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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 | pirenzepine |
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Molecular formula | C19H21N5O2 |
IUPAC name | 11-[2-(4-methylpiperazin-1-yl)acetyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one |
Molecular weight | 351.41 |
Hydrogen bond acceptor | 5 |
Hydrogen bond donor | 1 |
XlogP | 0.1 |
Synonyms | Gasteril KBio2_001858 Lopac-P-7412 NCGC00015836-04 11-[2-(4-methylpiperazin-1-yl)acetyl]-5H-pyrido[2,3-b][1,4]benzodiazepin-6-one;hydrochloride [ Show all ] |
Inchi Key | RMHMFHUVIITRHF-UHFFFAOYSA-N |
Inchi ID | InChI=1S/C19H21N5O2/c1-22-9-11-23(12-10-22)13-17(25)24-16-7-3-2-5-14(16)19(26)21-15-6-4-8-20-18(15)24/h2-8H,9-13H2,1H3,(H,21,26) |
PubChem CID | 4848 |
ChEMBL | CHEMBL9967 |
IUPHAR | 328 |
BindingDB | 39341 |
DrugBank | DB00670 |
Structure | |
Lipinski's druglikeness | This ligand satisfies Lipinski's rule of five. |
Parameter | Value | Reference | Database source |
---|---|---|---|
IC50 | 340.6 nM | PMID9986705 | ChEMBL |
IC50 | 341.0 nM | PMID9986705 | BindingDB |
Ki | <10000.0 nM | PMID3272174 | PDSP,BindingDB |
Ki | 35.48 nM | PMID13679167, PMID17889543 | BindingDB,ChEMBL |
Ki | 35.4813 nM | PMID13679167 | PDSP |
Ki | 79.4328 - 158.489 nM | PMID7925952, PMID9113359, PMID2043926 | IUPHAR |
Ki | 89.1251 nM | PMID1994002 | PDSP |
Ki | 89.13 nM | PMID1994002 | BindingDB |
Ki | 126.0 nM | PMID23379472 | BindingDB,ChEMBL |
Ki | 130.0 nM | PMID9121349 | PDSP |
Ki | 170.0 nM | PMID1346637 | PDSP,BindingDB |
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