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Name | Muscarinic acetylcholine receptor M5 |
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Species | Homo sapiens (Human) |
Gene | CHRM5 |
Synonym | M5R M5 receptor cholinergic receptor cholinergic receptor, muscarinic 5 |
Disease | Urinary incontinence Colitis Dysmenorrhea Irritable bowel syndrome Myasthenia gravis [ Show all ] |
Length | 532 |
Amino acid sequence | MEGDSYHNATTVNGTPVNHQPLERHRLWEVITIAAVTAVVSLITIVGNVLVMISFKVNSQLKTVNNYYLLSLACADLIIGIFSMNLYTTYILMGRWALGSLACDLWLALDYVASNASVMNLLVISFDRYFSITRPLTYRAKRTPKRAGIMIGLAWLISFILWAPAILCWQYLVGKRTVPLDECQIQFLSEPTITFGTAIAAFYIPVSVMTILYCRIYRETEKRTKDLADLQGSDSVTKAEKRKPAHRALFRSCLRCPRPTLAQRERNQASWSSSRRSTSTTGKPSQATGPSANWAKAEQLTTCSSYPSSEDEDKPATDPVLQVVYKSQGKESPGEEFSAEETEETFVKAETEKSDYDTPNYLLSPAAAHRPKSQKCVAYKFRLVVKADGNQETNNGCHKVKIMPCPFPVAKEPSTKGLNPNPSHQMTKRKRVVLVKERKAAQTLSAILLAFIITWTPYNIMVLVSTFCDKCVPVTLWHLGYWLCYVNSTVNPICYALCNRTFRKTFKMLLLCRWKKKKVEEKLYWQGNSKLP |
UniProt | P08912 |
Protein Data Bank | N/A |
GPCR-HGmod model | N/A |
3D structure model | No available structures or models |
BioLiP | N/A |
Therapeutic Target Database | T79961 |
ChEMBL | CHEMBL2035 |
IUPHAR | 17 |
DrugBank | BE0000247, BE0004890 |
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 | HMS2236L04 Carbachol,(S) Isopto Carbachol Carbacholum chloratum Lentine [ 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 |
---|---|---|---|
Activity | 14.7 /s | PMID20716489 | ChEMBL |
Activity | 200.0 % | PMID13678406 | ChEMBL |
EC50 | 360.0 nM | PMID7783150 | ChEMBL |
EC50 | 1000.0 nM | PMID17149881 | ChEMBL |
EC50 | 2800.0 nM | PMID20716489 | ChEMBL |
EC50 | 6309.57 nM | PMID13678406 | ChEMBL |
EC50 | 8900.0 nM | PMID11741475 | ChEMBL |
EC50 | 9.12011e+13 nM | PMID17084634 | ChEMBL |
ED50 | 2.7 uM | PMID9651157 | ChEMBL |
ED50 | 1400.0 nM | PMID9651157 | ChEMBL |
IC50 | 25200.0 nM | PMID9873472 | ChEMBL |
Intrinsic activity | 1.0 - | PMID17084634 | ChEMBL |
Ki | 4.3 nM | PMID12747793 | PDSP |
Ki | 4265.8 nM | PMID18182302 | ChEMBL |
Ki | 4300.0 nM | PMID12747793 | ChEMBL |
Ki | 19952.6 nM | PMID17149881, PMID13678406 | ChEMBL |
Ki | 69183.1 nM | PMID18543900, PMID24980056, PMID19896386, PMID16539379, PMID18077164 | ChEMBL |
PI | 100.0 % | Bioorg. Med. Chem. Lett., (1995) 5:6:631 | ChEMBL |
Smax | 110.0 % | PMID11741475 | ChEMBL |
Stimulation | 100.0 % | PMID9651157 | ChEMBL |
TIME | 1.889e-05 hr | PMID20716489 | ChEMBL |
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