Target family: Acetylcholine receptors (muscarinic) (type: gpcr)
Target: M<sub>2</sub> receptor

Ligand: 4-DAMP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 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: 4-DAMP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.2 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: 4-DAMP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: (+)-aceclidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The interaction of the enantiomers of aceclidine with subtypes of the muscarinic receptor.
Published in: J Pharmacol Exp Ther

Ligand: (+)-aceclidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Estimation of agonist activity at G protein-coupled receptors: analysis of M2 muscarinic receptor signaling through Gi/o,Gs, and G15.
Published in: J Pharmacol Exp Ther

Ligand: (-)-aceclidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): Estimation of agonist activity at G protein-coupled receptors: analysis of M2 muscarinic receptor signaling through Gi/o,Gs, and G15.
Published in: J Pharmacol Exp Ther

Ligand: (-)-aceclidine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pEC50
Reference (Journal): The interaction of the enantiomers of aceclidine with subtypes of the muscarinic receptor.
Published in: J Pharmacol Exp Ther

Ligand: acetylcholine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.4 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

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

Ligand: acetylcholine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: acetylcholine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Reverse engineering of the selective agonist TBPB unveils both orthosteric and allosteric modes of action at the M₁ muscarinic acetylcholine receptor.
Published in: Mol Pharmacol

Ligand: aclidinium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: no
Median affinity: 10.100000381469727 pIC50
Reference (Journal): Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide).
Published in: J Med Chem

Ligand: aclidinium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: no
Median affinity: 10.100000381469727 pIC50
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: AE9C90CB (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.600000381469727 pKi
Reference (Journal): AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder.
Published in: Br J Pharmacol

Ligand: AFDX384 (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: AFDX384 (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: alcuronium (Natural product)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands.
Published in: J Biol Chem

Ligand: alcuronium (Natural product)
Interaction type: Allosteric modulator
Action: Negative
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: alcuronium (Natural product)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors.
Published in: Mol Pharmacol

Ligand: Alexa-488-telenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Abundance, distribution, mobility and oligomeric state of M₂ muscarinic acetylcholine receptors in live cardiac muscle.
Published in: J Mol Cell Cardiol

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Primary target: yes
Median affinity: 7.929999828338623 pKi
Reference (Journal): Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics.
Published in: Biochem Pharmacol

Ligand: AQ-RA 741 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 pKi
Reference (Journal): Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: AQ-RA 741 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.399999618530273 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: arecaidine propargyl ester (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.7 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: arecoline (Natural product)
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: arecoline (Natural product)
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: arecoline (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pKi
Reference (Journal): Enhanced arecoline derivatives as muscarinic acetylcholine receptor M1 ligands for potential application as PET radiotracers.
Published in: Eur J Med Chem

Ligand: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Median affinity:  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: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Receptor binding studies of soft anticholinergic agents.
Published in: AAPS PharmSci

Ligand: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterization of PCS1055, a novel muscarinic M4 receptor antagonist.
Published in: Eur J Pharmacol

Ligand: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors.
Published in: EMBO J

Ligand: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity.
Published in: J Pharmacol Exp Ther

Ligand: benzatropine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1954)
Primary target: no
Median affinity: 8.59000015258789 pKi
Reference (Journal): Novel 4'-substituted and 4',4&quot;-disubstituted 3 alpha-(diphenylmethoxy)tropane analogs as potent and selective dopamine uptake inhibitors.
Published in: J Med Chem

Ligand: bethanechol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1948)
Primary target: yes
Median affinity: 4 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: bethanechol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1948)
Primary target: yes
Median affinity: 4 pKi
Reference (Journal): Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists.
Published in: Br J Pharmacol

Ligand: biperiden (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: no
Median affinity: 8.199999809265137 pKd
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: brucine (Natural product)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.
Published in: Mol Pharmacol

Ligand: brucine (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: brucine (Natural product)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 4.3 pKd
Reference (Journal): Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.
Published in: Mol Pharmacol

Ligand: brucine N-oxide (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 3.5 pKd
Reference (Journal): Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.
Published in: Mol Pharmacol

Ligand: brucine N-oxide (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 3.5 pKd
Reference (Journal): Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.
Published in: Mol Pharmacol

Ligand: carbachol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1972)
Median affinity: 5.7 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: carbachol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1972)
Primary target: no
Median affinity:  pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: carbachol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1972)
Primary target: no
Median affinity:  pKi
Reference (Journal): Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: cevimeline (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (2000)
Primary target: no
Median affinity: 6.070000171661377 pKi
Reference (Journal): SB 202026: a novel muscarinic partial agonist with functional selectivity for M1 receptors.
Published in: J Pharmacol Exp Ther

