Target family: Adrenoceptors (type: gpcr)
Target: &beta;<sub>3</sub>-adrenoceptor

Ligand: abediterol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.519999980926514 pIC50
Reference (Journal): Pharmacological characterization of abediterol, a novel inhaled β(2)-adrenoceptor agonist with long duration of action and a favorable safety profile in preclinical models.
Published in: J Pharmacol Exp Ther

Ligand: (-)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1951)
Primary target: no
Median affinity: 6.5 pEC50
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: (-)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1951)
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: (-)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1951)
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: amibegron (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.2 pKi
Reference (Journal): Structural and conformational features determining selective signal transduction in the beta 3-adrenergic receptor.
Published in: Mol Pharmacol

Ligand: BRL 37344 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 6.5 pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: BRL 37344 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: BRL 37344 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pEC50
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: BRL 37344 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: BRL 37344 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Beta-3 adrenoceptor selectivity of the dioxolane dicarboxylate phenethanolamines.
Published in: J Pharmacol Exp Ther

Ligand: BRL 37344 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Structural and conformational features determining selective signal transduction in the beta 3-adrenergic receptor.
Published in: Mol Pharmacol

Ligand: BRL 37344 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: bunolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1985)
Primary target: no
Median affinity: 6.400000095367432 pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: bunolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1985)
Primary target: no
Median affinity:  pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: bunolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1985)
Primary target: yes
Median affinity: 6.800000190734863 pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: bupranolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Structural and conformational features determining selective signal transduction in the beta 3-adrenergic receptor.
Published in: Mol Pharmacol

Ligand: bupranolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: bupranolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): Potent and selective human beta(3)-adrenergic receptor antagonists.
Published in: J Pharmacol Exp Ther

Ligand: bupranolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity:  pKi
Reference (Journal): LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: carazolol (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: carazolol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Median affinity: 7.7 pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: carazolol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Median affinity: 7.7 pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: carazolol (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Primary target: no
Median affinity: 8.800000190734863 pEC50
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: carvedilol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
Published in: Br J Pharmacol

Ligand: carvedilol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1995)
Primary target: no
Median affinity:  pKi
Reference (Journal): Potent and selective human beta(3)-adrenergic receptor antagonists.
Published in: J Pharmacol Exp Ther

Ligand: CGP 12177 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: CGP 12177 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Effects of (-)-RO363 at human atrial beta-adrenoceptor subtypes, the human cloned beta 3-adrenoceptor and rodent intestinal beta 3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: CGP 12177 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Structural and conformational features determining selective signal transduction in the beta 3-adrenergic receptor.
Published in: Mol Pharmacol

Ligand: CGP 12177 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: CGP 12177 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 6.8 pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: CGP 12177 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: CGP 20712A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
Published in: Br J Pharmacol

Ligand: CGP 20712A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: CGP 20712A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Potent and selective human beta(3)-adrenergic receptor antagonists.
Published in: J Pharmacol Exp Ther

Ligand: CGP 20712A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: cimaterol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pKi
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: cimaterol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 7 pEC50
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: CL316243 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pKi
Reference (Journal): Selectivity and potency of agonists for the three subtypes of cloned human beta-adrenoceptors expressed in Chinese hamster ovary cells.
Published in: Tohoku J Exp Med

Ligand: CL316243 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Ligand-directed signaling at the beta3-adrenoceptor produced by 3-(2-Ethylphenoxy)-1-[(1,S)-1,2,3,4-tetrahydronapth-1-ylamino]-2S-2-propanol oxalate (SR59230A) relative to receptor agonists.
Published in: Mol Pharmacol

Ligand: CL316243 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Agonist effects of zinterol at the mouse and human beta(3)-adrenoceptor.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: CL316243 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pKi
Reference (Journal): Ligand-directed signaling at the beta3-adrenoceptor produced by 3-(2-Ethylphenoxy)-1-[(1,S)-1,2,3,4-tetrahydronapth-1-ylamino]-2S-2-propanol oxalate (SR59230A) relative to receptor agonists.
Published in: Mol Pharmacol

Ligand: fenoterol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity: 5.400000095367432 pKi
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: fenoterol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity: 7.599999904632568 pEC50
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: ICI 118551 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
Published in: Br J Pharmacol

Ligand: ICI 118551 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: ICI 118551 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: ICI 118551 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: isoprenaline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: isoprenaline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: isoprenaline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Median affinity: 5.3 pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: isoprenaline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: isoprenaline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity: 7.400000095367432 pEC50
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: isoprenaline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: isoprenaline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Structure and function of the beta 3-adrenergic receptor.
Published in: Annu Rev Pharmacol Toxicol

Ligand: isoprenaline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Median affinity:  pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: isoprenaline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Effects of (-)-RO363 at human atrial beta-adrenoceptor subtypes, the human cloned beta 3-adrenoceptor and rodent intestinal beta 3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: isoprenaline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: isoprenaline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Molecular characterization of pharmacological properties of T-0509 for beta-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: L742791 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 8.8 pEC50
Reference (Journal): 3-Pyridyloxypropanolamine agonists of the beta 3 adrenergic receptor with improved pharmacokinetic properties.
Published in: Bioorg Med Chem Lett

Ligand: L-748328 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Potent and selective human beta(3)-adrenergic receptor antagonists.
Published in: J Pharmacol Exp Ther

Ligand: L-748328 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: L-748337 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pEC50
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: L-748337 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: L-748337 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Potent and selective human beta(3)-adrenergic receptor antagonists.
Published in: J Pharmacol Exp Ther

Ligand: L-748337 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): The beta3-adrenoceptor agonist 4-[[(Hexylamino)carbonyl]amino]-N-[4-[2-[[(2S)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]-phenyl]-benzenesulfonamide (L755507) and antagonist (S)-N-[4-[2-[[3-[3-(acetamidomethyl)phenoxy]-2-hydroxypropyl]amino]-ethyl]phenyl]benzenesulfonamide (L748337) activate different signaling pathways in Chinese hamster ovary-K1 cells stably expressing the human beta3-adrenoceptor.
Published in: Mol Pharmacol

Ligand: L 755507 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 10.100000381469727 pEC50
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: mirabegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: yes
Median affinity:  pEC50
Reference (Journal): Effect of (R)-2-(2-aminothiazol-4-yl)-4'-{2-[(2-hydroxy-2-phenylethyl)amino]ethyl} acetanilide (YM178), a novel selective beta3-adrenoceptor agonist, on bladder function.
Published in: J Pharmacol Exp Ther

Ligand: mirabegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: no
Median affinity:  pEC50
Reference (Journal): The metabolic effects of mirabegron are mediated primarily by &#x3b2;<sub>3</sub> -adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: mirabegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: no
Median affinity:  pEC50
Reference (Journal): The metabolic effects of mirabegron are mediated primarily by &#x3b2;<sub>3</sub> -adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: mirabegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: no
Median affinity: 7.699999809265137 pEC50
Reference (Journal): The metabolic effects of mirabegron are mediated primarily by &#x3b2;<sub>3</sub> -adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: mirabegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: yes
Median affinity:  pEC50
Reference (Journal): In vitro and in vivo pharmacological profile of the selective &#x3b2;3-adrenoceptor agonist mirabegron in rats.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: mirabegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: yes
Median affinity:  pEC50
Reference (Journal): Selectivity and Maximum Response of Vibegron and Mirabegron for &#x3b2;<sub>3</sub>-Adrenergic Receptors.
Published in: Curr Ther Res Clin Exp

Ligand: mirabegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: yes
Median affinity:  pEC50
Reference (Journal): The metabolic effects of mirabegron are mediated primarily by &#x3b2;<sub>3</sub> -adrenoceptors.
Published in: Pharmacol Res Perspect

Ligand: nadolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1979)
Primary target: no
Median affinity:  pKi
Reference (Journal): Potent and selective human beta(3)-adrenergic receptor antagonists.
Published in: J Pharmacol Exp Ther

Ligand: nadolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1979)
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
Published in: Br J Pharmacol

Ligand: nebivolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2007)
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: nebivolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2007)
Primary target: no
Median affinity:  pKi
Reference (Journal): Lack of evidence that nebivolol is a β₃-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pKi
Reference (Journal): Structure and function of the beta 3-adrenergic receptor.
Published in: Annu Rev Pharmacol Toxicol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity: 7.199999809265137 pEC50
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Median affinity: 3.8 pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Median affinity: 4.2 pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: (-)-noradrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: no
Median affinity:  pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: pindolol (Synthetic organic)
Interaction type: Antagonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity: 7.099999904632568 pKi
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: pindolol (Synthetic organic)
Interaction type: Antagonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1982)
Primary target: no
Median affinity:  pEC50
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: (±)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: (±)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: (±)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): Carazolol: a potent, selective beta 3-adrenoceptor agonist.
Published in: Eur J Pharmacol

Ligand: (±)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Structural and conformational features determining selective signal transduction in the beta 3-adrenergic receptor.
Published in: Mol Pharmacol

Ligand: (±)-adrenaline (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: propranolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967), EMA (2014)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors.
Published in: Br J Pharmacol

Ligand: propranolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967), EMA (2014)
Primary target: yes
Median affinity:  pKi
Reference (Journal): LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: propranolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967), EMA (2014)
Primary target: no
Median affinity:  pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: propranolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967), EMA (2014)
Primary target: no
Median affinity: 6.400000095367432 pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: propranolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1967), EMA (2014)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: SB251023 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Median affinity: 7.14 pEC50
Reference (Journal): Mouse beta 3a- and beta 3b-adrenoceptors expressed in Chinese hamster ovary cells display identical pharmacology but utilize distinct signalling pathways.
Published in: Br J Pharmacol

Ligand: solabegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity:  pEC50
Reference (Journal): Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
Published in: J Med Chem

Ligand: solabegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity:  pEC50
Reference (Journal): β3-Adrenoceptor agonists for overactive bladder syndrome: Role of translational pharmacology in a repositioning clinical drug development project.
Published in: Pharmacol Ther

Ligand: solabegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: yes
Median affinity:  pEC50
Reference (Journal): Pharmacological profile of &#x3b2;3-adrenoceptor agonists in clinical development for the treatment of overactive bladder syndrome.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: SR59230A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: SR59230A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: SR59230A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Functional evidence of atypical beta 3-adrenoceptors in the human colon using the beta 3-selective adrenoceptor antagonist, SR 59230A.
Published in: Br J Pharmacol

Ligand: SR59230A (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Potent and selective human beta(3)-adrenergic receptor antagonists.
Published in: J Pharmacol Exp Ther

Ligand: [125I]ICYP (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Molecular characterization of pharmacological properties of T-0509 for beta-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: [125I]ICYP (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 9.2 pKd
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: [125I]ICYP (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Effects of (-)-RO363 at human atrial beta-adrenoceptor subtypes, the human cloned beta 3-adrenoceptor and rodent intestinal beta 3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: [125I]ICYP (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Structure and function of the beta 3-adrenergic receptor.
Published in: Annu Rev Pharmacol Toxicol

Ligand: [125I]ICYP (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: [125I]ICYP (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: [125I]ICYP (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): LK 204-545, a highly selective beta1-adrenoceptor antagonist at human beta-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: [3H]CGP12177 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 7 pKd
Reference (Journal): The selectivity of beta-adrenoceptor agonists at human beta1-, beta2- and beta3-adrenoceptors.
Published in: Br J Pharmacol

Ligand: [3H]L748337 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): The new radioligand [(3)H]-L 748,337 differentially labels human and rat β3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: tertatolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: tertatolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7 pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: tertatolol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Stereoselectivity for interactions of agonists and antagonists at mouse, rat and human beta3-adrenoceptors.
Published in: Eur J Pharmacol

Ligand: vibegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2020)
Primary target: yes
Median affinity:  pEC50
Reference (Journal): Selectivity and Maximum Response of Vibegron and Mirabegron for &#x3b2;<sub>3</sub>-Adrenergic Receptors.
Published in: Curr Ther Res Clin Exp

Ligand: vibegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2020)
Primary target: yes
Median affinity:  pEC50
Reference (Journal): Pharmacological Characterization of a Novel Beta 3 Adrenergic Agonist, Vibegron: Evaluation of Antimuscarinic Receptor Selectivity for Combination Therapy for Overactive Bladder.
Published in: J Pharmacol Exp Ther

Ligand: vibegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2020)
Primary target: no
Median affinity: 9.239999771118164 pEC50
Reference (Journal): Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Published in: J Med Chem

Ligand: vibegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2020)
Primary target: yes
Median affinity:  pEC50
Reference (Journal): Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Published in: J Med Chem

Ligand: vibegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2020)
Primary target: no
Median affinity: 7.960000038146973 pEC50
Reference (Journal): Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Published in: J Med Chem

Ligand: vibegron (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2020)
Primary target: no
Median affinity: 7.070000171661377 pEC50
Reference (Journal): Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.
Published in: J Med Chem