Target family: Bombesin receptors (type: gpcr)
Target: BB<sub>3</sub> receptor

Ligand: [3H]bag-2 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.59000015258789 pKd
Reference (Journal): Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Published in: Cell Metab

Ligand: [125I][D-Tyr6,β-Ala11,Phe13,Nle14]bombesin-(6-14) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Discovery of a high affinity radioligand for the human orphan receptor, bombesin receptor subtype 3, which demonstrates that it has a unique pharmacology compared with other mammalian bombesin receptors.
Published in: J Biol Chem

Ligand: [125I][D-Tyr6,β-Ala11,Phe13,Nle14]bombesin-(6-14) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Comparative Pharmacology of Bombesin Receptor Subtype-3, Nonpeptide Agonist MK-5046, a Universal Peptide Agonist, and Peptide Antagonist Bantag-1 for Human Bombesin Receptors.
Published in: Pharmacol Exp Therap

Ligand: [125I]bantag-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.579999923706055 pKi
Reference (Journal): Development and Characterization of a Novel, High-Affinity, Specific, Radiolabeled Ligand for BRS-3 Receptors.
Published in: J Pharmacol Exp Ther

Ligand: phenylacetyl-Ala,DTrp-phenthylamide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.96 pEC50
Reference (Journal): Pharmacological characterization of a selective agonist for bombesin receptor subtype-3.
Published in: Biochem Biophys Res Commun

Ligand: phenylacetyl-Ala,DTrp-phenthylamide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacological characterization of a selective agonist for bombesin receptor subtype-3.
Published in: Biochem Biophys Res Commun

Ligand: phenylacetyl-Ala,DTrp-phenthylamide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.48 pEC50
Reference (Journal): Pharmacological characterization of a selective agonist for bombesin receptor subtype-3.
Published in: Biochem Biophys Res Commun

Ligand: phenylacetyl-Ala,DTrp-phenthylamide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Systematic optimization of a lead-structure identities for a selective short peptide agonist for the human orphan receptor BRS-3.
Published in: J Pept Sci

Ligand: phenylacetyl-Ala,DTrp-phenthylamide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacology of putative selective hBRS-3 receptor agonists for human bombesin receptors (BnR): affinities, potencies and selectivity in multiple native and BnR transfected cells.
Published in: Peptides

Ligand: NMU (104-114) (Peptide)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.659999847412109 pEC50
Reference (Journal): Discovery of Human Signaling Systems: Pairing Peptides to G Protein-Coupled Receptors.
Published in: Cell

Ligand: ML-18 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.320000171661377 pIC50
Reference (Journal): ML-18 is a non-peptide bombesin receptor subtype-3 antagonist which inhibits lung cancer growth.
Published in: Peptides

Ligand: MK-7725 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.520000457763672 pIC50
Reference (Journal): Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Published in: ACS Med Chem Lett

Ligand: MK-5046 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Comparative Pharmacology of Bombesin Receptor Subtype-3, Nonpeptide Agonist MK-5046, a Universal Peptide Agonist, and Peptide Antagonist Bantag-1 for Human Bombesin Receptors.
Published in: Pharmacol Exp Therap

Ligand: MK-5046 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparative Pharmacology of Bombesin Receptor Subtype-3, Nonpeptide Agonist MK-5046, a Universal Peptide Agonist, and Peptide Antagonist Bantag-1 for Human Bombesin Receptors.
Published in: Pharmacol Exp Therap

Ligand: MK-5046 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.6 pEC50
Reference (Journal): Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Published in: ACS Med Chem Lett

Ligand: MK-5046 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Published in: ACS Med Chem Lett

Ligand: MK-5046 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.8 pKi
Reference (Journal): Antiobesity effect of MK-5046, a novel bombesin receptor subtype-3 agonist.
Published in: J Pharmacol Exp Ther

Ligand: MK-5046 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Published in: ACS Med Chem Lett

