Target family: Acetylcholine receptors (muscarinic) (type: gpcr)
Target: M<sub>4</sub> receptor

Ligand: methacholine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity: 5.800000190734863 pKi
Reference (Journal): Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists.
Published in: Br J Pharmacol

Ligand: methacholine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity: 5.800000190734863 pKi
Reference (Journal): 6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
Published in: J Med Chem

Ligand: methylfurmethide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.7 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: methoctramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
Published in: Mol Pharmacol

Ligand: methoctramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Stimulation of cyclic AMP accumulation and phosphoinositide hydrolysis by M3 muscarinic receptors in the rat peripheral lung.
Published in: Biochem Pharmacol

Ligand: methoctramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo.
Published in: Br J Pharmacol

Ligand: methoctramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: milameline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.5 pKi
Reference (Journal): Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1, hM2, hM3, hM4 and hM5 using microphysiometry.
Published in: Br J Pharmacol

Ligand: ML381 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 4.519999980926514 pKi
Reference (Journal): Discovery, synthesis and characterization of a highly muscarinic acetylcholine receptor (mAChR)-selective M5-orthosteric antagonist, VU0488130 (ML381): a novel molecular probe.
Published in: ChemMedChem

Ligand: muscarinic toxin 1 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 pKi
Reference (Journal): Effects of muscarinic toxins MT1 and MT2 from green mamba on different muscarinic cholinoceptors.
Published in: Neurochem Res

Ligand: muscarinic toxin 2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.9 pKi
Reference (Journal): Effects of muscarinic toxins MT1 and MT2 from green mamba on different muscarinic cholinoceptors.
Published in: Neurochem Res

Ligand: muscarinic toxin 3 (Peptide)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): A toxin from the green mamba Dendroaspis angusticeps: amino acid sequence and selectivity for muscarinic m4 receptors.
Published in: FEBS Lett

Ligand: muscarinic toxin 3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.520000457763672 pKi
Reference (Journal): Myopia-Inhibiting Concentrations of Muscarinic Receptor Antagonists Block Activation of Alpha2A-Adrenoceptors In Vitro.
Published in: Invest Ophthalmol Vis Sci

Ligand: muscarinic toxin 3 (Peptide)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): Selectivity profile of muscarinic toxin 3 in functional assays of cloned and native receptors.
Published in: J Pharmacol Exp Ther

Ligand: muscarinic toxin 7 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 pKi
Reference (Journal): Recombinant expression of a selective blocker of M(1) muscarinic receptors.
Published in: Biochem Biophys Res Commun

Ligand: N-chloromethyl-brucine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Neutral
Ligand approved: no
Median affinity: 4.4 pKd
Reference (Journal): Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.
Published in: Mol Pharmacol

Ligand: NNC 11-1314 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.3 pKi
Reference (Journal): Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists.
Published in: J Pharmacol Exp Ther

Ligand: NNC 11-1585 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists.
Published in: J Pharmacol Exp Ther

Ligand: NNC 11-1607 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.1 pKi
Reference (Journal): Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists.
Published in: J Pharmacol Exp Ther

Ligand: otenzepad (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7 pKd
Reference (Journal): Stimulation of cyclic AMP accumulation and phosphoinositide hydrolysis by M3 muscarinic receptors in the rat peripheral lung.
Published in: Biochem Pharmacol

Ligand: otenzepad (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Cloning of the rat M3, M4 and M5 muscarinic acetylcholine receptor genes by the polymerase chain reaction (PCR) and the pharmacological characterization of the expressed genes.
Published in: Life Sci

Ligand: oxotremorine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pKi
Reference (Journal): Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists.
Published in: Br J Pharmacol

Ligand: oxotremorine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: oxotremorine-M (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.2 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: oxybutynin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2004)
Primary target: no
Median affinity:  pKi
Reference (Journal): 1,4-dioxane, a suitable scaffold for the development of novel M₃ muscarinic receptor antagonists.
Published in: J Med Chem

Ligand: oxybutynin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2004)
Primary target: no
Median affinity:  pKi
Reference (Journal): AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder.
Published in: Br J Pharmacol

Ligand: oxyphenonium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 9.84000015258789 pKi
Reference (Journal): Myopia-Inhibiting Concentrations of Muscarinic Receptor Antagonists Block Activation of Alpha2A-Adrenoceptors In Vitro.
Published in: Invest Ophthalmol Vis Sci

Ligand: PCS1055 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): Characterization of PCS1055, a novel muscarinic M4 receptor antagonist.
Published in: Eur J Pharmacol

Ligand: PD 102807 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterization of PCS1055, a novel muscarinic M4 receptor antagonist.
Published in: Eur J Pharmacol

Ligand: PD 102807 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): PD 102807, a novel muscarinic M4 receptor antagonist, discriminates between striatal and cortical muscarinic receptors coupled to cyclic AMP.
Published in: Life Sci

Ligand: pentylthio-TZTP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.7 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: pilocarpine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: no
Median affinity: 5.199999809265137 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: mepenzolic acid (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1956)
Primary target: no
Median affinity: 9.4399995803833 pKi
Reference (Journal): Myopia-Inhibiting Concentrations of Muscarinic Receptor Antagonists Block Activation of Alpha2A-Adrenoceptors In Vitro.
Published in: Invest Ophthalmol Vis Sci

