Target family: Class A Orphans (type: gpcr)
Target: <i>MRGPRX2</i>

Ligand: TAN-67 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.739999771118164 pEC50
Reference (Journal): Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors.
Published in: J Biomol Screen

Ligand: TAN-67 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.739999771118164 pEC50
Reference (Journal): Synthesis of optically active TAN-67, a highly selective delta opioid receptor agonist, and investigation of its pharmacological properties.
Published in: Drug Des Discov

Ligand: TAN-67 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.739999771118164 pEC50
Reference (Journal): In silico design of novel probes for the atypical opioid receptor MRGPRX2.
Published in: Nat Chem Biol

Ligand: substance P (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.96999979019165 pEC50
Reference (Journal): In silico design of novel probes for the atypical opioid receptor MRGPRX2.
Published in: Nat Chem Biol

Ligand: substance P (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.96999979019165 pEC50
Reference (Journal): Identification of a mast-cell-specific receptor crucial for pseudo-allergic drug reactions.
Published in: Nature

Ligand: SRIF-28 (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.380000114440918 pEC50
Reference (Journal): Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors.
Published in: J Biomol Screen

Ligand: (R)-ZINC-3573 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 6.119999885559082 pEC50
Reference (Journal): In silico design of novel probes for the atypical opioid receptor MRGPRX2.
Published in: Nat Chem Biol

Ligand: QWF (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Dual action of neurokinin-1 antagonists on Mas-related GPCRs.
Published in: JCI Insight

Ligand: PAMP-20 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  -
Reference (Journal): Identification of MrgX2 as a human G-protein-coupled receptor for proadrenomedullin N-terminal peptides.
Published in: Biochem Biophys Res Commun

Ligand: PAMP-12 (human) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Identification of MrgX2 as a human G-protein-coupled receptor for proadrenomedullin N-terminal peptides.
Published in: Biochem Biophys Res Commun

Ligand: GPR15L (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.71999979019165 pEC50
Reference (Journal): GPR15L is an epithelial inflammation-derived pruritogen.
Published in: Sci Adv

Ligand: ERAS-5024 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.380000114440918 pEC50
Reference (Journal): The pharmacologic and toxicologic characterization of the potent and selective KRAS G12D inhibitors ERAS-4693 and ERAS-5024.
Published in: Toxicol Appl Pharmacol

Ligand: cortistatin-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Identification of MrgX2 as a human G-protein-coupled receptor for proadrenomedullin N-terminal peptides.
Published in: Biochem Biophys Res Commun

Ligand: cortistatin-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Screening β-Arrestin Recruitment for the Identification of Natural Ligands for Orphan G-Protein-Coupled Receptors.
Published in: J Biomol Screen

Ligand: cortistatin-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): MrgX2 is a high potency cortistatin receptor expressed in dorsal root ganglion.
Published in: J Biol Chem

Ligand: cortistatin-14 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): In silico design of novel probes for the atypical opioid receptor MRGPRX2.
Published in: Nat Chem Biol

Ligand: compound 48/80 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.739999771118164 pEC50
Reference (Journal): In silico design of novel probes for the atypical opioid receptor MRGPRX2.
Published in: Nat Chem Biol

Ligand: compound 2 [PMID: 19230660] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 pEC50
Reference (Journal): Discovery of non-peptidergic MrgX1 and MrgX2 receptor agonists and exploration of an initial SAR using solid-phase synthesis.
Published in: Bioorg Med Chem Lett