Ligand: C7/3-phth (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pKd
Reference (Journal): Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands.
Published in: J Biol Chem

Ligand: C7/3-phth (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 pKd
Reference (Journal): Characterization of the subtype selectivity of the allosteric modulator heptane-1,7-bis-(dimethyl-3'-phthalimidopropyl) ammonium bromide (C7/3-phth) at cloned muscarinic acetylcholine receptors.
Published in: Biochem Pharmacol

Ligand: Cy3B-telenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.399999618530273 pKi
Reference (Journal): Abundance, distribution, mobility and oligomeric state of M₂ muscarinic acetylcholine receptors in live cardiac muscle.
Published in: J Mol Cell Cardiol

Ligand: darifenacin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: EMA & FDA (2004)
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity.
Published in: J Pharmacol Exp Ther

Ligand: darifenacin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: EMA & FDA (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: darifenacin (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
Ligand approved: yes
Approval source: EMA & FDA (2004)
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: dexetimide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
Median affinity: 8.899999618530273 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: dexetimide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity: 8.8 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: dicyclomine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1950)
Median affinity: 6.6 pKi
Reference (Journal): Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
Published in: Mol Pharmacol

Ligand: dimethyl-W84 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 8.5 pKi
Reference (Journal): Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors.
Published in: Mol Pharmacol

Ligand: dosulepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 6.960000038146973 pKi
Reference (Journal): Antagonism of the five cloned human muscarinic cholinergic receptors expressed in CHO-K1 cells by antidepressants and antihistaminics.
Published in: Biochem Pharmacol

Ligand: Duo3 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 7.050000190734863 pEC50
Reference (Journal): Atypical muscarinic allosteric modulation: cooperativity between modulators and their atypical binding topology in muscarinic M2 and M2/M5 chimeric receptors.
Published in: Mol Pharmacol

Ligand: ethopropazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 8.140000343322754 pKi
Reference (Journal): The relative selectivity of anticholinergic drugs for the M1 and M2 muscarinic receptor subtypes.
Published in: Mov Disord

Ligand: furtrethonium (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.5 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: gallamine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: yes
Primary target: no
Median affinity:  pKd
Reference (Journal): The inhibitory effect of gallamine on muscarinic receptors.
Published in: Br J Pharmacol

Ligand: gallamine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: yes
Median affinity: 5.6 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: gallamine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Utility of an &quot;Allosteric Site-Impaired&quot; M<sub>2</sub> Muscarinic Acetylcholine Receptor as a Novel Construct for Validating Mechanisms of Action of Synthetic and Putative Endogenous Allosteric Modulators.
Published in: Mol Pharmacol

Ligand: gallamine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: yes
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: gallamine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors.
Published in: Mol Pharmacol

Ligand: gallamine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: yes
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: glycopyrrolate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961), EMA (2012)
Primary target: yes
Median affinity:  pIC50
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: glycopyrrolate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961), EMA (2012)
Primary target: yes
Median affinity:  pIC50
Reference (Journal): The discovery of new spirocyclic muscarinic M3 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: Gö 7874 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 5 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: guanylpirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5.300000190734863 pKi
Reference (Journal): Binding of the labelled muscarinic toxin 125I-MT1 to rat brain muscarinic M1 receptors.
Published in: Eur J Pharmacol

Ligand: hexahydrodifenidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.7 pKi
Reference (Journal): Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
Published in: Mol Pharmacol

Ligand: hexahydrosiladifenidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: hexahydrosiladifenidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

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

Ligand: hexocyclium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
Published in: Mol Pharmacol

Ligand: himbacine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Binding and functional selectivity of himbacine for cloned and neuronal muscarinic receptors.
Published in: J Pharmacol Exp Ther

Ligand: himbacine (Natural product)
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: himbacine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: himbacine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.9 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: himbacine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
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: imipramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1959)
Median affinity: 6.9 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: N-benzyl brucine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 4.8 pKd
Reference (Journal): Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.
Published in: Mol Pharmacol

Ligand: N-benzyl brucine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 4.8 pKd
Reference (Journal): Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.
Published in: Mol Pharmacol

Ligand: iperoxo (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pEC50
Reference (Journal): New insight into active muscarinic receptors with the novel radioagonist [³H]iperoxo.
Published in: Biochem Pharmacol

Ligand: iperoxo (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 9.800000190734863 pEC50
Reference (Journal): Agonists with supraphysiological efficacy at the muscarinic M2 ACh receptor.
Published in: Br J Pharmacol

