3 analogue (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): LGR8 signal activation by the relaxin-like factor.
Published in: J Biol Chem

Ligand: europium-labelled INSL3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9 pKd
Reference (Journal): Solid-phase synthesis of europium-labeled human INSL3 as a novel probe for the study of ligand-receptor interactions.
Published in: Bioconjug Chem

Ligand: INSL3 (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: INSL3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.350000381469727 pKd
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: INSL3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Multiple binding sites revealed by interaction of relaxin family peptides with native and chimeric relaxin family peptide receptors 1 and 2 (LGR7 and LGR8).
Published in: J Pharmacol Exp Ther

Ligand: INSL3 [A(5-26):B(7-27)] (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pKi
Reference (Journal): The structural determinants of insulin-like Peptide 3 activity.
Published in: Front Endocrinol (Lausanne)

Ligand: INSL3 [A(5-26):B(7-27)] (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10 pEC50
Reference (Journal): The structural determinants of insulin-like Peptide 3 activity.
Published in: Front Endocrinol (Lausanne)

Ligand: INSL3 B-chain analogue (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 pKi
Reference (Journal): Analogs of insulin-like peptide 3 (INSL3) B-chain are LGR8 antagonists in vitro and in vivo.
Published in: J Biol Chem

Ligand: INSL3 B chain dimer analogue 8 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKi
Reference (Journal): Design and development of analogues of dimers of insulin-like peptide 3 B-chain as high-affinity antagonists of the RXFP2 receptor.
Published in: Biopolymers

Ligand: NanoLuc-INSL3 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKd
Reference (Journal): A novel ultrasensitive bioluminescent receptor-binding assay of INSL3 through chemical conjugation with nanoluciferase.
Published in: Biochimie

Ligand: relaxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.130000114440918 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 (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 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Multiple binding sites revealed by interaction of relaxin family peptides with native and chimeric relaxin family peptide receptors 1 and 2 (LGR7 and LGR8).
Published in: J Pharmacol Exp Ther

Ligand: relaxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Multiple binding sites revealed by interaction of relaxin family peptides with native and chimeric relaxin family peptide receptors 1 and 2 (LGR7 and LGR8).
Published in: J Pharmacol Exp Ther

Ligand: relaxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Multiple binding sites revealed by interaction of relaxin family peptides with native and chimeric relaxin family peptide receptors 1 and 2 (LGR7 and LGR8).
Published in: J Pharmacol Exp Ther

Ligand: relaxin-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Relaxin-3: Improved Synthesis Strategy and Demonstration of Its High-Affinity Interaction with the Relaxin Receptor LGR7 Both In Vitro and In Vivo.
Published in: Biochemistry

Ligand: relaxin-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Relaxin-3: Improved Synthesis Strategy and Demonstration of Its High-Affinity Interaction with the Relaxin Receptor LGR7 Both In Vitro and In Vivo.
Published in: Biochemistry

Ligand: RLF-(A11-B10)-isopeptide amideA26 (xA11-B10) (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Replacement of disulfides by amide bonds in the relaxin-like factor (RLF/INSL3) reveals a role for the A11-B10 link in transmembrane signaling.
Published in: Biochemistry

Ligand: [125I]INSL3 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pKd
Reference (Journal): Splice variants of the relaxin and INSL3 receptors reveal unanticipated molecular complexity.
Published in: Mol Hum Reprod

Ligand: [125I]INSL3 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 10 pKd
Reference (Journal): Splice variants of the relaxin and INSL3 receptors reveal unanticipated molecular complexity.
Published in: Mol Hum Reprod