DGIdb - CHRM5 Gene Record

CHRM5 1133 Druggable Genome

Alternate Names:

1133
CHOLINERGIC RECEPTOR MUSCARINIC 5
CHRM5
HM5
118496
1954
ENSG00000184984
OTTHUMG00000129369
Muscarinic acetylcholine receptor M5
MUSCARINIC ACETYLCHOLINE RECEPTOR M5. [SOURCE:UNIPROT/SWISSPROT;ACC:P08912]
ACM5_HUMAN
P08912
T79961

Gene Info:

Human Readable Name	G PROTEIN COUPLED RECEPTOR
Human Readable Name	DRUGGABLE GENOME
Target Subclass	Rhodopsin
Target Main Class	Receptors
Target Subclass	GPCR
Transmembrane Helix Count	7
Target Class	Receptors
Interpro Acc	IPR000276
Interpro Short Name	7TM_GPCR_Rhodpsn
Interpro Type	Family
Uniprot Evidence	2: Evidence at transcript level
Interpro Name	GPCR, rhodopsin-like, 7TM
Uniprot Status	Swiss-Prot
Gene Biotype	PROTEIN_CODING

(6 More Sources)

Gene Categories: Category Details

G PROTEIN COUPLED RECEPTOR
DRUGGABLE GENOME

Publications:

Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
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
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Maruyama et al., 2006, Human muscarinic receptor binding characteristics of antimuscarinic agents to treat overactive bladder., J. Urol.
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.
Irmen M et al., 2018, Characterization of methanthelinium binding and function at human M<sub>1</sub>-M<sub>5</sub> muscarinic acetylcholine receptors., Naunyn Schmiedebergs Arch 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.
Mansfield et al., 2009, Comparison of receptor binding characteristics of commonly used muscarinic antagonists in human bladder detrusor and mucosa., J. Pharmacol. Exp. Ther.
Bridges et al., 2009, 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., J. Med. Chem.
Golembiewski et al., 2002, A systematic approach to the management of postoperative nausea and vomiting., J. Perianesth. Nurs.
Salmon et al., 2013, Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases., 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.

PROPIVERINE CHRM5

Interaction Score: 3.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16406943

Sources:
TTD
CHEMBL523685 CHRM5

Interaction Score: 3.02

Interaction Types & Directionality:

allosteric modulator

Interaction Info:

PMIDs:
19438238

Sources:
DTC
MEBEVERINE CHRM5

Interaction Score: 1.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
HYOSCYAMINE CHRM5

Interaction Score: 1.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
SCOPOLAMINE HYDROBROMIDE CHRM5

Interaction Score: 1.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
EMEPRONIUM CHRM5

Interaction Score: 1.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PRAMIRACETAM CHRM5

Interaction Score: 1.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
UMECLIDINIUM CHRM5

Interaction Score: 1.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
23435542

Sources:
TTD
BELLADONNA CHRM5

Interaction Score: 1.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BUTYLSCOPOLAMINE CHRM5

Interaction Score: 1.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
METHIXENE CHRM5

Interaction Score: 1.51

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND
DAROTROPIUM BROMIDE CHRM5

Interaction Score: 1.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PRIFINIUM CHRM5

Interaction Score: 1.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
METHANTHELINE CHRM5

Interaction Score: 1.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
29938305

Sources:
TTD
ATROPINE CHRM5

Interaction Score: 0.96

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name inhaled atropine

Novel drug target Established target

PMIDs:
7855217 17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND TTD
BENZQUINAMIDE CHRM5

Interaction Score: 0.86

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
TROSPIUM CHRM5

Interaction Score: 0.75

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
BETHANECHOL CHRM5

Interaction Score: 0.75

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CYCLOPENTOLATE CHRM5

Interaction Score: 0.75

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
SOLIFENACIN CHRM5

Interaction Score: 0.6

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Solifenacin succinate, YM-905,Vesicare

Novel drug target Established target

PMIDs:
19029429

Sources:
TdgClinicalTrial
PROMAZINE CHRM5

Interaction Score: 0.53

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND TTD
PSYLLIUM SEED HUSKS CHRM5

Interaction Score: 0.5

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
MEPENZOLATE CHRM5

Interaction Score: 0.5

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
LEVOMEPROMAZINE CHRM5

Interaction Score: 0.43

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
2899826 2870716

Sources:
TdgClinicalTrial TEND
PROPIOMAZINE CHRM5

Interaction Score: 0.43

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
TRIDIHEXETHYL CHRM5

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
FLAVOXATE CHRM5

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PROCYCLIDINE CHRM5

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
OXYPHENCYCLIMINE CHRM5

Interaction Score: 0.38

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
DOXEPIN CHRM5

Interaction Score: 0.34

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial
DAROTROPIUM BROMIDE CHRM5

Interaction Score: 0.3

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PIPERTRAMINE CHRM5

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PROMETHAZINE CHRM5

Interaction Score: 0.3

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12476402

Sources:
TdgClinicalTrial TEND
ACECLIDINE CHRM5

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
ACLIDINIUM CHRM5

Interaction Score: 0.3

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Aclidinium

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
PIPERTRAMINE AMIDE CHRM5

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TOLTERODINE CHRM5

Interaction Score: 0.3

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name tolterodine extended release capsules,Detrol LA

