Target family: Relaxin family peptide receptors (type: gpcr)
Target: RXFP1

Ligand: A(4-24)(B7-24)H2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.220000267028809 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: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.989999771118164 pKd
Reference (Journal): The minimal active structure of human relaxin-2.
Published in: J Biol Chem

Ligand: A(4-24)(F23A)H2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.819999694824219 pEC50
Reference (Journal): Identification of key residues essential for the structural fold and receptor selectivity within the A-chain of human gene-2 (H2) relaxin.
Published in: J Biol Chem

Ligand: A(4-24)(F23A)H2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.170000076293945 pKi
Reference (Journal): Identification of key residues essential for the structural fold and receptor selectivity within the A-chain of human gene-2 (H2) relaxin.
Published in: J Biol Chem

Ligand: AZD5462 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pEC50
Reference (Journal): Discovery of Clinical Candidate AZD5462, a Selective Oral Allosteric RXFP1 Agonist for Treatment of Heart Failure.
Published in: J Med Chem

Ligand: AZD5462 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 5.309999942779541 pEC50
Reference (Journal): Discovery of Clinical Candidate AZD5462, a Selective Oral Allosteric RXFP1 Agonist for Treatment of Heart Failure.
Published in: J Med Chem

Ligand: AZD5462 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pEC50
Reference (Journal): Discovery of Clinical Candidate AZD5462, a Selective Oral Allosteric RXFP1 Agonist for Treatment of Heart Failure.
Published in: J Med Chem

Ligand: (B7-33)H2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.5 pKi
Reference (Journal): A single-chain derivative of the relaxin hormone is a functionally selective agonist of the G protein-coupled receptor, RXFP1.
Published in: Chem Sci

Ligand: (B7-33)H2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.5 pKi
Reference (Journal): B7-33, a Functionally Selective Relaxin Receptor 1 Agonist, Attenuates Myocardial Infarction-Related Adverse Cardiac Remodeling in Mice.
Published in: J Am Heart Assoc

Ligand: B-R13/17K H2 relaxin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Relaxin receptor antagonist AT-001 synergizes with docetaxel in androgen-independent prostate xenografts.
Published in: Endocr Relat Cancer

Ligand: B-R13/17K H2 relaxin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Relaxin receptor antagonist AT-001 synergizes with docetaxel in androgen-independent prostate xenografts.
Published in: Endocr Relat Cancer

Ligand: B-R13/17K H2 relaxin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): The chemically synthesized human relaxin-2 analog, B-R13/17K H2, is an RXFP1 antagonist.
Published in: Amino Acids

Ligand: B-R13/17K H2 relaxin (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The chemically synthesized human relaxin-2 analog, B-R13/17K H2, is an RXFP1 antagonist.
Published in: Amino Acids

Ligand: compound 54 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7.920000076293945 pEC50
Reference (Journal): Identification of Potent and Long-Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular Diseases.
Published in: J Med Chem

Ligand: europium-labelled relaxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKd
Reference (Journal): Solid phase synthesis and structural analysis of novel A-chain dicarba analogs of human relaxin-3 (INSL7) that exhibit full biological activity.
Published in: Org Biomol Chem

Ligand: europium-labelled relaxin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKd
Reference (Journal): Site-specific conjugation of a lanthanide chelator and its effects on the chemical synthesis and receptor binding affinity of human relaxin-2 hormone.
Published in: Biochem Biophys Res Commun

Ligand: INSL3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 pKi
Reference (Journal): Relaxin family peptides and their receptors.
Published in: Physiol Rev

Ligand: LY3540378 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKd
Reference (Journal): Development of a long-acting relaxin analogue, LY3540378, for treatment of chronic heart failure.
Published in: Br J Pharmacol

Ligand: LY3540378 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.09000015258789 pKd
Reference (Journal): Development of a long-acting relaxin analogue, LY3540378, for treatment of chronic heart failure.
Published in: Br J Pharmacol

Ligand: LY3540378 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.399999618530273 pKd
Reference (Journal): Development of a long-acting relaxin analogue, LY3540378, for treatment of chronic heart failure.
Published in: Br J Pharmacol

Ligand: ML290 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 7.03000020980835 pEC50
Reference (Journal): ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.
Published in: Sci Rep

Ligand: ML290 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 7.03000020980835 pEC50
Reference (Journal): Discovery, optimization, and biological activity of the first potent and selective small-molecule agonist series of human relaxin receptor 1 (RXFP1).
Published in: Probe Reports from the NIH Molecular Libraries Program

Ligand: ML290 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Biased agonist
Ligand approved: no
Primary target: no
Median affinity: 7.03000020980835 pEC50
Reference (Journal): Identification and optimization of small-molecule agonists of the human relaxin hormone receptor RXFP1.
Published in: Nat Commun

Ligand: Nanoluciferase-labelled relaxin (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Application of the novel bioluminescent ligand-receptor binding assay to relaxin-RXFP1 system for interaction studies.
Published in: Amino Acids

Ligand: relaxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.3 pKd
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): H3 relaxin is a specific ligand for LGR7 and activates the receptor by interacting with both the ectodomain and the exoloop 2.
Published in: J Biol Chem

Ligand: relaxin (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9.1 pKd
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: 9.4 pKd
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 (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
Primary target: no
Median affinity: 10.369999885559082 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-1 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pEC50
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:  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-3 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): H3 relaxin is a specific ligand for LGR7 and activates the receptor by interacting with both the ectodomain and the exoloop 2.
Published in: J Biol Chem

Ligand: SA10SC-RLX (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pEC50
Reference (Journal): Identification of Potent and Long-Acting Single-Chain Peptide Mimetics of Human Relaxin-2 for Cardiovascular Diseases.
Published in: J Med Chem

Ligand: SA10SC-RLX (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.699999809265137 pEC50
Reference (Journal): Characterization of a new potent and long-lasting single chain peptide agonist of RXFP1 in cells and in vivo translational models.
Published in: Sci Rep

Ligand: [125I]relaxin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -

Ligand: [33P]relaxin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
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: [33P]relaxin (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): H3 relaxin is a specific ligand for LGR7 and activates the receptor by interacting with both the ectodomain and the exoloop 2.
Published in: J Biol Chem

Ligand: TamRLX (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 9.0600004196167 pEC50
Reference (Journal): Multi-Component Mechanism of H2 Relaxin Binding to RXFP1 through NanoBRET Kinetic Analysis.
Published in: iScience