Ligand: [D-Tyr6,(R)-APA11,Phe13,Nle14]bombesin-(6-14) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Molecular basis for agonist selectivity and activation of the orphan bombesin receptor subtype 3 receptor.
Published in: J Pharmacol Exp Ther

Ligand: [D-Tyr6,(R)-APA11,Phe13,Nle14]bombesin-(6-14) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacology of putative selective hBRS-3 receptor agonists for human bombesin receptors (BnR): affinities, potencies and selectivity in multiple native and BnR transfected cells.
Published in: Peptides

Ligand: [D-Tyr6,(R)-APA11,Phe13,Nle14]bombesin-(6-14) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.39 pKi
Reference (Journal): Rational design of a peptide agonist that interacts selectively with the orphan receptor, bombesin receptor subtype 3.
Published in: J Biol Chem

Ligand: [D-Tyr6,Apa-4Cl11,Phe13,Nle14]bombesin-(6-14) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): Development of bombesin analogs with conformationally restricted amino acid substitutions with enhanced selectivity for the orphan receptor human bombesin receptor subtype 3.
Published in: J Pharmacol Exp Ther

Ligand: [D-Tyr6,Apa-4Cl11,Phe13,Nle14]bombesin-(6-14) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Molecular basis for agonist selectivity and activation of the orphan bombesin receptor subtype 3 receptor.
Published in: J Pharmacol Exp Ther

Ligand: [D-Tyr6,Apa-4Cl11,Phe13,Nle14]bombesin-(6-14) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacology of putative selective hBRS-3 receptor agonists for human bombesin receptors (BnR): affinities, potencies and selectivity in multiple native and BnR transfected cells.
Published in: Peptides

Ligand: [D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.82 pKi
Reference (Journal): Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368.
Published in: J Pharmacol Exp Ther

Ligand: [D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368.
Published in: J Pharmacol Exp Ther

Ligand: [D-Phe6,β-Ala11,Phe13,Nle14]bombesin-(6-14) (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Discovery of a high affinity radioligand for the human orphan receptor, bombesin receptor subtype 3, which demonstrates that it has a unique pharmacology compared with other mammalian bombesin receptors.
Published in: J Biol Chem

Ligand: D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pIC50
Reference (Journal): Discovery of a high affinity radioligand for the human orphan receptor, bombesin receptor subtype 3, which demonstrates that it has a unique pharmacology compared with other mammalian bombesin receptors.
Published in: J Biol Chem

Ligand: D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pIC50
Reference (Journal): Ability of various bombesin receptor agonists and antagonists to alter intracellular signaling of the human orphan receptor BRS-3.
Published in: J Biol Chem

Ligand: D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pIC50
Reference (Journal): Pharmacology and intracellular signaling mechanisms of the native human orphan receptor BRS-3 in lung cancer cells.
Published in: J Pharmacol Exp Ther

Ligand: compound A [PMID: 28324017] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7 pEC50
Reference (Journal): A Selective Bombesin Receptor Subtype 3 Agonist Promotes Weight Loss in Male Diet-Induced-Obese Rats With Circadian Rhythm Change.
Published in: Endocrinology

Ligand: compound A [PMID: 28324017] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pEC50
Reference (Journal): A Selective Bombesin Receptor Subtype 3 Agonist Promotes Weight Loss in Male Diet-Induced-Obese Rats With Circadian Rhythm Change.
Published in: Endocrinology

Ligand: compound 9g [PMID: 24412111] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.770000457763672 pEC50
Reference (Journal): The Nonpeptide Agonist MK-5046 Functions As an Allosteric Agonist for the Bombesin Receptor Subtype-3.
Published in: J Pharmacol Exp Ther

Ligand: compound 9g [PMID: 24412111] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.770000457763672 pEC50
Reference (Journal): Discovery of novel chiral diazepines as bombesin receptor subtype-3 (BRS-3) agonists with low brain penetration.
Published in: Bioorg Med Chem Lett

Ligand: compound 9g [PMID: 24412111] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.770000457763672 pEC50
Reference (Journal): Novel chiral-diazepines function as specific, selective receptor agonists with variable coupling and species variability in human, mouse and rat BRS-3 receptor cells.
Published in: Peptides

