Target family: Acetylcholine receptors (muscarinic) (type: gpcr)
Target: M<sub>1</sub> receptor

Ligand: 4-DAMP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.9 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
Primary target: no
Median affinity: 9.300000190734863 pKi
Reference (Journal): Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: AC-260584 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.9 pIC50
Reference (Journal): Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation.
Published in: Mol Pharmacol

Ligand: AC-42 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M(1) receptor: direct pharmacological evidence that AC-42 is an allosteric agonist.
Published in: Mol Pharmacol

Ligand: AC-42 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 6.2 pKi
Reference (Journal): Probing the molecular mechanism of interaction between 4-n-butyl-1-[4-(2-methylphenyl)-4-oxo-1-butyl]-piperidine (AC-42) and the muscarinic M(1) receptor: direct pharmacological evidence that AC-42 is an allosteric agonist.
Published in: Mol Pharmacol

Ligand: (+)-aceclidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.4 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: Partial agonist
Ligand approved: no
Median affinity: 5 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
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): 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: acetylcholine (Metabolite)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5 pKi
Reference (Journal): Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: aclidinium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA and EMA (2012)
Primary target: no
Median affinity:  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:  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: AFDX384 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.5 pKi
Reference (Journal): Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: alcuronium (Natural product)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 5 pKd
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: Alexa-488-telenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.300000190734863 pKd
Reference (Journal): Formation and dissociation of M1 muscarinic receptor dimers seen by total internal reflection fluorescence imaging of single molecules.
Published in: Proc Natl Acad Sci USA

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Primary target: yes
Median affinity: 7.829999923706055 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:  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:  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
Primary target: no
Median affinity: 6.400000095367432 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: 5.699999809265137 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: arecoline (Natural product)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.699999809265137 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: 5.699999809265137 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: Partial agonist
Ligand approved: no
Median affinity: 5.3 pKi
Reference (Journal): Pharmacological characterization of the M1 muscarinic receptors expressed in murine fibroblast B82 cells.
Published in: J Pharmacol Exp Ther

Ligand: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Primary target: yes
Median affinity:  pKi
Reference (Journal): Characterisation of [3H]-darifenacin as a novel radioligand for the study of muscarinic M3 receptors.
Published in: J Recept Signal Transduct Res

Ligand: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Median affinity:  pKi
Reference (Journal): Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist.
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): Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
Published in: Mol 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: atropine (Natural product)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1973)
Primary target: yes
Median affinity:  pKi
Reference (Journal): On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor.
Published in: Mol Pharmacol

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): Identification of various allosteric interaction sites on M1 muscarinic receptor using 125I-Met35-oxidized muscarinic toxin 7.
Published in: Mol Pharmacol

Ligand: AZD6088 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: yes
Median affinity: 8.300000190734863 pEC50
Reference (Webpage): M1 muscarinic receptor agonist.

Ligand: benzatropine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1954)
Primary target: no
Median affinity: 9.020000457763672 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: benzoquinazolinone 12 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.599999904632568 pKB
Reference (Journal): Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor.
Published in: J Biol Chem

Ligand: bethanechol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1948)
Primary target: no
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: bethanechol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1948)
Median affinity: 3.7 pKi
Reference (Journal): Pharmacological characterization of the M1 muscarinic receptors expressed in murine fibroblast B82 cells.
Published in: J Pharmacol Exp Ther

Ligand: bethanechol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1948)
Primary target: no
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: biperiden (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1959)
Primary target: yes
Median affinity: 9.319999694824219 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: BODIPY-pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7 pKi
Reference (Journal): Pirenzepine promotes the dimerization of muscarinic M1 receptors through a three-step binding process.
Published in: J Biol Chem

Ligand: BQCA (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor.
Published in: J Biol Chem

Ligand: BQCA (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation.
Published in: Proc Natl Acad Sci USA

Ligand: BQCA (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): A Monod-Wyman-Changeux mechanism can explain G protein-coupled receptor (GPCR) allosteric modulation.
Published in: J Biol Chem