Novel drug target Established target

Trial Name THVD-201

PMIDs:
16406943

Sources:
TdgClinicalTrial
THIETHYLPERAZINE CHRM5

Interaction Score: 0.27

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
AFACIFENACIN CHRM5

Interaction Score: 0.22

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Mechanism of Interaction Muscarinic acetylcholine receptor antagonist

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
PILOCARPINE CHRM5

Interaction Score: 0.12

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

PMIDs:
None found

Sources:
TTD
OLANZAPINE CHRM5

Interaction Score: 0.09

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

Sources:
TdgClinicalTrial TEND

Ensembl: ENSG00000184984
- Version: 101_38
Alternate Names:

CHRM5 Ensembl Gene Name

Gene Info:

Gene Biotype PROTEIN_CODING

Publications:
TdgClinicalTrial: P08912
- Version: January-2014
Alternate Names:

CHRM5 Gene Symbol

Gene Info:

Target Subclass Rhodopsin

Target Class Receptors

Target Subclass GPCR

Publications:
RussLampel: ENSG00000184984
- Version: 26-July-2011
Alternate Names:

MUSCARINIC ACETYLCHOLINE RECEPTOR M5. [SOURCE:UNIPROT/SWISSPROT;ACC:P08912] Description

CHRM5 Display Id

ENSG00000184984 Ensembl Gene Id

Gene Info:

Human Readable Name DRUGGABLE GENOME

Gene Categories:

DRUGGABLE GENOME

Publications:
TEND: P08912
- Version: 01-August-2011
Alternate Names:

ACM5_HUMAN Uniprot Id

ENSG00000184984 Ensembl Gene Id

P08912 Uniprot Accession

Gene Info:

Target Subclass Rhodopsin

Target Main Class Receptors

Target Subclass GPCR

Publications:
HopkinsGroom: P08912
- Version: 11-September-2012
Alternate Names:

CHRM5 Uniprot Gene Name

ENSG00000184984 Ensembl Gene Id

ACM5_HUMAN Uniprot Id

Gene Info:

Interpro Acc IPR000276

Human Readable Name G PROTEIN COUPLED RECEPTOR

Interpro Short Name 7TM_GPCR_Rhodpsn

Gene Categories:

G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

Publications:

DTC: CHRM5

Version: 02-September-2020

Alternate Names:

Gene Info:

Publications:

Bridges et al., 2009, 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., J. Med. Chem.

ChemblInteractions: CHRM5
- Version: chembl_23
Alternate Names:

CHRM5 GENE_SYMBOL

Muscarinic acetylcholine receptor M5 UNIPROT

Gene Info:

Publications:
HingoraniCasas: ENSG00000184984
- Version: 31-May-2017
Alternate Names:

ENSG00000184984 Gene Symbol

CHRM5 Ensembl Id

Gene Info:

Gene Categories:

DRUGGABLE GENOME

Publications:
dGene: CHRM5
- Version: 27-Jun-2013
Alternate Names:

1133 Gene ID

HM5 dGene Synonym

Gene Info:

Gene Categories:

G PROTEIN COUPLED RECEPTOR

Publications:
TTD: Muscarinic acetylcholine receptor M5
- Version: 2020.06.01
Alternate Names:

CHRM5 TTD Gene Abbreviation

T79961 TTD Target ID

Gene Info:

Publications:

Trial Name	inhaled atropine
Novel drug target	Established target

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

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

Mechanism of Interaction	Muscarinic acetylcholine receptor antagonist
Direct Interaction	yes

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

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

MUSCARINIC ACETYLCHOLINE RECEPTOR M5. [SOURCE:UNIPROT/SWISSPROT;ACC:P08912]	Description
CHRM5	Display Id
ENSG00000184984	Ensembl Gene Id

ACM5_HUMAN	Uniprot Id
ENSG00000184984	Ensembl Gene Id
P08912	Uniprot Accession

CHRM5	Uniprot Gene Name
ENSG00000184984	Ensembl Gene Id
ACM5_HUMAN	Uniprot Id

CHRM5 Gene Record

CHRM5 1133 Druggable Genome

Alternate Names:

Gene Info:

Gene Categories: Category Details

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16406943

Sources: TTD

Interaction Types & Directionality: allosteric modulator

Interaction Info:

PMIDs: 19438238

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 23435542

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 17016423 17139284 11752352

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 29938305

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

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

PMIDs: 7855217 17016423 17139284 11752352

Sources: TdgClinicalTrial TEND TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

Interaction Types & Directionality:

n/a

PMIDs:
16406943

Sources:
TTD

Interaction Types & Directionality:

allosteric modulator

PMIDs:
19438238

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
23435542

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
29938305

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name inhaled atropine

Novel drug target Established target

PMIDs:
7855217 17016423 17139284 11752352

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

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 11752352

Sources:
TdgClinicalTrial TEND TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
2899826 2870716

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -