DGIdb - CHRM3 Gene Record

CHRM3 1131 Druggable Genome

Alternate Names:

1131
CHOLINERGIC RECEPTOR MUSCARINIC 3
CHRM3
EGBRS
HM3
PBS
118494
1952
ENSG00000133019
OTTHUMG00000039649
P20309
MUSCARINIC ACETYLCHOLINE RECEPTOR M3
ACM3_HUMAN
MUSCARINIC ACETYLCHOLINE RECEPTOR M3. [SOURCE:UNIPROT/SWISSPROT;ACC:P20309]
T67684

Gene Info:

Uniprot Status	Swiss-Prot
Interpro Acc	IPR000276
Interpro Type	Family
Interpro Name	GPCR, rhodopsin-like, 7TM
Uniprot Evidence	1: Evidence at protein level
Human Readable Name	DRUGGABLE GENOME
Interpro Short Name	7TM_GPCR_Rhodpsn
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Transmembrane Helix Count	7
Target Subclass	GPCR
Target Subclass	Rhodopsin
Target Main Class	Receptors
Target Class	Receptors
Gene Biotype	PROTEIN_CODING

(6 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Hou et al., 1998, Neuromuscular relaxants as antagonists for M2 and M3 muscarinic receptors., Anesthesiology
Barnes, 2001, Tiotropium bromide., Expert Opin Investig Drugs
Barnes et al., 1995, Tiotropium bromide (Ba 679 BR), a novel long-acting muscarinic antagonist for the treatment of obstructive airways disease., Life Sci.
Hansel et al., 2002, Tiotropium bromide: a novel once-daily anticholinergic bronchodilator for the treatment of COPD., Drugs Today
Nasrallah, 2008, Atypical antipsychotic-induced metabolic side effects: insights from receptor-binding profiles., Mol. Psychiatry
Bymaster et al., 1999, Antagonism by olanzapine of dopamine D1, serotonin2, muscarinic, histamine H1 and alpha 1-adrenergic receptors in vitro., Schizophr. Res.
Brafford MV et al., 2014, Olanzapine: an antiemetic option for chemotherapy-induced nausea and vomiting., J Adv Pract Oncol
Sinha et al., 2010, AE9C90CB: a novel, bladder-selective muscarinic receptor antagonist for the treatment of overactive bladder., Br. J. Pharmacol.
Mansfield et al., 2009, Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa., J. Pharmacol. Exp. Ther.
Ito et al., 2009, Comparison of muscarinic receptor selectivity of solifenacin and oxybutynin in the bladder and submandibular gland of muscarinic receptor knockout mice., Eur. J. Pharmacol.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Bachrach, 1972, Clinical evaluation of anisotropine methyl bromide (valpin), an anticholinergic drug., Am J Dig Dis
Waelbroeck et al., 1992, Stereoselective interaction of procyclidine, hexahydro-difenidol, hexbutinol and oxyphencyclimine, and of related antagonists, with four muscarinic receptors., Eur. J. Pharmacol.
Schjelderup et al., 1988, Antimuscarinic effects of (R)- and (S)- oxyphencyclimine hydrochloride., Pharm. Res.
Baldwin et al., 2009, Transdermal oxybutynin., Drugs
Oki et al., 2007, Comparative evaluation of central muscarinic receptor binding activity by oxybutynin, tolterodine and darifenacin used to treat overactive bladder., J. Urol.
Maruyama et al., 2006, Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder., J. Urol.
Yarker YE et al., 1995, Oxybutynin. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic use in detrusor instability., Drugs Aging
Li et al., 2008, Degradation of submandibular gland AQP5 by parasympathetic denervation of chorda tympani and its recovery by cevimeline, an M3 muscarinic receptor agonist., Am. J. Physiol. Gastrointest. Liver Physiol.
Betz et al., 2007, The muscarinic receptor antagonist tropicamide suppresses tremulous jaw movements in a rodent model of parkinsonian tremor: possible role of M4 receptors., Psychopharmacology (Berl.)
McNamara et al., 2009, Pharmacological properties of TD-6301, a novel bladder selective muscarinic receptor antagonist., Eur. J. Pharmacol.
