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Name | Muscarinic acetylcholine receptor M2 |
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Species | Homo sapiens (Human) |
Gene | CHRM2 |
Synonym | cholinergic receptor AChR M2 M2 muscarinic acetylcholine receptor M2 receptor Chrm-2 [ Show all ] |
Disease | Urinary incontinence Heart failure Nausea; Addiction Parkinson's disease Peptic ulcer [ Show all ] |
Length | 466 |
Amino acid sequence | MNNSTNSSNNSLALTSPYKTFEVVFIVLVAGSLSLVTIIGNILVMVSIKVNRHLQTVNNYFLFSLACADLIIGVFSMNLYTLYTVIGYWPLGPVVCDLWLALDYVVSNASVMNLLIISFDRYFCVTKPLTYPVKRTTKMAGMMIAAAWVLSFILWAPAILFWQFIVGVRTVEDGECYIQFFSNAAVTFGTAIAAFYLPVIIMTVLYWHISRASKSRIKKDKKEPVANQDPVSPSLVQGRIVKPNNNNMPSSDDGLEHNKIQNGKAPRDPVTENCVQGEEKESSNDSTSVSAVASNMRDDEITQDENTVSTSLGHSKDENSKQTCIRIGTKTPKSDSCTPTNTTVEVVGSSGQNGDEKQNIVARKIVKMTKQPAKKKPPPSREKKVTRTILAILLAFIITWAPYNVMVLINTFCAPCIPNTVWTIGYWLCYINSTINPACYALCNATFKKTFKHLLMCHYKNIGATR |
UniProt | P08172 |
Protein Data Bank | 5zkc, 4mqs, 4mqt, 5yc8, 5zk3, 5zkb, 5zk8 |
GPCR-HGmod model | P08172 |
3D structure model | This structure is from PDB ID 5zkc. |
BioLiP | BL0433341, BL0433216, BL0263147, BL0263146, BL0263145, BL0433339, BL0433340, BL0433338 |
Therapeutic Target Database | T46185 |
ChEMBL | CHEMBL211 |
IUPHAR | 14 |
DrugBank | BE0000560 |
Name | Oxotremorine |
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Molecular formula | C12H18N2O |
IUPAC name | 1-(4-pyrrolidin-1-ylbut-2-ynyl)pyrrolidin-2-one |
Molecular weight | 206.289 |
Hydrogen bond acceptor | 2 |
Hydrogen bond donor | 0 |
XlogP | 0.4 |
Synonyms | CHEMBL7634 FT-0631303 KBio2_001928 KBioSS_001928 NCGC00015773-02 [ Show all ] |
Inchi Key | RSDOPYMFZBJHRL-UHFFFAOYSA-N |
Inchi ID | InChI=1S/C12H18N2O/c15-12-6-5-11-14(12)10-4-3-9-13-7-1-2-8-13/h1-2,5-11H2 |
PubChem CID | 4630 |
ChEMBL | CHEMBL7634 |
IUPHAR | 302 |
BindingDB | 50004665 |
DrugBank | N/A |
Structure | |
Lipinski's druglikeness | This ligand satisfies Lipinski's rule of five. |
Parameter | Value | Reference | Database source |
---|---|---|---|
EC50 | 19.0 nM | PMID7783150 | BindingDB,ChEMBL |
Efficacy | 112.8 % | PMID25765911 | ChEMBL |
IC50 | 400.0 nM | PMID9438027 | BindingDB,ChEMBL |
Ki | 17.0 nM | PMID10891110 | BindingDB,ChEMBL |
Ki | 235.0 nM | PMID9454790 | PDSP,BindingDB |
Ki | 251.189 - 10000.0 nM | PMID9224827, PMID9454790 | IUPHAR |
Ki | 323.59 nM | PMID18182302 | ChEMBL |
Ki | 660.0 nM | PMID10891110 | BindingDB,ChEMBL |
Ratio | 2.4 - | Bioorg. Med. Chem. Lett., (1991) 1:3:147 | ChEMBL |
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