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GPCR

Name	Muscarinic acetylcholine receptor M4
Species	Homo sapiens (Human)
Gene	CHRM4
Synonym	HM3 M4 receptor cholinergic receptor Chrm-4 cholinergic receptor, muscarinic 4
Disease	Produce mydriasis and cycloplegia for diagnostic purposes Hypertension Irritable bowel syndrome Moderate and severe psychomotor agitation Mydriasis diagnosis Nausea; Vomiting; Emesis Organophosphate poisoning Overactive bladder disorder; Spasm Parkinson's disease Urinary retention Peptic ulcer Peptic ulcer disease; Irritable bowel syndrome; Pancreatitis; Gastritis Solid tumours Peptic ulcer; Gastrointestinal disease Peptic ulcer; Uveitis Glaucoma Gastrointestinal disease Bronchodilator Poison intoxication Chronic obstructive pulmonary disease Cough Central and peripheral nervous diseases Depression Alzheimer disease Dysuria; Urgency; Nocturia; Suprapubic pain Gastric motility disorder; Spasm Acquired nystagmus [ Show all ]
Length	479
Amino acid sequence	MANFTPVNGSSGNQSVRLVTSSSHNRYETVEMVFIATVTGSLSLVTVVGNILVMLSIKVNRQLQTVNNYFLFSLACADLIIGAFSMNLYTVYIIKGYWPLGAVVCDLWLALDYVVSNASVMNLLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTVPDNQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAKTLAFLKSPLMKQSVKKPPPGEAAREELRNGKLEEAPPPALPPPPRPVADKDTSNESSSGSATQNTKERPATELSTTEATTPAMPAPPLQPRALNPASRWSKIQIVTKQTGNECVTAIEIVPATPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMVLVNTFCQSCIPDTVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
UniProt	P08173
Protein Data Bank	5dsg
GPCR-HGmod model	P08173
3D structure model	This structure is from PDB ID 5dsg.
BioLiP	BL0339919,BL0339921, BL0339920
Therapeutic Target Database	T20709, T50918
ChEMBL	CHEMBL1821
IUPHAR	16
DrugBank	BE0000405

Ligand

Name	biperiden
Molecular formula	C21H29NO
IUPAC name	1-(2-bicyclo[2.2.1]hept-5-enyl)-1-phenyl-3-piperidin-1-ylpropan-1-ol
Molecular weight	311.469
Hydrogen bond acceptor	2
Hydrogen bond donor	1
XlogP	4.3
Synonyms	D0B4TN HY-13204A .alpha.-5-Norbornen-2-yl-.alpha.-phenyl-1-piperidinepropanol NCIOpen2_009564 1-Piperidinepropanol, .alpha.-5-norbornen-2-yl-.alpha.-phenyl- Prestwick2_000502 3-Piperidino-1-phenyl-1-bicyclo(2.2.1)hepten-(5)-yl-propanol-(1) [German] VA10409 AC1L1DJT alpha-Bicyclo(2.2.1)hept-5-en-2-yl-alpha-phenyl-1-piperidinepropanol Biperidene BRD-A00546892-001-01-8 DTXSID6022680 LS-116068 1-(5-bicyclo[2.2.1]hept-2-enyl)-1-phenyl-3-piperidin-1-ylpropan-1-ol PDSP1_000821 1-PIPERIDINEPROPANOL, alpha-5-NORBORNEN-2-YL-alpha-PHENYL- SCHEMBL34957 5-Norbornene-2-methanol, .alpha.-phenyl-.alpha.-(2-piperidinoethyl)- Akinophyl AX8116739 Biperiden hydrochloride Biperideno CCG-213474 HMS2093N17 NCGC00182965-03 1-Bicycloheptenyl-1-phenyl-3-piperidino-propanol-1 Prestwick0_000502 1235-82-1 (hydrochloride) SR-05000001649-1 514-65-8 alpha-(Bicyclo(2.2.1)hept-5-en-2-yl)-alpha-phenyl-1-piperidino propanol Bicyclo[2.2.1]hept-5-ene-2-methanol, .alpha.-phenyl-.alpha.-[2-(1-piperidinyl)ethyl]- Biperiden [USAN:INN:BAN:JAN] Biperidenum [INN-Latin] CS-1797 KL 373 0FRP6G56LD NSC-759145 1-Piperidinepropanol, .alpha.-bicyclo[2.2.1]hept-5-en-2-yl-.alpha.-phenyl- SBI-0206797.P001 3-Piperidino-1-phenyl-1-bicycloheptenyl-1-propanol YSXKPIUOCJLQIE-UHFFFAOYSA-N Akineton alpha-bicyclo[2.2.1]hept-5-en-2-yl-alpha-phenyl-1-piperidinepropanol Biperiden (JAN/USP/INN) Biperidene hydrochloride BRN 0290038 EINECS 208-184-6 NCGC00182965-01 1-(Bicyclo(2.2.1)hept-5-en-2alpha-yl)-1-phenyl-3-piperidinopropanol PDSP2_000808 1-Piperidinepropanol, alpha-bicyclo(2.2.1)hept-5-en-2-yl-alpha-phenyl- SPBio_002344 5-Norbornene-2-methanol, alpha-phenyl-alpha-(2-piperidinoethyl)- Akinophyl (Salt/Mix) BDBM50240680 Biperiden lactate Biperideno [INN-Spanish] CHEBI:3112 HSDB 7639 .alpha.-(Bicyclo(2.2.1)hept-5-en-2-yl)-.alpha.-phenyl-1-piperidino propanol NCGC00182965-04 1-Bicyclo[2.2.1]hept-5-en-2-yl-1-phenyl-3-(1-piperidinyl)-1-propanol # Prestwick1_000502 3-Piperidino-1-phenyl-1-bicyclo(2.2.1)hepten-(5)-yl-propanol-(1) UNII-0FRP6G56LD alpha-5-Norbornen-2-yl-alpha-phenyl-1-piperidinepropanol Bipariden Biperiden [USP:INN:BAN:JAN] Biperidine D00779 DB00810 L001222 1-(5-bicyclo[2.2.1]hept-2-enyl)-1-phenyl-3-(1-piperidyl)propan-1-ol NSC759145 1-Piperidinepropanol, .alpha.-bicyclo[2.2.1]hept-5-en-2-yl-.alpha.-phenyl-, hydrochloride SCHEMBL20229360 5-20-02-00242 (Beilstein Handbook Reference) Akineton (TN) AN-45471 Biperiden HCl Biperidene [INN-French] C07941 GTPL7128 NCGC00182965-02 1-(bicyclo[2.2.1]hept-5-en-2-yl)-1-phenyl-3-(piperidin-1-yl)propan-1-ol Pharmakon1600-01505514 1-{bicyclo[2.2.1]hept-5-en-2-yl}-1-phenyl-3-(piperidin-1-yl)propan-1-ol SR-05000001649 AKOS016008819 Beperiden Biperiden [USAN:BAN:INN:JAN] Biperidenum CHEMBL1101 [ Show all ]
Inchi Key	YSXKPIUOCJLQIE-UHFFFAOYSA-N
Inchi ID	InChI=1S/C21H29NO/c23-21(19-7-3-1-4-8-19,11-14-22-12-5-2-6-13-22)20-16-17-9-10-18(20)15-17/h1,3-4,7-10,17-18,20,23H,2,5-6,11-16H2
PubChem CID	2381
ChEMBL	N/A
IUPHAR	7128
BindingDB	50240680
DrugBank	DB00810
Structure SDF download
Lipinski's druglikeness	This ligand satisfies Lipinski's rule of five.

Experimental Data

Parameter	Value	Reference	Database source
Kd	2.4 nM	PMID1346637	IUPHAR
Ki	2.4 nM	PMID1346637	PDSP,BindingDB

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