Details of the Target

General Information of Target

Target ID LDTP03045
Target Name Muscarinic acetylcholine receptor M3 (CHRM3)
Gene Name CHRM3
Gene ID 1131
Synonyms
Muscarinic acetylcholine receptor M3
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MTLHNNSTTSPLFPNISSSWIHSPSDAGLPPGTVTHFGSYNVSRAAGNFSSPDGTTDDPL
GGHTVWQVVFIAFLTGILALVTIIGNILVIVSFKVNKQLKTVNNYFLLSLACADLIIGVI
SMNLFTTYIIMNRWALGNLACDLWLAIDYVASNASVMNLLVISFDRYFSITRPLTYRAKR
TTKRAGVMIGLAWVISFVLWAPAILFWQYFVGKRTVPPGECFIQFLSEPTITFGTAIAAF
YMPVTIMTILYWRIYKETEKRTKELAGLQASGTEAETENFVHPTGSSRSCSSYELQQQSM
KRSNRRKYGRCHFWFTTKSWKPSSEQMDQDHSSSDSWNNNDAAASLENSASSDEEDIGSE
TRAIYSIVLKLPGHSTILNSTKLPSSDNLQVPEEELGMVDLERKADKLQAQKSVDDGGSF
PKSFSKLPIQLESAVDTAKTSDVNSSVGKSTATLPLSFKEATLAKRFALKTRSQITKRKR
MSLVKEKKAAQTLSAILLAFIITWTPYNIMVLVNTFCDSCIPKTFWNLGYWLCYINSTVN
PVCYALCNKTFRTTFKMLLLCQCDKKKRRKQQYQQRQSVIFHKRAPEQAL
Target Type
Successful
Target Bioclass
GPCR
Family
G-protein coupled receptor 1 family, Muscarinic acetylcholine receptor subfamily, CHRM3 sub-subfamily
Subcellular location
Cell membrane
Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is Pi turnover.
TTD ID
T67684
Uniprot ID
P20309
DrugMap ID
TTQ13Z5
Ensemble ID
ENST00000255380.8
HGNC ID
HGNC:1952
ChEMBL ID
CHEMBL245

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 1 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FBPP2
 Probe Info  		4.98  LDD0318  [1]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Sodium leak channel NALCN (NALCN) NALCN family Q8IZF0
GPCR
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Muscarinic acetylcholine receptor M5 (CHRM5) G-protein coupled receptor 1 family P08912