Ligand: pilocarpine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: no
Median affinity: 5.199999809265137 pKi
Reference (Journal): Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists.
Published in: Br J Pharmacol

Ligand: pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 8.100000381469727 pKi
Reference (Journal): Myopia-Inhibiting Concentrations of Muscarinic Receptor Antagonists Block Activation of Alpha2A-Adrenoceptors In Vitro.
Published in: Invest Ophthalmol Vis Sci

Ligand: pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 7.1 pKi
Reference (Journal): Cloning of the rat M3, M4 and M5 muscarinic acetylcholine receptor genes by the polymerase chain reaction (PCR) and the pharmacological characterization of the expressed genes.
Published in: Life Sci

Ligand: pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo.
Published in: Br J Pharmacol

Ligand: pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): A toxin from the green mamba Dendroaspis angusticeps: amino acid sequence and selectivity for muscarinic m4 receptors.
Published in: FEBS Lett

Ligand: pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Selectivity profile of the novel muscarinic antagonist UH-AH 37 determined by the use of cloned receptors and isolated tissue preparations.
Published in: Br J Pharmacol

Ligand: pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Receptor binding studies of soft anticholinergic agents.
Published in: AAPS PharmSci

Ligand: propantheline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1953)
Primary target: no
Median affinity: 10.199999809265137 pKi
Reference (Journal): Receptor binding studies of soft anticholinergic agents.
Published in: AAPS PharmSci

Ligand: revefenacin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2018)
Primary target: no
Median affinity: 9.260000228881836 pKi
Reference (Journal): Pharmacological properties of revefenacin (TD-4208), a novel, nebulized long-acting, and lung selective muscarinic antagonist, at human recombinant muscarinic receptors and in rat, guinea pig, and human isolated airway tissues.
Published in: Pharmacol Res Perspect

Ligand: sabcomeline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 7.2 pKi
Reference (Journal): Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1, hM2, hM3, hM4 and hM5 using microphysiometry.
Published in: Br J Pharmacol

Ligand: scopolamine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1953)
Primary target: no
Median affinity:  pKi
Reference (Journal): Antagonism by antimuscarinic and neuroleptic compounds at the five cloned human muscarinic cholinergic receptors expressed in Chinese hamster ovary cells.
Published in: J Pharmacol Exp Ther

Ligand: scopolamine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1953)
Primary target: no
Median affinity:  pKi
Reference (Journal): Receptor binding studies of soft anticholinergic agents.
Published in: AAPS PharmSci

Ligand: (S)-dimetindene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.53000020980835 pKi
Reference (Journal): Structure-activity relationships of dimethindene derivatives as new M2-selective muscarinic receptor antagonists.
Published in: J Med Chem

Ligand: silahexocyclium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
Published in: Mol Pharmacol

Ligand: solifenacin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2004), UK (2009)
Primary target: no
Median affinity: 6.800000190734863 pKi
Reference (Journal): AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder.
Published in: Br J Pharmacol

Ligand: staurosporine (Natural product)
Interaction type: Allosteric modulator
Action: Neutral
Ligand approved: no
Median affinity: 5.3 pKd
Reference (Journal): Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-(3)H]scopolamine and acetylcholine at muscarinic receptor subtypes: identification of a second allosteric site.
Published in: Mol Pharmacol

Ligand: strychnine (Natural product)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: strychnine (Natural product)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors.
Published in: Mol Pharmacol

Ligand: [3H]acetylcholine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pKd
Reference (Journal): Thiochrome enhances acetylcholine affinity at muscarinic M4 receptors: receptor subtype selectivity via cooperativity rather than affinity.
Published in: Mol Pharmacol

Ligand: [3H]AF DX-384 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKd
Reference (Journal): The Impact of Removal of Ovarian Hormones on Cholinergic Muscarinic Receptors: Examining Prepulse Inhibition and Receptor Binding.
Published in: Brain Sci

Ligand: [3H]AF DX-384 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKd
Reference (Journal): Autoradiography of <sup>3</sup>H-pirenzepine and <sup>3</sup>H-AFDX-384 in Mouse Brain Regions: Possible Insights into M<sub>1</sub>, M<sub>2</sub>, and M<sub>4</sub> Muscarinic Receptors Distribution.
Published in: Front Pharmacol

Ligand: [3H]AF DX-384 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKd
Reference (Journal): Binding of [3H]AF-DX 384 to cloned and native muscarinic receptors.
Published in: J Pharmacol Exp Ther

Ligand: [3H]iperoxo (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 10.100000381469727 pKd
Reference (Journal): New insight into active muscarinic receptors with the novel radioagonist [³H]iperoxo.
Published in: Biochem Pharmacol

Ligand: [3H]N-methyl scopolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): High level stable expression of pharmacologically active human M1-M5 muscarinic receptor subtypes in mammalian cells.
Published in: Biotechnol Lett