Sellers et al., 2000, M3 muscarinic receptors but not M2 mediate contraction of the porcine detrusor muscle in vitro., J Auton Pharmacol
Schneider et al., 2004, Signal transduction underlying carbachol-induced contraction of human urinary bladder., J. Pharmacol. Exp. Ther.
Bozkurt et al., 2009, M(1) and M(3) muscarinic receptors are involved in the release of urinary bladder-derived relaxant factor., Pharmacol. Res.
Bharucha et al., 2010, Comparison of selective M3 and nonselective muscarinic receptor antagonists on gastrointestinal transit and bowel habits in humans., Am. J. Physiol. Gastrointest. Liver Physiol.
Jha et al., 2006, Treatment of overactive bladder in the aging population: focus on darifenacin., Clin Interv Aging
Figueroa et al., 2009, Selectivity of agonists for the active state of M1 to M4 muscarinic receptor subtypes., J. Pharmacol. Exp. Ther.
Sykes et al., 2009, Exploring the mechanism of agonist efficacy: a relationship between efficacy and agonist dissociation rate at the muscarinic M3 receptor., Mol. Pharmacol.
Hals et al., 1988, Muscarinic cholinergic and histamine H1 receptor binding of phenothiazine drug metabolites., Life Sci.
Dahl et al., 1986, Phenothiazine drugs and metabolites: molecular conformation and dopaminergic, alpha adrenergic and muscarinic cholinergic receptor binding., Biochem. Pharmacol.
Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
Golembiewski et al., 2002, A systematic approach to the management of postoperative nausea and vomiting., J. Perianesth. Nurs.
Almadhoun K et al., 2020, Bronchodilators,
Wellington, 2005, Ipratropium bromide HFA., Treat Respir Med
Rehder KJ, 2017, Adjunct Therapies for Refractory Status Asthmaticus in Children., Respir Care
Varoli et al., 1999, Synthesis and antagonistic activity at muscarinic receptor subtypes of some 2-carbonyl derivatives of diphenidol., Bioorg. Med. Chem.
Braverman et al., 2002, Interaction between muscarinic receptor subtype signal transduction pathways mediating bladder contraction., Am. J. Physiol. Regul. Integr. Comp. Physiol.
Waelbroeck et al., 1991, Stereoselectivity of (R)- and (S)-hexahydro-difenidol binding to neuroblastoma M1, cardiac M2, pancreatic M3, and striatum M4 muscarinic receptors., Chirality
Nilvebrant, 2002, Tolterodine and its active 5-hydroxymethyl metabolite: pure muscarinic receptor antagonists., Pharmacol. Toxicol.
Figueiredo et al., 1990, Mechanism of action of doxepin in the treatment of chronic urticaria., Fundam Clin Pharmacol
Ehlert et al., 1990, The interaction of amitriptyline, doxepin, imipramine and their N-methyl quaternary ammonium derivatives with subtypes of muscarinic receptors in brain and heart., J. Pharmacol. Exp. Ther.
Lainé et al., 2009, Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists., J. Med. Chem.

DARIFENACIN CHRM3

Interaction Score: 3.09

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name darifenacin,Enablex, Emselex

Novel drug target Established target

PMIDs:
19416629 20395537 18046909 11752352

Sources:
TdgClinicalTrial TEND TTD
UMECLIDINIUM BROMIDE CHRM3

Interaction Score: 2.65

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
19317446

Sources:
DTC ChemblInteractions
TARAFENACIN CHRM3

Interaction Score: 2.65

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

Trial Name SVT-40776

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD
OXYBUTYNIN CHRM3

Interaction Score: 2.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

Trial Name transdermal oxybutynin patch, oxybutynin topical gel,Oxytrol, Kentera, Gelnique

PMIDs:
20590605 19275276 17222678 11752352 16406943 19446545 17016423 17139284 7620236

