DGIdb - CHRM4 Gene Record

CHRM4 1132 Druggable Genome

Alternate Names:

1132
CHOLINERGIC RECEPTOR MUSCARINIC 4
CHRM4
HM4
M4R
118495
1953
ENSG00000180720
OTTHUMG00000154371
P08173
ACM4_HUMAN
Muscarinic acetylcholine receptor M4
T20709

Gene Info:

Target Subclass	Rhodopsin
Target Class	Receptors
Target Subclass	GPCR
Target Main Class	Receptors
Transmembrane Helix Count	6
Human Readable Name	G PROTEIN COUPLED RECEPTOR
Interpro Short Name	7TM_GPCR_Rhodpsn
Human Readable Name	DRUGGABLE GENOME
Interpro Acc	IPR000276
Uniprot Evidence	1: Evidence at protein level
Uniprot Status	Swiss-Prot
Interpro Type	Family
Interpro Name	GPCR, rhodopsin-like, 7TM
Gene Biotype	PROTEIN_CODING

(5 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Mansfield et al., 2009, Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa., J. Pharmacol. Exp. Ther.
Maruyama et al., 2006, Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder., J. Urol.
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
Golembiewski et al., 2002, A systematic approach to the management of postoperative nausea and vomiting., J. Perianesth. Nurs.
Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
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.)
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Shirey JK et al., 2008, An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission., Nat Chem Biol
Waelbroeck et al., 1992, Stereoselective interaction of procyclidine, hexahydro-difenidol, hexbutinol and oxyphencyclimine, and of related antagonists, with four muscarinic receptors., Eur. J. Pharmacol.
Waelbroeck et al., 1990, Stereoselectivity of procyclidine binding to muscarinic receptor subtypes M1, M2 and M4., Eur. J. Pharmacol.
Myhrer, 2010, Identification of neuronal target areas for nerve agents and specification of receptors for pharmacological treatment., Neurotoxicology
Alberts, 1995, Classification of the presynaptic muscarinic receptor subtype that regulates 3H-acetylcholine secretion in the guinea pig urinary bladder in vitro., J. Pharmacol. Exp. Ther.
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.
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.
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

TROPICAMIDE CHRM4

Interaction Score: 9.84

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17594079 17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND TTD
PROCYCLIDINE CHRM4

Interaction Score: 5.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
1426023 2253700 20624420 7616431 17016423 17139284

Sources:
TdgClinicalTrial TEND
CHEMBL1212994 CHRM4

Interaction Score: 5.62

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18059262

Sources:
DTC
METHIXENE CHRM4

Interaction Score: 2.25

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
BENZQUINAMIDE CHRM4

Interaction Score: 1.61

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
ATROPINE CHRM4

Interaction Score: 1.28

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name inhaled atropine

PMIDs:
7855217 17016423 17139284

Sources:
TdgClinicalTrial TEND
SOLIFENACIN CHRM4

Interaction Score: 1.12

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Solifenacin succinate, YM-905,Vesicare

Novel drug target Established target

PMIDs:
19029429

Sources:
TdgClinicalTrial
PROPIOMAZINE CHRM4

Interaction Score: 0.8

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
LEVOMEPROMAZINE CHRM4

Interaction Score: 0.8

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2899826 2870716

Sources:
TdgClinicalTrial TEND
PROMAZINE CHRM4

Interaction Score: 0.66

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
DOXEPIN CHRM4

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial
DIPHENIDOL CHRM4

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PIPERTRAMINE CHRM4

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ACLIDINIUM CHRM4

Interaction Score: 0.56

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Aclidinium

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
ACECLIDINE CHRM4

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
DAROTROPIUM BROMIDE CHRM4

Interaction Score: 0.56

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions
PROMETHAZINE CHRM4

Interaction Score: 0.56

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
12476402

Sources:
TdgClinicalTrial TEND
PIPERTRAMINE AMIDE CHRM4

Interaction Score: 0.56

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TOLTERODINE CHRM4

Interaction Score: 0.56

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:
16406943

Sources:
TdgClinicalTrial
THIETHYLPERAZINE CHRM4

Interaction Score: 0.51

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
AFACIFENACIN CHRM4

Interaction Score: 0.4

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
OLANZAPINE CHRM4

Interaction Score: 0.21

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: ENSG00000180720
- Version: 101_38
Alternate Names:

CHRM4 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
HopkinsGroom: P08173
- Version: 11-September-2012
Alternate Names:

P08173 Uniprot Accession

MUSCARINIC ACETYLCHOLINE RECEPTOR M4 Uniprot Protein Name

ENSG00000180720 Ensembl Gene Id

Gene Info:

Interpro Short Name 7TM_GPCR_Rhodpsn

Human Readable Name DRUGGABLE GENOME

Interpro Acc IPR000276

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:
TEND: P08173
- Version: 01-August-2011
Alternate Names:

ENSG00000180720 Ensembl Gene Id

P08173 Uniprot Accession

1132 Entrez Gene Id

Gene Info:

Target Main Class Receptors

Target Subclass Rhodopsin

Target Subclass GPCR

Publications:
TdgClinicalTrial: P08173
- Version: January-2014
Alternate Names:

CHRM4 Gene Symbol

Gene Info:

Target Class Receptors

Target Subclass GPCR

Target Subclass Rhodopsin

Publications:
DTC: CHRM4
- Version: 02-September-2020
Alternate Names:

Gene Info:

Publications:

Shirey JK et al., 2008, An allosteric potentiator of M4 mAChR modulates hippocampal synaptic transmission., Nat Chem Biol
HingoraniCasas: ENSG00000180720
- Version: 31-May-2017
Alternate Names:

ENSG00000180720 Gene Symbol

CHRM4 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
ChemblInteractions: CHRM4
- Version: chembl_23
Alternate Names:

CHRM4 GENE_SYMBOL

Muscarinic acetylcholine receptor M4 UNIPROT

Gene Info:

Publications:
dGene: CHRM4
- Version: 27-Jun-2013
Alternate Names:

1132 Gene ID

HM4 dGene Synonym

M4R dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: Muscarinic acetylcholine receptor M4
- Version: 2020.06.01
Alternate Names:

CHRM4 TTD Gene Abbreviation

T20709 TTD Target ID

Gene Info:

Publications:

Novel drug target	Established target
Trial Name	inhaled atropine

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

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

Direct Interaction	yes
Mechanism of Interaction	Muscarinic acetylcholine receptor antagonist

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

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

P08173	Uniprot Accession
MUSCARINIC ACETYLCHOLINE RECEPTOR M4	Uniprot Protein Name
ENSG00000180720	Ensembl Gene Id

CHRM4 Gene Record

CHRM4 1132 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17594079 17016423 17139284 11752352

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 1426023 2253700 20624420 7616431 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18059262

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name inhaled atropine

PMIDs: 7855217 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 19029429

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 2899826 2870716

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 7855217 2141000 2329499

Sources: TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Aclidinium Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 12476402

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

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

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17594079 17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
1426023 2253700 20624420 7616431 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
18059262

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name inhaled atropine

PMIDs:
7855217 17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Solifenacin succinate, YM-905,Vesicare

Novel drug target Established target

PMIDs:
19029429

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
2899826 2870716

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Aclidinium

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction Muscarinic acetylcholine receptor antagonist

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
12476402

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

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:
16406943

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

antagonist (inhibitory)