The Drug(s) Related To This Target

Approved
Click To Hide/Show 85 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Aceclidine Small molecular drug D0R7WU
Acetylcholine Small molecular drug DB03128
Aclidinium Small molecular drug DB08897
Amitriptyline Small molecular drug DB00321
Amoxapine Small molecular drug DB00543
Anisotropine Methylbromide Small molecular drug DB00517
Aripiprazole Small molecular drug DB01238
Atropine Small molecular drug DB00572
Bethanechol Small molecular drug DB01019
Brompheniramine Small molecular drug DB00835
Butylscopolamine Small molecular drug DB09300
Carbamoylcholine Small molecular drug DB00411
Cevimeline Small molecular drug D0Q4CS
Chlorpromazine Small molecular drug DB00477
Chlorprothixene Small molecular drug DB01239
Cinnarizine Small molecular drug DB00568
Clozapine Small molecular drug DB00363
Cyproheptadine Small molecular drug DB00434
Darifenacin Small molecular drug D0Y5AM
Desipramine Small molecular drug DB01151
Dicyclomine Small molecular drug DB00804
Diphenidol Small molecular drug DB01231
Disopyramide Small molecular drug DB00280
Doxepin Small molecular drug DB01142
Doxylamine Small molecular drug DB00366
Fesoterodine Small molecular drug DB06702
Glycopyrronium Small molecular drug DB00986
Haloperidol Small molecular drug DB00502
Hexocyclium Small molecular drug DB06787
Homatropine Methylbromide Small molecular drug DB00725
Hyoscyamine Small molecular drug DB00424
Imipramine Small molecular drug DB00458
Ipratropium Small molecular drug D0S0AS
Isopropamide Small molecular drug DB01625
Ketamine Small molecular drug DB01221
Las-34273 Small molecular drug D07KHH
Loxapine Small molecular drug DB00408
Maprotiline Small molecular drug DB00934
Mepenzolate Small molecular drug DB04843
Meperidine Small molecular drug DB00454
Methacholine Small molecular drug DB06709
Methacholine Chloride Small molecular drug D04MWJ
Methantheline Small molecular drug DB00940
Methotrimeprazine Small molecular drug DB01403
Methscopolamine Bromide Small molecular drug D04LHJ
Methscopolamine Bromide Small molecular drug DB00462
Methylscopolamine Small molecular drug D0M6VK
Mivacurium Small molecular drug DB01226
Nicardipine Small molecular drug DB00622
Nortriptyline Small molecular drug DB00540
Olanzapine Small molecular drug DB00334
Oxybutynin Small molecular drug DB01062
Oxyphencyclimine Small molecular drug DB00383
Pancuronium Small molecular drug DB01337
Paroxetine Small molecular drug DB00715
Pilocarpine Small molecular drug DB01085
Pipecuronium Small molecular drug DB01338
Pizotifen Small molecular drug DB06153
Procyclidine Small molecular drug DB00387
Promethazine Small molecular drug DB01069
Propiomazine Small molecular drug DB00777
Propiverine Small molecular drug DB12278
Quetiapine Small molecular drug DB01224
Scopolamine Small molecular drug DB00747
Solifenacin Small molecular drug D0L4YD
Succinylcholine Small molecular drug D0Q7ZQ
Terfenadine Small molecular drug DB00342
Thiopental Small molecular drug DB00599
Tiotropium Small molecular drug D0P1WA
Tolterodine Small molecular drug D0BZ7W
Tramadol Small molecular drug DB00193
Trihexyphenidyl Small molecular drug DB00376
Trimebutine Small molecular drug DB09089
Trimipramine Small molecular drug DB00726
Tropicamide Small molecular drug DB00809
Trospium Small molecular drug DB00209
Umeclidinium Small molecular drug DB09076
Ziprasidone Small molecular drug DB00246
Aripiprazole Lauroxil . DB14185
Diphemanil . DB13720
Dosulepin . DB09167
Homatropine . DB11181
Smt-d002 . D05KZK
Thonzylamine . DB11235
Viloxazine . DB09185
Phase 2
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tarafenacin Small molecular drug D04YEW
Trn-157 . D02TXV
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Chf 5407 . D0V0JQ
Investigative
Click To Hide/Show 76 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
1'-benzyl-3-phenyl-[3,4bipiperidinyl-2,6-dione Small molecular drug D05EML
1,1-diphenyl-2-(3-tropanyl)Ethanol Small molecular drug D00JTE
1-methyl-1-(4-pyrrolidin-1-yl-but-2-ynyl)-urea Small molecular drug D02PFJ