Sources:
TdgClinicalTrial ChemblInteractions TEND
CEVIMELINE CHRM3

Interaction Score: 2.06

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752352 17016423 17139284 18450949

Sources:
TdgClinicalTrial TEND TTD
ACLIDINIUM BROMIDE CHRM3

Interaction Score: 1.77

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD
ANISOTROPINE METHYLBROMIDE CHRM3

Interaction Score: 1.77

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

PMIDs:
4555460 17016423 17139284

Sources:
ChemblInteractions
DIPHEMANIL METHYLSULFATE CHRM3

Interaction Score: 1.77

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
17016423 17139284 11752352

Sources:
ChemblInteractions
SOLIFENACIN CHRM3

Interaction Score: 1.59

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Solifenacin succinate, YM-905,Vesicare

Novel drug target Established target

PMIDs:
20590605 11752352 19029429 19446545 17016423 17139284

Sources:
TdgClinicalTrial TEND TTD
OXYPHENCYCLIMINE CHRM3

Interaction Score: 1.32

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
1426023 3247303 17016423 17139284

Sources:
TdgClinicalTrial TEND
DIPHENIDOL CHRM3

Interaction Score: 1.24

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
10530931 12185001 17016423 17139284 1863523

Sources:
TdgClinicalTrial TEND
TIOTROPIUM CHRM3

Interaction Score: 1.24

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name tiotropium bromide,Spiriva

PMIDs:
11281822 10188785 12582447 11752352

Sources:
TdgClinicalTrial TEND TTD
AZD8683 CHRM3

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
CHEMBL1084941 CHRM3

Interaction Score: 0.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
CHEMBL1917204 CHRM3

Interaction Score: 0.88

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
IPRATROPIUM BROMIDE CHRM3

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

PMIDs:
None found

Sources:
ChemblInteractions
CYCLOPENTOLATE HYDROCHLORIDE CHRM3

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TIOTROPIUM BROMIDE CHRM3

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TRIDIHEXETHYL CHRM3

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
TROPICAMIDE CHRM3

Interaction Score: 0.88

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
17594079

Sources:
ChemblInteractions
FESOTERODINE CHRM3

Interaction Score: 0.71

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name fesoterodine fumarate, SPM 907,Toviaz

Novel drug target Established target

PMIDs:
12076307 11752352

Sources:
TdgClinicalTrial TEND
METHIXENE CHRM3

Interaction Score: 0.71

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
TOLTERODINE CHRM3

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name THVD-201

Novel drug target Established target

Trial Name tolterodine extended release capsules,Detrol LA

PMIDs:
19168050 11193006 11752352 14769832

Sources:
TdgClinicalTrial TEND TTD
SUXAMETHONIUM CHRM3

Interaction Score: 0.53

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
11752352 9523819

Sources:
TTD
IPRATROPIUM CHRM3

Interaction Score: 0.5

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
30085570 15987237 28546381

Sources:
TTD
BENZQUINAMIDE CHRM3

Interaction Score: 0.5

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
ATROPINE CHRM3

Interaction Score: 0.48

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

Trial Name inhaled atropine

PMIDs:
7855217 17016423 17139284

Sources:
TdgClinicalTrial ChemblInteractions TEND
DARIFENACIN HYDROBROMIDE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
LAS190792 CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
SOLIFENACIN SUCCINATE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ZAMIFENACIN CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TOLTERODINE TARTRATE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TROSPIUM CHLORIDE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
MEPENZOLATE BROMIDE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

PMIDs:
None found

Sources:
ChemblInteractions
CLIDINIUM BROMIDE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
TRIDIHEXETHYL CHLORIDE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

PMIDs:
None found

Sources:
ChemblInteractions
CEVIMELINE HYDROCHLORIDE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BETHANECHOL CHLORIDE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M3 agonist

PMIDs:
None found

Sources:
ChemblInteractions
FESOTERODINE FUMARATE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
HEXOCYCLIUM METHYLSULFATE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
GLYCOPYRROLATE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
METHSCOPOLAMINE BROMIDE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ACETYLCHOLINE CHLORIDE CHRM3

