Target family: Acetylcholine receptors (muscarinic) (type: gpcr)
Target: M<sub>5</sub> receptor

Ligand: 4-DAMP (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 9 pKi
Reference (Journal): Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
Published in: J Pharmacol Exp Ther

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: (+)-aceclidine (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 5.5 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: 5.1 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: 6.099999904632568 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: 9.899999618530273 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: AE9C90CB (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 9.5 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: 6.300000190734863 pKi
Reference (Journal): Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
Published in: J Pharmacol Exp Ther

Ligand: amiodarone (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: yes
Approval source: FDA (1985)
Primary target: no
Median affinity: 7.25 pKB
Reference (Journal): Novel allosteric effects of amiodarone at the muscarinic M5 receptor.
Published in: J Pharmacol Exp Ther

Ligand: amitriptyline (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961)
Primary target: yes
Median affinity: 7.800000190734863 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: arecoline (Natural product)
Interaction type: Agonist
Action: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
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: Agonist
Ligand approved: no
Primary target: no
Median affinity:  -
Reference (Journal): Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists.
Published in: Br 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): 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): Affinity profiles of various muscarinic antagonists for cloned human muscarinic acetylcholine receptor (mAChR) subtypes and mAChRs in rat heart and submandibular gland.
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): 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)
Median affinity: 9.4 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: bethanechol (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (no history prior to 1948)
Primary target: no
Median affinity:  -
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: Negative
Ligand approved: no
Median affinity: 2.9 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: 2.3 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: 2.3 pKd
Reference (Journal): Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: radioligand binding studies.
Published in: Mol Pharmacol

Ligand: carbachol (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: yes
Approval source: FDA (1972)
Primary target: no
Median affinity: 4.900000095367432 pKi
Reference (Journal): Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators.
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: 4.900000095367432 pKi
Reference (Journal): Persistent binding and functional antagonism by xanomeline at the muscarinic M5 receptor.
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: 4.900000095367432 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: 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: 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): 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: dosulepin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Primary target: no
Median affinity: 7.039999961853027 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: glycopyrrolate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961), EMA (2012)
Primary target: yes
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: glycopyrrolate (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1961), EMA (2012)
Primary target: yes
Median affinity:  pKi
Reference (Journal): The discovery of new spirocyclic muscarinic M3 antagonists.
Published in: Bioorg Med Chem Lett

Ligand: guanylpirenzepine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.800000190734863 pKd
Reference (Journal): Selective labeling and localization of the M4 (m4) muscarinic receptor subtype.
Published in: Mol Pharmacol

Ligand: hexahydrodifenidol (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 7.1 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): 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): 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: 7.4 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: hexocyclium (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 8.4 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): 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: 3.7 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: Neutral
Ligand approved: no
Median affinity: 3.7 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: 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: 6.3 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: 8.800000190734863 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: lithocholylcholine (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Median affinity: 5.2 pKi
Reference (Journal): Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist.
Published in: J Pharmacol Exp Ther

Ligand: McN-A-343 (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 4.9 pKi
Reference (Journal): Human muscarinic receptors expressed in A9L and CHO cells: activation by full and partial agonists.
Published in: Br J Pharmacol

Ligand: methacholine (Synthetic organic)
Interaction type: Agonist
Action: Agonist
Ligand approved: yes
Approval source: FDA (1986)
Primary target: no
Median affinity:  -
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): 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): Stimulation of cyclic AMP accumulation and phosphoinositide hydrolysis by M3 muscarinic receptors in the rat peripheral lung.
Published in: Biochem Pharmacol

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

Ligand: milameline (Synthetic organic)
Interaction type: Agonist
Action: Partial agonist
Ligand approved: no
Median affinity: 5.4 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: ML375 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators.
Published in: Mol Pharmacol

Ligand: ML375 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375).
Published in: J Med Chem

Ligand: ML375 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Negative
Ligand approved: no
Primary target: no
Median affinity:  pKB
Reference (Journal): Identification of a Novel Allosteric Site at the M<sub>5</sub> Muscarinic Acetylcholine Receptor.
Published in: ACS Chem Neurosci

Ligand: ML380 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 4.800000190734863 pKB
Reference (Journal): Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380).
Published in: J Med Chem

Ligand: ML380 (Synthetic organic)
Interaction type: Allosteric modulator
Action: Positive
Ligand approved: no
Primary target: no
Median affinity: 4.800000190734863 pKB
Reference (Journal): Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators.
Published in: Mol Pharmacol

Ligand: ML381 (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: no
Primary target: no
Median affinity: 6.300000190734863 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 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: 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: NNC 11-1314 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 7.8 pKi
Reference (Journal): Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists.
Published in: J Pharmacol Exp Ther

Ligand: NNC 11-1585 (Synthetic organic)
Interaction type: Agonist
Action: Full agonist
Ligand approved: no
Median affinity: 8.3 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
Primary target: no
Median affinity: 5.599999904632568 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: 5.7 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: oxybutynin (Synthetic organic)
Interaction type: Antagonist
Action: Antagonist
Ligand approved: yes
Approval source: FDA (1975), EMA (2004)
Primary target: no
Median affinity: 7.900000095367432 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: 7.900000095367432 pKi
Reference (Journal): 1,4-dioxane, a suitable scaffold for the development of novel M₃ muscarinic receptor antagonists.
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 pKi
Reference (Journal): Persistent binding and functional antagonism by xanomeline at the muscarinic M5 receptor.
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 pKi
Reference (Journal): Ligand binding properties of muscarinic acetylcholine receptor subtypes (m1-m5) expressed in baculovirus-infected insect 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 pKi
Reference (Journal): Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators.
Published in: Mol Pharmacol

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): A toxin from the green mamba Dendroaspis angusticeps: amino acid sequence and selectivity for muscarinic m4 receptors.
Published in: FEBS Lett

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