Ligand: BQCA (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): Molecular determinants of allosteric modulation at the M1 muscarinic acetylcholine receptor.
Published in: J Biol Chem

Ligand: brucine (Natural product)
Interaction type: Allosteric modulator
Action: Neutral
Ligand approved: no
Primary target: no
Median affinity: 4.5 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 (Natural product)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Subtype-selective positive cooperative interactions between brucine analogs and acetylcholine at muscarinic receptors: functional studies.
Published in: Mol Pharmacol

Ligand: brucine (Natural product)
Interaction type: Allosteric modulator
Action: Positive
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: brucine (Natural product)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: 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 N-oxide (Synthetic organic)
Interaction type: Allosteric modulator
Action: Neutral
Ligand approved: no
Median affinity: 3.2 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
Primary target: no
Median affinity: 3.200000047683716 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)
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): On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor.
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): Functional comparison of muscarinic partial agonists at muscarinic receptor subtypes hM1, hM2, hM3, hM4 and hM5 using microphysiometry.
Published in: Br J Pharmacol

Ligand: carbachol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1972)
Median affinity: 3.9 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: 5.309999942779541 pKi
Reference (Journal): SB 202026: a novel muscarinic partial agonist with functional selectivity for M1 receptors.
Published in: J Pharmacol Exp Ther

Ligand: clozapine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1989)
Median affinity: 7.9 pIC50
Reference (Journal): N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity.
Published in: Proc Natl Acad Sci USA

Ligand: clozapine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1989)
Median affinity: 7.7 pIC50
Reference (Journal): Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation.
Published in: Mol Pharmacol

Ligand: Cy3B-telenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 10.5 pKd
Reference (Journal): Formation and dissociation of M1 muscarinic receptor dimers seen by total internal reflection fluorescence imaging of single molecules.
Published in: Proc Natl Acad Sci USA

Ligand: darifenacin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
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: Antagonist
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: Antagonist
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: dicyclomine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1950)
Primary target: yes
Median affinity: 9.079999923706055 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: dosulepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 7.739999771118164 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: droxidopa (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2014)
Primary target: no
Median affinity: 7.099999904632568 pKi
Reference (Journal): Characterization of PCS1055, a novel muscarinic M4 receptor antagonist.
Published in: Eur J Pharmacol

Ligand: ethopropazine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 8.510000228881836 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: 4.1 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

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: 5.8 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:  pKi
Reference (Journal): Binding of the labelled muscarinic toxin 125I-MT1 to rat brain muscarinic M1 receptors.
Published in: Eur J Pharmacol

Ligand: guanylpirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Subtypes of muscarinic receptors in rat duodenum: a comparison with rabbit vas deferens, rat atria, guinea-pig ileum and gallbladder by using imperialine.
Published in: Gen Pharmacol

Ligand: hexahydrodifenidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8 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: 7.7 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: 8.6 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): 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): 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): A toxin from the green mamba Dendroaspis angusticeps: amino acid sequence and selectivity for muscarinic m4 receptors.
Published in: FEBS Lett

Ligand: N-benzyl brucine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
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: N-desmethylclozapine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 7.3 pIC50
Reference (Journal): N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity.
Published in: Proc Natl Acad Sci USA

Ligand: N-desmethylclozapine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 6.8 pIC50
Reference (Journal): Structural requirements of transmembrane domain 3 for activation by the M1 muscarinic receptor agonists AC-42, AC-260584, clozapine, and N-desmethylclozapine: evidence for three distinct modes of receptor activation.
Published in: Mol Pharmacol

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

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: 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: 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: K-252a (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: KT 5720 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.400000095367432 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: 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: lithocholylcholine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.6 pKi
Reference (Journal): Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: LY593093 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 6.210000038146973 pKi
Reference (Journal): Pharmacological characterization of LY593093, an M1 muscarinic acetylcholine receptor-selective partial orthosteric agonist.
Published in: J Pharmacol Exp Ther

