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TargetMuscarinic acetylcholine receptor M2
LigandBDBM50296329
Substrate/Competitorn/a
Meas. Tech.ChEMBL_581961
IC50 0.18±n/a nM
Citation Prat MFernández DBuil MACrespo MICasals GFerrer MTort LCastro JMonleón JMGavaldà AMiralpeix MRamos IDoménech TVilella DAntón FHuerta JMEspinosa SLópez MSentellas SGonzález MAlbertí JSegarra VCárdenas ABeleta JRyder H Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinol esters as potent and long-acting muscarinic antagonists with potential for minimal systemic exposure after inhaled administration: identification of (3R)-3-{[hydroxy(di-2-thienyl)acetyl]oxy}-1-(3-phenoxypropyl)-1-azoniabicyclo J Med Chem 52:5076-92 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Muscarinic acetylcholine receptor M2
Name:Muscarinic acetylcholine receptor M2 and M5
Synonyms:CHRM2 | Cholinergic, muscarinic M2 | RecName: Full=Muscarinic acetylcholine receptor M2
Type:GPCR
Mol. Mass.:51730.61
Organism:Homo sapiens (Human)
Description:P08172
Residue:466
Sequence:
MNNSTNSSNNSLALTSPYKTFEVVFIVLVAGSLSLVTIIGNILVMVSIKVNRHLQTVNNY
FLFSLACADLIIGVFSMNLYTLYTVIGYWPLGPVVCDLWLALDYVVSNASVMNLLIISFD
RYFCVTKPLTYPVKRTTKMAGMMIAAAWVLSFILWAPAILFWQFIVGVRTVEDGECYIQF
FSNAAVTFGTAIAAFYLPVIIMTVLYWHISRASKSRIKKDKKEPVANQDPVSPSLVQGRI
VKPNNNNMPSSDDGLEHNKIQNGKAPRDPVTENCVQGEEKESSNDSTSVSAVASNMRDDE
ITQDENTVSTSLGHSKDENSKQTCIRIGTKTPKSDSCTPTNTTVEVVGSSGQNGDEKQNI
VARKIVKMTKQPAKKKPPPSREKKVTRTILAILLAFIITWAPYNVMVLINTFCAPCIPNT
VWTIGYWLCYINSTINPACYALCNATFKKTFKHLLMCHYKNIGATR
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  Blast E-value cutoff:
BDBM50296329
n/a
NameBDBM50296329
Synonyms:(3R)-3-{[Hydroxy(di-2-thienyl)acetyl]oxy}-1-(2-phenylethyl)-1-azoniabicyclo[2.2.2]octane bromide | CHEMBL564057 | US9333195, 36 | US9687478, 36
TypeSmall organic molecule
Emp. Form.C25H28NO3S2
Mol. Mass.454.624
SMILESOC(C(=O)O[C@H]1C[N+]2(CCc3ccccc3)CCC1CC2)(c1cccs1)c1cccs1 |r,wD:5.4,(12.26,-17.08,;11.17,-18.17,;12.51,-18.94,;12.51,-20.48,;13.84,-18.17,;15.17,-18.93,;15.17,-20.47,;16.5,-21.23,;16.49,-22.77,;17.82,-23.56,;19.16,-22.8,;20.48,-23.59,;21.82,-22.83,;21.84,-21.29,;20.5,-20.51,;19.17,-21.27,;17.83,-20.47,;17.83,-18.93,;16.5,-18.15,;16.92,-19.4,;15.87,-19.75,;11.17,-16.63,;9.92,-15.73,;10.39,-14.26,;11.93,-14.26,;12.41,-15.72,;9.84,-18.95,;8.42,-18.32,;7.4,-19.47,;8.17,-20.8,;9.68,-20.48,)|
Structure
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