2,8-dimethyl-1-oxa-8-aza-spiro[4.5]Decan-3-one Small molecular drug D05MDY
2-methyl-6-pyrrolidin-1-yl-hex-4-ynal Oxime Small molecular drug D0U2IL
3-(3-benzylamino)-piperidin-2-one Small molecular drug D07DEY
3-methyl-7-pyrrolidin-1-yl-hept-5-yn-2-one Small molecular drug D06VST
3-tetrazol-2-yl-1-aza-bicyclo[2.2.2]Octane Small molecular drug D0OE0K
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one Small molecular drug D0T2RY
4-damp Small molecular drug D0A2KT
6-dimethylamino-2-methyl-hex-4-ynal Oxime Small molecular drug D08ZTA
7-dimethylamino-3-methyl-hept-5-yn-2-one Small molecular drug D0QL1X
7-dimethylamino-hept-5-yn-2-one Small molecular drug D0R8FS
7-pyrrolidin-1-yl-hept-5-yn-2-one Small molecular drug D0B8AQ
A-987306 Small molecular drug D0F9QT
Acetic Acid 8-aza-bicyclo[3.2.1]Oct-6-yl Ester Small molecular drug D01UDC
Arecaidine Propargyl Ester Small molecular drug D0I9LU
Arecoline Small molecular drug DB04365
Benzoic Acid 8-aza-bicyclo[3.2.1]Oct-6-yl Ester Small molecular drug D0C9ZE
Brl-55473 Small molecular drug D07VZG
Brucine Small molecular drug D0H2UT
Cremastrine Small molecular drug D0Z5RQ
Dau-5750 Small molecular drug D05EEV
Flumezapine Small molecular drug D0HV3A
Fm1-10 Small molecular drug D06IUC
Fm1-43 Small molecular drug D0AR0H
Furtrethonium Small molecular drug D0PL0Y
Gnf-pf-5618 Small molecular drug D02EXX
Go7874 Small molecular drug D07OAK
Guanylpirenzepine Small molecular drug D0I9AL
Hexahydrodifenidol Small molecular drug D0W8XI
Hexahydrosiladifenidol Small molecular drug D07LDP
Isoclozapine Small molecular drug D0P0IX
Isoloxapine Small molecular drug D0Q2GP
J-104135 Small molecular drug D0BP7C
Lithocholylcholine Small molecular drug D03DMR
Mcn-a-343 Small molecular drug D02BOW
Methylfurmethide Small molecular drug D0WO3A
Ml381 Small molecular drug D00WNA
N-(4-dimethylamino-but-2-ynyl)-n-methyl-acetamide Small molecular drug D0C9VH
N-benzyl Brucine Small molecular drug D08KNP
N-chloromethyl-brucine Small molecular drug D08BGK
N-methoxyquinuclidine-3-carboximidoyl Chloride Small molecular drug D0R2JE
N-methoxyquinuclidine-3-carboximidoyl Fluoride Small molecular drug D0X2JU
Nnc 11-1314 Small molecular drug D02MJE
Nnc 11-1585 Small molecular drug D07CAB
Nnc 11-1607 Small molecular drug D08XBQ
Nocardimicin A Small molecular drug D09YBC
Nocardimicin C Small molecular drug D05YBO
Nocardimicin D Small molecular drug D0I2XG
Nocardimicin F Small molecular drug D0J4DJ
Noccardimicin E Small molecular drug D07QGQ
Olterodine Small molecular drug D07TDE
Oxybutynine Small molecular drug D0F5LH
P-f-hhsid Small molecular drug D0K3VR
Pentylthio-tztp Small molecular drug D0T6ID
Propionic Acid 8-aza-bicyclo[3.2.1]Oct-6-yl Ester Small molecular drug D04XNH
Ptac Small molecular drug D09AAZ
Silahexocyclium Small molecular drug D00NRJ
Sulfoarecoline Small molecular drug D0O1BN
Thiochrome Small molecular drug D05WXF
Tripitramine Small molecular drug D07GPQ
Ucb-101333-3 Small molecular drug D02ZPV
Uh-ah 37 Small molecular drug D03LSH
Vinburnine Small molecular drug D0S4DT
Vu0255035 Small molecular drug D02UNX
Win 51,708 Small molecular drug D05PSD
Win 62,577 Small molecular drug D02IIN
[3h]Oxotremorine-m Small molecular drug D0G4CG
[3h]Qnb Small molecular drug D02VGM
3-(1-carbamoyl-1,1-diphenylmethyl)-1-(4-methoxyphenylethyl)Pyrrolidine (App) . D06UOE
Ae-9c90cb . D0IM7C
Alks 27 . DB05752
Dau-5884 . D0R8AZ
Imidafenacin . DB09262
Rociverine . DB13581
Discontinued
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Alvameline Small molecular drug D0X8MZ
Benzquinamide Small molecular drug DB00767
Revatropate Small molecular drug D09LMX
Tridihexethyl Small molecular drug DB00505
Zamifenacin Small molecular drug D04SBH
Etoperidone . DB09194
Psd-506 . D06GCP

References

1 Tranylcypromine specificity for monoamine oxidase is limited by promiscuous protein labelling and lysosomal trapping. RSC Chem Biol. 2020 Aug 12;1(4):209-213. doi: 10.1039/d0cb00048e. eCollection 2020 Oct 1.
Mass spectrometry data entry: PXD018580