Ligand: p-F-HHSiD (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Receptor binding studies of soft anticholinergic agents.
Published in: AAPS PharmSci

Ligand: p-F-HHSiD (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: 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: ipratropium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity:  pKi
Reference (Journal): Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide).
Published in: J Med Chem

Ligand: ipratropium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity.
Published in: J Pharmacol Exp Ther

Ligand: KT 5823 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.7 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: levetimide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 4.8 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: levetimide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: lithocholylcholine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.4 pKi
Reference (Journal): Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: LY2033298 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 4.400000095367432 pKd
Reference (Journal): Probe dependence in the allosteric modulation of a G protein-coupled receptor: implications for detection and validation of allosteric ligand effects.
Published in: Mol Pharmacol

Ligand: LY2119620 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Activation and allosteric modulation of a muscarinic acetylcholine receptor.
Published in: Nature

Ligand: LY2119620 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M(2) and M(4) receptors.
Published in: Mol Pharmacol

Ligand: McN-A-343 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): New functionally selective muscarinic agonists.
Published in: Life Sci

Ligand: mepenzolic acid (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1956)
Primary target: no
Median affinity: 9.170000076293945 pKi
Reference (Journal): Synthesis and biological comparison of enantiomers of mepenzolate bromide, a muscarinic receptor antagonist with bronchodilatory and anti-inflammatory activities.
Published in: Bioorg Med Chem

Ligand: methacholine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity: 7.230000019073486 pKi
Reference (Journal): 6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
Published in: J Med Chem

Ligand: methacholine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity: 7.230000019073486 pKi
Reference (Journal): Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists.
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): Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor.
Published in: J Pharmacol Exp Ther

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: methoctramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

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
Median affinity: 7.3 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

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): Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
Published in: Mol Pharmacol

Ligand: methylfurmethide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.9 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol 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 3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 pA2
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 3 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6 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 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: Positive
Ligand approved: no
Median affinity: 4.6 pKd
Reference (Journal): Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.
Published in: Mol Pharmacol

Ligand: N-chloromethyl-brucine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 4.6 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: 7.2 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: 10.1 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: 8.2 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
Median affinity:  pKi
Reference (Journal): Cloned M1 muscarinic receptors mediate both adenylate cyclase inhibition and phosphoinositide turnover.
Published in: EMBO J

Ligand: otenzepad (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  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: otenzepad (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: otenzepad (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: otenzepad (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: oxotremorine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.5 pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: oxotremorine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  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:  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: 4.9 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: Inverse agonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2004)
Primary target: no
Median affinity: 7.929999828338623 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): 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: pentylthio-TZTP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.9 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: 4.900000095367432 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: 4.900000095367432 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
Median affinity:  pKi
Reference (Journal): Cloned M1 muscarinic receptors mediate both adenylate cyclase inhibition and phosphoinositide turnover.
Published in: EMBO J

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): Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor.
Published in: J Pharmacol Exp Ther

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: 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
Median affinity:  pKi
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

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
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: pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Median affinity:  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): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: propantheline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1953)
Primary target: yes
Median affinity: 9.5 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: 9.520000457763672 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: SCH 57790 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): SCH 57790: a novel M2 receptor selective antagonist.
Published in: Life Sci

Ligand: scopolamine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1953)
Primary target: no
Median affinity: 8.699999809265137 pKi
Reference (Journal): Receptor binding studies of soft anticholinergic agents.
Published in: AAPS PharmSci

Ligand: scopolamine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1953)
Primary target: no
Median affinity: 8.699999809265137 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: (S)-dimetindene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.519999980926514 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: 7.5 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: yes
Median affinity: 6.239999771118164 pIC50
Reference (Journal): Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl carbamates as potent and long acting muscarinic antagonists.
Published in: Bioorg Med Chem Lett

Ligand: solifenacin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2004), UK (2009)
Primary target: yes
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: solifenacin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2004), UK (2009)
Primary target: yes
Median affinity:  pKi
Reference (Journal): M(3) receptor antagonism by the novel antimuscarinic agent solifenacin in the urinary bladder and salivary gland.
Published in: Naunyn Schmiedebergs Arch Pharmacol

Ligand: staurosporine (Natural product)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.1 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: strychnine (Natural product)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  pKd
Reference (Journal): Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors.
Published in: Mol Pharmacol

