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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 | carbachol |
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Molecular formula | C6H15ClN2O2 |
IUPAC name | 2-carbamoyloxyethyl(trimethyl)azanium;chloride |
Molecular weight | 182.648 |
Hydrogen bond acceptor | 3 |
Hydrogen bond donor | 1 |
XlogP | None |
Synonyms | AC1LAVH8 Ethanaminium, 2-((aminocarbonyl)oxy)-N,N,N-trimethyl-, chloride C6H15N2O2.Cl HMS1920I15 Carbachol, European Pharmacopoeia (EP) Reference Standard [ Show all ] |
Inchi Key | AIXAANGOTKPUOY-UHFFFAOYSA-N |
Inchi ID | InChI=1S/C6H14N2O2.ClH/c1-8(2,3)4-5-10-6(7)9;/h4-5H2,1-3H3,(H-,7,9);1H |
PubChem CID | 5831 |
ChEMBL | CHEMBL14 |
IUPHAR | N/A |
BindingDB | N/A |
DrugBank | DB00411 |
Structure | |
Lipinski's druglikeness | Partition coefficient log P of this ligand is not available. |
Parameter | Value | Reference | Database source |
---|---|---|---|
N/A | N/A | DrugBank | |
Activity | 50.0 % | PMID13678406 | ChEMBL |
EC50 | 75.0 nM | PMID7783150 | ChEMBL |
EC50 | 290.0 nM | PMID11741475 | ChEMBL |
EC50 | 3981.07 nM | PMID17084634 | ChEMBL |
EC50 | 60000.0 nM | PMID9651157 | ChEMBL |
ED50 | 100.0 nM | PMID9651157 | ChEMBL |
IC50 | 0.4 nM | PMID9873472 | ChEMBL |
IC50 | 50.12 nM | PMID17149881 | ChEMBL |
IC50 | 1000.0 nM | PMID13678406 | ChEMBL |
IC50 | 7200.0 nM | PMID9435896 | ChEMBL |
Inhibition | 6.3 % | PMID9651157 | ChEMBL |
Inhibition | 60.0 % | Bioorg. Med. Chem. Lett., (1995) 5:6:631 | ChEMBL |
Intrinsic activity | 1.0 - | PMID17084634 | ChEMBL |
Ki | 7.6 nM | PMID12747793 | PDSP |
Ki | 24.0 nM | PMID10891110 | ChEMBL |
Ki | 398.11 nM | PMID17149881, PMID13678406 | ChEMBL |
Ki | 1548.81 nM | PMID8968358 | PDSP |
Ki | 2600.0 nM | PMID9622546, PMID10891110 | ChEMBL |
Ki | 6309.57 nM | PMID19896386, PMID18543900, PMID16539379, PMID18077164, PMID24980056 | ChEMBL |
Ki | 7600.0 nM | PMID12747793 | ChEMBL |
pD2 | 5.43 - | PMID16539379, PMID17084634 | ChEMBL |
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