Ligand: McN-A-343 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: 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: McN-A-343 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.1 pKi
Reference (Journal): Pharmacological characterization of the M1 muscarinic receptors expressed in murine fibroblast B82 cells.
Published in: J Pharmacol Exp Ther

Ligand: methacholine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity: 6.400000095367432 pEC50
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: 6.400000095367432 pEC50
Reference (Journal): 6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
Published in: J Med Chem

Ligand: methoctramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Characterisation of [3H]-darifenacin as a novel radioligand for the study of muscarinic M3 receptors.
Published in: J Recept Signal Transduct Res

Ligand: methoctramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.8 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): 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): 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): Stimulation of cyclic AMP accumulation and phosphoinositide hydrolysis by M3 muscarinic receptors in the rat peripheral lung.
Published in: Biochem Pharmacol

Ligand: methylfurmethide (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 4.6 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: milameline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 4.8 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: MK-7622 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): MK-7622: A First-in-Class M<sub>1</sub> Positive Allosteric Modulator Development Candidate.
Published in: ACS Med Chem Lett

Ligand: ML169 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 5.900000095367432 pEC50
Reference (Journal): Targeting selective activation of M(1) for the treatment of Alzheimer's disease: further chemical optimization and pharmacological characterization of the M(1) positive allosteric modulator ML169.
Published in: ACS Chem Neurosci

Ligand: ML381 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 5 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:  pKi
Reference (Journal): Effects of muscarinic toxins MT1 and MT2 from green mamba on different muscarinic cholinoceptors.
Published in: Neurochem Res

Ligand: muscarinic toxin 1 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Identification of various allosteric interaction sites on M1 muscarinic receptor using 125I-Met35-oxidized muscarinic toxin 7.
Published in: Mol Pharmacol

Ligand: muscarinic toxin 2 (Peptide)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 6.4 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: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.099999904632568 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: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Recombinant expression of a selective blocker of M(1) muscarinic receptors.
Published in: Biochem Biophys Res Commun

Ligand: muscarinic toxin 7 (Peptide)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Inhibition of acetylcholine muscarinic M(1) receptor function by the M(1)-selective ligand muscarinic toxin 7 (MT-7).
Published in: Br J Pharmacol

Ligand: muscarinic toxin 7 (Peptide)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKi
Reference (Journal): Identification of various allosteric interaction sites on M1 muscarinic receptor using 125I-Met35-oxidized muscarinic toxin 7.
Published in: Mol Pharmacol

Ligand: N-chloromethyl-brucine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 4.1 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-methyl scopolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1953)
Primary target: yes
Median affinity: 9.899999618530273 pKi
Reference (Journal): Identification of various allosteric interaction sites on M1 muscarinic receptor using 125I-Met35-oxidized muscarinic toxin 7.
Published in: Mol Pharmacol

Ligand: NNC 11-1314 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.4 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: 9.9 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: 8.6 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: 6.199999809265137 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:  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
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: oxotremorine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 5.5 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: oxotremorine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Primary target: no
Median affinity: 5.5 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: Partial agonist
Ligand approved: no
Median affinity: 6 pKi
Reference (Journal): Pharmacological characterization of the M1 muscarinic receptors expressed in murine fibroblast B82 cells.
Published in: J Pharmacol Exp Ther

Ligand: oxotremorine-M (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity: 5.099999904632568 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: 5.6 pKi
Reference (Journal): Pharmacological characterization of the M1 muscarinic receptors expressed in murine fibroblast B82 cells.
Published in: J Pharmacol Exp Ther

Ligand: oxybutynin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2004)
Primary target: yes
Median affinity: 8.600000381469727 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: yes
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: oxybutynin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2004)
Primary target: no
Median affinity: 8.199999809265137 pKi
Reference (Journal): Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists.
Published in: J Med Chem

Ligand: pentylthio-TZTP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.6 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: PF-06767832 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: yes
Median affinity: 7.21999979019165 pEC50
Reference (Journal): Discovery of the Potent and Selective M1 PAM-Agonist N-[(3R,4S)-3-Hydroxytetrahydro-2H-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects.
Published in: J Med Chem