Ligand: [3H]N-methyl scopolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: interactions of strychnine and acetylcholine at muscarinic receptors.
Published in: Mol Pharmacol

Ligand: [3H]N-methyl scopolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Subtype selectivity of the positive allosteric action of alcuronium at cloned M1-M5 muscarinic acetylcholine receptors.
Published in: J Pharmacol Exp Ther

Ligand: [3H]N-methyl scopolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Interaction of neuromuscular blocking drugs with recombinant human m1-m5 muscarinic receptors expressed in Chinese hamster ovary cells.
Published in: Br J Pharmacol

Ligand: [3H]N-methyl scopolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: [3H]N-methyl scopolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Application of transfected cell lines in studies of functional receptor subtype selectivity of muscarinic agonists.
Published in: J Pharmacol Exp Ther

Ligand: [3H]QNB (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Differential regulation of PI hydrolysis and adenylyl cyclase by muscarinic receptor subtypes.
Published in: Nature

Ligand: [3H]QNB (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Subtype selectivity of the positive allosteric action of alcuronium at cloned M1-M5 muscarinic acetylcholine receptors.
Published in: J Pharmacol Exp Ther

Ligand: thiochrome (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Primary target: no
Median affinity: 4 pKd
Reference (Journal): Thiochrome enhances acetylcholine affinity at muscarinic M4 receptors: receptor subtype selectivity via cooperativity rather than affinity.
Published in: Mol Pharmacol

Ligand: tiotropium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2004)
Primary target: no
Median affinity:  pKi
Reference (Journal): The Influence of receptor kinetics on the onset and duration of action and the therapeutic index of NVA237 and tiotropium.
Published in: J Pharmacol Exp Ther

Ligand: tiotropium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2004)
Primary target: no
Median affinity:  pKi
Reference (Journal): Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK.
Published in: Bioorg Med Chem Lett

Ligand: tolterodine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: no
Median affinity:  pKi
Reference (Journal): AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder.
Published in: Br J Pharmacol

Ligand: tolterodine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1998)
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparison of the in vitro and in vivo profiles of tolterodine with those of subtype-selective muscarinic receptor antagonists.
Published in: Eur J Pharmacol

Ligand: tripitramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.940000057220459 pKi
Reference (Journal): Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
Published in: Bioorg Med Chem

Ligand: tropicamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1960)
Primary target: no
Median affinity: 6.900000095367432 pKi
Reference (Journal): Myopia-Inhibiting Concentrations of Muscarinic Receptor Antagonists Block Activation of Alpha2A-Adrenoceptors In Vitro.
Published in: Invest Ophthalmol Vis Sci

Ligand: UH-AH 37 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Comparison of the in vitro and in vivo profiles of tolterodine with those of subtype-selective muscarinic receptor antagonists.
Published in: Eur J Pharmacol

Ligand: UH-AH 37 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Selectivity profile of the novel muscarinic antagonist UH-AH 37 determined by the use of cloned receptors and isolated tissue preparations.
Published in: Br J Pharmacol

Ligand: umeclidinium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2013), EMA (2014)
Primary target: no
Median affinity: 10.300000190734863 pKi
Reference (Journal): Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases.
Published in: J Pharmacol Exp Ther

Ligand: vinburnine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 4.6 pKd
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: vincamine (Natural product)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 4.2 pKd
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: VU0010010 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders.
Published in: Trends Pharmacol Sci

Ligand: VU0152099 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.389999866485596 pEC50
Reference (Journal): Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats.
Published in: J Pharmacol Exp Ther

Ligand: VU0152100 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.420000076293945 pEC50
Reference (Journal): Centrally active allosteric potentiators of the M4 muscarinic acetylcholine receptor reverse amphetamine-induced hyperlocomotor activity in rats.
Published in: J Pharmacol Exp Ther

Ligand: VU0255035 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pKi
Reference (Journal): A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning.
Published in: Mol Pharmacol

Ligand: VU0467154 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6 pEC50
Reference (Journal): Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents.
Published in: ACS Chem Neurosci

Ligand: VU0467154 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pEC50
Reference (Journal): Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents.
Published in: ACS Chem Neurosci

Ligand: VU0467154 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 7.75 pEC50
Reference (Journal): Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents.
Published in: ACS Chem Neurosci

Ligand: WIN 51,708 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.2 pKd
Reference (Journal): Analogs of WIN 62,577 define a second allosteric site on muscarinic receptors.
Published in: Mol Pharmacol

Ligand: WIN 62,577 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 5.9 pKd
Reference (Journal): Analogs of WIN 62,577 define a second allosteric site on muscarinic receptors.
Published in: Mol Pharmacol

Ligand: xanomeline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Structural basis of efficacy-driven ligand selectivity at GPCRs.
Published in: Nat Chem Biol

Ligand: xanomeline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1, hM2, hM3, hM4 and hM5 using microphysiometry.
Published in: Br J Pharmacol

Ligand: xanomeline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Biased Profile of Xanomeline at the Recombinant Human M<sub>4</sub> Muscarinic Acetylcholine Receptor.
Published in: ACS Chem Neurosci

Ligand: xanomeline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.
Published in: Br J Pharmacol