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Name | Muscarinic acetylcholine receptor M4 |
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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 [ 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 |
Name | CHEMBL3354075 |
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Molecular formula | C26H42N2O2 |
IUPAC name | 1-[3-[4-(9-hydroxynonyl)piperidin-1-yl]propyl]-3,4-dihydroquinolin-2-one |
Molecular weight | 414.634 |
Hydrogen bond acceptor | 3 |
Hydrogen bond donor | 1 |
XlogP | 5.7 |
Synonyms | BDBM50030247 |
Inchi Key | AWEBVNCNTLOVSN-UHFFFAOYSA-N |
Inchi ID | InChI=1S/C26H42N2O2/c29-22-9-5-3-1-2-4-6-11-23-16-20-27(21-17-23)18-10-19-28-25-13-8-7-12-24(25)14-15-26(28)30/h7-8,12-13,23,29H,1-6,9-11,14-22H2 |
PubChem CID | 118719928 |
ChEMBL | CHEMBL3354075 |
IUPHAR | N/A |
BindingDB | 50030247 |
DrugBank | N/A |
Structure | |
Lipinski's druglikeness | This ligand has a partition coefficient log P greater than 5. |
Parameter | Value | Reference | Database source |
---|---|---|---|
Emax | 0.0 % | PMID25275964 | ChEMBL |
IC50 | 588.84 nM | PMID25275964 | ChEMBL |
IC50 | 589.0 nM | PMID25275964 | BindingDB |
IC50 | 812.83 nM | PMID25275964 | ChEMBL |
IC50 | 813.0 nM | PMID25275964 | BindingDB |
IC50 | 3630.78 nM | PMID25275964 | ChEMBL |
IC50 | 3631.0 nM | PMID25275964 | BindingDB |
Imax | 90.0 % | PMID25275964 | ChEMBL |
Imax | 92.0 % | PMID25275964 | ChEMBL |
Imax | >100.0 % | PMID25275964 | ChEMBL |
Ki | 154.88 nM | PMID25275964 | ChEMBL |
Ki | 155.0 nM | PMID25275964 | BindingDB |
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