Interaction Score: 0.44

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ATROPINE SULFATE CHRM3

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OXYPHENONIUM BROMIDE CHRM3

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
BATEFENTEROL CHRM3

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OXYBUTYNIN CHLORIDE CHRM3

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OXYPHENCYCLIMINE HYDROCHLORIDE CHRM3

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
DICYCLOMINE HYDROCHLORIDE CHRM3

Interaction Score: 0.29

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

PMIDs:
None found

Sources:
ChemblInteractions
PILOCARPINE HYDROCHLORIDE CHRM3

Interaction Score: 0.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M3 agonist

PMIDs:
None found

Sources:
ChemblInteractions
METHACHOLINE CHLORIDE CHRM3

Interaction Score: 0.29

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
METHSCOPOLAMINE CHRM3

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PILOCARPINE CHRM3

Interaction Score: 0.27

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name THVD-201

Mechanism of Interaction Muscarinic acetylcholine receptor M3 agonist

PMIDs:
18824613 19498041

Sources:
TdgClinicalTrial ChemblInteractions
LEVOMEPROMAZINE CHRM3

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
2899826 2870716

Sources:
TdgClinicalTrial TEND
PROPIOMAZINE CHRM3

Interaction Score: 0.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
ISOPROPAMIDE IODIDE CHRM3

Interaction Score: 0.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

PMIDs:
None found

Sources:
ChemblInteractions
PROMAZINE CHRM3

Interaction Score: 0.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
DOXEPIN CHRM3

Interaction Score: 0.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial
CARBACHOL CHRM3

Interaction Score: 0.18

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 agonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PROPANTHELINE BROMIDE CHRM3

Interaction Score: 0.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PIPERTRAMINE CHRM3

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ACECLIDINE CHRM3

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PIPERTRAMINE AMIDE CHRM3

Interaction Score: 0.18

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PROMETHAZINE CHRM3

Interaction Score: 0.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12476402

Sources:
TdgClinicalTrial TEND
DAROTROPIUM BROMIDE CHRM3

Interaction Score: 0.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ACLIDINIUM CHRM3

Interaction Score: 0.18

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Aclidinium

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
THIETHYLPERAZINE CHRM3

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
AFACIFENACIN CHRM3

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ASM-024 CHRM3

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

PMIDs:
None found

Sources:
ChemblInteractions
OLANZAPINE CHRM3

Interaction Score: 0.07

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv

Novel drug target Established target

Trial Name Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

PMIDs:
17848919 10227113 25032030

Sources:
TdgClinicalTrial TEND

Ensembl: ENSG00000133019
- Version: 101_38
Alternate Names:

CHRM3 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P20309
- Version: 11-September-2012
Alternate Names:

1131 Entrez Gene Id

P20309 Uniprot Accession

ACM3_HUMAN Uniprot Id

Gene Info:

Uniprot Status Swiss-Prot

Interpro Acc IPR000276

Interpro Type Family

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TEND: P20309
- Version: 01-August-2011
Alternate Names:

1131 Entrez Gene Id

P20309 Uniprot Accession

ACM3_HUMAN Uniprot Id

Gene Info:

Transmembrane Helix Count 7

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
TdgClinicalTrial: P20309
- Version: January-2014
Alternate Names:

CHRM3 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
RussLampel: ENSG00000133019
- Version: 26-July-2011
Alternate Names:

CHRM3 Display Id

ENSG00000133019 Ensembl Gene Id

MUSCARINIC ACETYLCHOLINE RECEPTOR M3. [SOURCE:UNIPROT/SWISSPROT;ACC:P20309] Description

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
DTC: CHRM3
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Lainé et al., 2009, Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists., J. Med. Chem.
ChemblInteractions: CHRM3
- Version: chembl_23
Alternate Names:

CHRM3 GENE_SYMBOL

Muscarinic acetylcholine receptor M3 UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000133019
- Version: 31-May-2017
Alternate Names:

ENSG00000133019 Gene Symbol

CHRM3 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
dGene: CHRM3
- Version: 27-Jun-2013
Alternate Names:

1131 Gene ID

EGBRS dGene Synonym

HM3 dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: Muscarinic acetylcholine receptor M3
- Version: 2020.06.01
Alternate Names:

CHRM3 TTD Gene Abbreviation

T67684 TTD Target ID

Gene Info:

Publications:

Trial Name	darifenacin,Enablex, Emselex
Novel drug target	Established target

Mechanism of Interaction	Muscarinic acetylcholine receptor M3 antagonist
Direct Interaction	yes

Trial Name	Solifenacin succinate, YM-905,Vesicare
Novel drug target	Established target

Trial Name	fesoterodine fumarate, SPM 907,Toviaz
Novel drug target	Established target

Trial Name	THVD-201
Novel drug target	Established target
Trial Name	tolterodine extended release capsules,Detrol LA

Mechanism of Interaction	Muscarinic acetylcholine receptor M3 agonist
Direct Interaction	yes

Trial Name	Silenor (SO-101)
Novel drug target	Established target

Mechanism of Interaction	Muscarinic acetylcholine receptor antagonist
Direct Interaction	yes

Trial Name	olanzapine,Zyprexa, Zypadhera, Zyprexa Relprevv
Novel drug target	Established target
Trial Name	Olanzapine/fluoxetine combination,Symbyax (Zyprexa/Prozac)

1131	Entrez Gene Id
P20309	Uniprot Accession
ACM3_HUMAN	Uniprot Id

CHRM3	Display Id
ENSG00000133019	Ensembl Gene Id
MUSCARINIC ACETYLCHOLINE RECEPTOR M3. [SOURCE:UNIPROT/SWISSPROT;ACC:P20309]	Description

CHRM3 Gene Record

CHRM3 1131 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name darifenacin,Enablex, Emselex Novel drug target Established target

PMIDs: 19416629 20395537 18046909 11752352

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist Direct Interaction yes

PMIDs: 19317446

Sources: DTC ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist Direct Interaction yes Trial Name SVT-40776

PMIDs: None found

Sources: TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist Direct Interaction yes Trial Name transdermal oxybutynin patch, oxybutynin topical gel,Oxytrol, Kentera, Gelnique

PMIDs: 20590605 19275276 17222678 11752352 16406943 19446545 17016423 17139284 7620236

Sources: TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 11752352 17016423 17139284 18450949

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

PMIDs: 4555460 17016423 17139284

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist Direct Interaction yes

PMIDs: 17016423 17139284 11752352

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Solifenacin succinate, YM-905,Vesicare Novel drug target Established target

PMIDs: 20590605 11752352 19029429 19446545 17016423 17139284

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 1426023 3247303 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 10530931 12185001 17016423 17139284 1863523

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name tiotropium bromide,Spiriva

PMIDs: 11281822 10188785 12582447 11752352

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Direct Interaction yes Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name darifenacin,Enablex, Emselex

Novel drug target Established target

PMIDs:
19416629 20395537 18046909 11752352

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
19317446

Sources:
DTC ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

Trial Name SVT-40776

PMIDs:
None found

Sources:
TdgClinicalTrial ChemblInteractions TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

Trial Name transdermal oxybutynin patch, oxybutynin topical gel,Oxytrol, Kentera, Gelnique

PMIDs:
20590605 19275276 17222678 11752352 16406943 19446545 17016423 17139284 7620236

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
11752352 17016423 17139284 18450949

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

PMIDs:
4555460 17016423 17139284

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
17016423 17139284 11752352

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Solifenacin succinate, YM-905,Vesicare

Novel drug target Established target

PMIDs:
20590605 11752352 19029429 19446545 17016423 17139284

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
1426023 3247303 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
10530931 12185001 17016423 17139284 1863523

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name tiotropium bromide,Spiriva

PMIDs:
11281822 10188785 12582447 11752352

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor M3 antagonist

Direct Interaction yes

PMIDs:
17594079

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name fesoterodine fumarate, SPM 907,Toviaz

Novel drug target Established target