Ligand: [18F]FP-TZTP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Regional brain uptake of the muscarinic ligand, [18F]FP-TZTP, is greatly decreased in M2 receptor knockout mice but not in M1, M3 and M4 receptor knockout mice.
Published in: Neuropharmacology

Ligand: [3H]4NMPB (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.4 pKd
Reference (Journal): Cloned M1 muscarinic receptors mediate both adenylate cyclase inhibition and phosphoinositide turnover.
Published in: EMBO J

Ligand: [3H]acetylcholine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 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: 9 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: 9 pKd
Reference (Journal): Binding of [3H]AF-DX 384 to cloned and native muscarinic receptors.
Published in: J Pharmacol Exp Ther

Ligand: [3H]AF DX-384 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9 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]clidinium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.6 pKd
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: [3H]clidinium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.5 pKd
Reference (Journal): Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
Published in: J Pharmacol Exp Ther

Ligand: [3H]dimethyl-W84 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 8.5 pKd
Reference (Journal): Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors.
Published in: Mol Pharmacol

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): Differences in kinetics of xanomeline binding and selectivity of activation of G proteins at M(1) and M(2) 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): 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): Pharmacological properties of (2R)-N-[1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl]-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: a novel mucarinic antagonist with M(2)-sparing antagonistic activity.
Published in: J Pharmacol Exp Ther

Ligand: [3H]N-methyl scopolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.5 pKd
Reference (Journal): Cloned M1 muscarinic receptors mediate both adenylate cyclase inhibition and phosphoinositide turnover.
Published in: EMBO J

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]oxotremorine-M (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 pKd
Reference (Journal): Solubilization and characterization of guanine nucleotide-sensitive muscarinic agonist binding sites from rat myocardium.
Published in: Br J Pharmacol

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: [3H]QNB (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors.
Published in: EMBO J

Ligand: [3H]tiotropium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.300000190734863 pKd
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: tacrine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: yes
Approval source: FDA (1993)
Primary target: no
Median affinity: 5.679999828338623 pIC50
Reference (Journal): Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
Published in: J Med Chem

Ligand: thiochrome (Synthetic organic)
Interaction type: Allosteric modulator
Action: Neutral
Median affinity: 3.9 pKd
Reference (Journal): Thiochrome enhances acetylcholine affinity at muscarinic M4 receptors: receptor subtype selectivity via cooperativity rather than affinity.
Published in: Mol Pharmacol

Ligand: THRX160209 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 pKi
Reference (Journal): A novel multivalent ligand that bridges the allosteric and orthosteric binding sites of the M2 muscarinic receptor.
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): Ba 679 BR, a novel long-acting anticholinergic bronchodilator.
Published in: Life Sci

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: tiotropium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2004)
Primary target: no
Median affinity:  pKi
Reference (Journal): Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide).
Published in: J Med Chem

Ligand: tolterodine (Synthetic organic)
Interaction type: Antagonist
Action: Inverse agonist
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: Inverse agonist
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: 9.600000381469727 pKi
Reference (Journal): Binding profile of the selective muscarinic receptor antagonist tripitramine.
Published in: Eur J Pharmacol

Ligand: tropicamide (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1960)
Primary target: no
Median affinity: 7.199999809265137 pKi
Reference (Journal): Characterization of PCS1055, a novel muscarinic M4 receptor antagonist.
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: 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: umeclidinium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2013), EMA (2014)
Primary target: no
Median affinity: 9.819999694824219 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: umeclidinium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2013), EMA (2014)
Primary target: no
Median affinity: 9.819999694824219 pKi
Reference (Journal): Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists.
Published in: J Med Chem

Ligand: vinburnine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Neutral
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: vincamine (Natural product)
Interaction type: Allosteric modulator
Action: Neutral
Ligand approved: no
Median affinity: 5.1 pKd
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: VU0255035 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.199999809265137 pKi
Reference (Journal): A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning.
Published in: Mol Pharmacol

Ligand: W-84 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Development of a new type of allosteric modulator of muscarinic receptors: hybrids of the antagonist AF-DX 384 and the hexamethonio derivative W84.
Published in: J Med Chem

Ligand: W-84 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.6 pKi
Reference (Journal): Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors.
Published in: Mol Pharmacol

Ligand: W-84 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors.
Published in: Mol Pharmacol

Ligand: WDuo3 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.9 pKi
Reference (Journal): Interactions of orthosteric and allosteric ligands with [3H]dimethyl-W84 at the common allosteric site of muscarinic M2 receptors.
Published in: Mol Pharmacol

Ligand: WIN 51,708 (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: WIN 62,577 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 5.3 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: Full 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: Full 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: Full 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