Ligand: compound 9f [PMID: 24412111] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.769999980926514 pEC50
Reference (Journal): Discovery of novel chiral diazepines as bombesin receptor subtype-3 (BRS-3) agonists with low brain penetration.
Published in: Bioorg Med Chem Lett

Ligand: compound 8a [PMID: 24900283] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.850000381469727 pIC50
Reference (Journal): Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality.
Published in: ACS Med Chem Lett

Ligand: compound 22e [PMID: 20167483] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.599999904632568 pIC50
Reference (Journal): Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.
Published in: Bioorg Med Chem Lett

Ligand: compound 21b [PMID: 12723954] (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Design of selective peptidomimetic agonists for the human orphan receptor BRS-3.
Published in: J Med Chem

Ligand: compound 17c [PMID: 25497965] (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity: 7.920000076293945 pEC50
Reference (Journal): Synthesis and biological evaluation of novel chiral diazepine derivatives as bombesin receptor subtype-3 (BRS-3) agonists incorporating an antedrug approach.
Published in: Bioorg Med Chem

Ligand: bantag-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Comparative Pharmacology of Bombesin Receptor Subtype-3, Nonpeptide Agonist MK-5046, a Universal Peptide Agonist, and Peptide Antagonist Bantag-1 for Human Bombesin Receptors.
Published in: Pharmacol Exp Therap

Ligand: bantag-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Development and Characterization of a Novel, High-Affinity, Specific, Radiolabeled Ligand for BRS-3 Receptors.
Published in: J Pharmacol Exp Ther

Ligand: bantag-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.09 pIC50
Reference (Journal): Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Published in: Cell Metab

Ligand: bantag-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.77 pIC50
Reference (Journal): Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Published in: Cell Metab

Ligand: bantag-1 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pIC50
Reference (Journal): Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Published in: Cell Metab

Ligand: bag-2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.18 pIC50
Reference (Journal): Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Published in: Cell Metab

Ligand: bag-2 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.99 pIC50
Reference (Journal): Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Published in: Cell Metab

Ligand: bag-2 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.019999980926514 pIC50
Reference (Journal): Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Published in: Cell Metab

Ligand: bag-1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.62 pIC50
Reference (Journal): Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Published in: Cell Metab

Ligand: bag-1 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.16 pIC50
Reference (Journal): Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Published in: Cell Metab

Ligand: bag-1 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 7.739999771118164 pIC50
Reference (Journal): Regulation of energy homeostasis by bombesin receptor subtype-3: selective receptor agonists for the treatment of obesity.
Published in: Cell Metab

Ligand: Ac-Phe-Trp-Ala-His(τBZL)-Nip-Gly-Arg-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The design of a new potent and selective ligand for the orphan bombesin receptor subtype 3 (BRS3).
Published in: J Pept Sci

Ligand: Ac-Phe-Trp-Ala-His(τBZL)-Nip-Gly-Arg-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Pharmacology of putative selective hBRS-3 receptor agonists for human bombesin receptors (BnR): affinities, potencies and selectivity in multiple native and BnR transfected cells.
Published in: Peptides

Ligand: Ac-Phe-Trp-Ala-His(τBZL)-Nip-Gly-Arg-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Molecular basis for agonist selectivity and activation of the orphan bombesin receptor subtype 3 receptor.
Published in: J Pharmacol Exp Ther

Ligand: Ac-Phe-Trp-Ala-His(τBZL)-Nip-Gly-Arg-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Pharmacology of putative selective hBRS-3 receptor agonists for human bombesin receptors (BnR): affinities, potencies and selectivity in multiple native and BnR transfected cells.
Published in: Peptides

Ligand: Ac-Phe-Trp-Ala-His(τBZL)-Nip-Gly-Arg-NH2 (Peptide)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pIC50
Reference (Journal): Molecular basis for agonist selectivity and activation of the orphan bombesin receptor subtype 3 receptor.
Published in: J Pharmacol Exp Ther