Ligand: pilocarpine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: no
Median affinity: 5.099999904632568 pKi
Reference (Journal): Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists.
Published in: Br J Pharmacol

Ligand: pilocarpine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1974)
Median affinity: 4.9 pKi
Reference (Journal): Pharmacological characterization of the M1 muscarinic receptors expressed in murine fibroblast B82 cells.
Published in: J Pharmacol Exp Ther

Ligand: pilocarpine (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: yes
Approval source: FDA (1974)
Primary target: no
Median affinity: 5.099999904632568 pKi
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: yes
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
Primary target: yes
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: yes
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: yes
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
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: yes
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: yes
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: (±)YM796 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of a novel muscarinic partial agonist, YM796, in transfected cells expressing the m1 or m2 muscarinic receptor gene.
Published in: Life Sci

Ligand: propantheline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1953)
Primary target: yes
Median affinity: 9.699999809265137 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: 9.380000114440918 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: 6.7 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: yes
Median affinity: 9 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: yes
Median affinity: 9 pKi
Reference (Journal): Characterization of PCS1055, a novel muscarinic M4 receptor antagonist.
Published in: Eur J Pharmacol

Ligand: (S)-dimetindene (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.71999979019165 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: 8.7 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: 7.599999904632568 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: no
Median affinity: 7.599999904632568 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: solifenacin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2004), UK (2009)
Primary target: no
Median affinity: 8 pKi
Reference (Journal): Synthesis and antimuscarinic properties of quinuclidin-3-yl 1,2,3,4-tetrahydroisoquinoline-2-carboxylate derivatives as novel muscarinic receptor antagonists.
Published in: J Med Chem

Ligand: solifenacin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (2004), UK (2009)
Primary target: no
Median affinity: 7.199999809265137 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: SPP1 (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Identification and pharmacological profile of SPP1, a potent, functionally selective and brain penetrant agonist at muscarinic M<sub>1</sub> receptors.
Published in: Br J Pharmacol

Ligand: staurosporine (Natural product)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity: 5.9 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: Neutral
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: Negative
Ligand approved: no
Median affinity: 4.9 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: Neutral
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: [11C]butylthio-TZTP (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): PET study of the M1-agonists [11C]xanomeline and [11C]butylthio-TZTP in monkey and man.
Published in: Dementia

Ligand: [11C]xanomeline (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): PET study of the M1-agonists [11C]xanomeline and [11C]butylthio-TZTP in monkey and man.
Published in: Dementia

Ligand: [18F](R,R)-quinuclidinyl-4-fluoromethyl-benzilate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): In vivo muscarinic binding selectivity of (R,S)- and (R,R)-[18F]-fluoromethyl QNB.
Published in: Bioorg Med Chem

Ligand: [3H]acetylcholine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -

Ligand: [3H]darifenacin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKd
Reference (Journal): Characterisation of [3H]-darifenacin as a novel radioligand for the study of muscarinic M3 receptors.
Published in: J Recept Signal Transduct Res

Ligand: [3H]iperoxo (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 8.699999809265137 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): 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): On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor.
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): 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): 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
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
Median affinity: 9.7 pKd
Reference (Journal): Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist.
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 anandamide with the M(1) and M(4) muscarinic acetylcholine receptors.
Published in: Brain Res

Ligand: [3H]N-methyl scopolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): A toxin from the green mamba Dendroaspis angusticeps: amino acid sequence and selectivity for muscarinic m4 receptors.
Published in: FEBS Lett

Ligand: [3H]N-methyl scopolamine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9.7 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]pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 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]pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): The existence of stable enantiomers of telenzepine and their stereoselective interaction with muscarinic receptor subtypes.
Published in: Mol Pharmacol

Ligand: [3H]pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity:  pKd
Reference (Journal): Pirenzepine distinguishes between different subclasses of muscarinic receptors.
Published in: Nature

Ligand: [3H]pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKd
Reference (Journal): Muscarinic receptors: do they have a role in the pathology and treatment of schizophrenia?
Published in: J Neurochem

Ligand: [3H]pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 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]pirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.900000095367432 pKd
Reference (Journal): [3H]Pirenzepine identifies putative M1 muscarinic receptors in human stellate ganglia.
Published in: Brain Res

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](+)telenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.399999618530273 pKi
Reference (Journal): The existence of stable enantiomers of telenzepine and their stereoselective interaction with muscarinic receptor subtypes.
Published in: Mol Pharmacol

Ligand: T440 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 8.199999809265137 pEC50
Reference (Journal): Effects and sites of action of a M1 receptor positive allosteric modulator on colonic motility in rats and dogs compared with 5-HT<sub>4</sub> agonism and cholinesterase inhibition.
Published in: Neurogastroenterol Motil

Ligand: T440 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 8.229999542236328 pEC50
Reference (Journal): Effects and sites of action of a M1 receptor positive allosteric modulator on colonic motility in rats and dogs compared with 5-HT<sub>4</sub> agonism and cholinesterase inhibition.
Published in: Neurogastroenterol Motil

Ligand: T‐495 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): T-495, a novel low cooperative M<sub>1</sub> receptor positive allosteric modulator, improves memory deficits associated with cholinergic dysfunction and is characterized by low gastrointestinal side effect risk.
Published in: Pharmacol Res Perspect

Ligand: T532 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity:  pEC50
Reference (Journal): Muscarinic receptor 1 allosteric modulators stimulate colorectal emptying in dog, mouse and rat and resolve constipation.
Published in: Neurogastroenterol Motil

Ligand: tacrine (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: yes
Approval source: FDA (1993)
Primary target: no
Median affinity: 5.699999809265137 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: 4.1 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): 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: 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): Ba 679 BR, a novel long-acting anticholinergic bronchodilator.
Published in: Life Sci

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: trihexyphenidyl (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1949)
Primary target: yes
Median affinity: 8.869999885559082 pKi
Reference (Webpage): National Toxicology Program: Dept of Health and Human Services.

Ligand: tripitramine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 8.800000190734863 pKi
Reference (Journal): Binding profile of the selective muscarinic receptor antagonist tripitramine.
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: 9.800000190734863 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: 9.800000190734863 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: 5.1 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: 4.8 pKd
Reference (Journal): Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors.
Published in: Mol Pharmacol

Ligand: VU0029767 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity.
Published in: Mol Pharmacol

Ligand: VU0090157 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Median affinity:  -
Reference (Journal): Discovery and characterization of novel allosteric potentiators of M1 muscarinic receptors reveals multiple modes of activity.
Published in: Mol Pharmacol

Ligand: VU0119498 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 5.199999809265137 pEC50
Reference (Journal): Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.
Published in: J Med Chem

Ligand: VU0255035 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 7.800000190734863 pKi
Reference (Journal): A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning.
Published in: Mol Pharmacol

Ligand: VU0486846 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity: 5.400000095367432 pEC50
Reference (Journal): A Novel M<sub>1</sub> PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity.
Published in: ACS Chem Neurosci

Ligand: VU0486846 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 6.510000228881836 pEC50
Reference (Journal): A Novel M<sub>1</sub> PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity.
Published in: ACS Chem Neurosci

Ligand: WIN 51,708 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Median affinity: 5.8 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: 5.5 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): Functional effects of the muscarinic receptor agonist, xanomeline, at 5-HT1 and 5-HT2 receptors.
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): On the unique binding and activating properties of xanomeline at the M1 muscarinic acetylcholine receptor.
Published in: Mol Pharmacol

Ligand: (-)-YM796 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity:  pKi
Reference (Journal): Pharmacological characterization of a novel muscarinic partial agonist, YM796, in transfected cells expressing the m1 or m2 muscarinic receptor gene.
Published in: Life Sci