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TargetMuscarinic acetylcholine receptor M4
LigandBDBM50521763
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1885222 (CHEMBL4386804)
EC50 8.0±n/a nM
Citation Chopko, TCHan, CGregro, AREngers, DWFelts, ASPoslusney, MSBollinger, KAMorrison, RDBubser, MLamsal, ALuscombe, VBCho, HPSchnetz-Boutaud, NCRodriguez, ALChang, SDaniels, JSStec, DFNiswender, CMJones, CKWood, MRWood, MWDuggan, MEBrandon, NJConn, PJBridges, TMLindsley, CWMelancon, BJ SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M Bioorg Med Chem Lett29:2224-2228 (2019) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Muscarinic acetylcholine receptor M4
Name:Muscarinic acetylcholine receptor M4
Synonyms:ACM4_HUMAN | CHRM4 | Cholinergic, muscarinic M4 | Muscarinic acetylcholine receptor | Muscarinic acetylcholine receptor M2 and M4
Type:Enzyme Catalytic Domain
Mol. Mass.:53079.31
Organism:Homo sapiens (Human)
Description:Cholinergic, muscarinic M4 CHRM4 HUMAN M3::P08173
Residue:479
Sequence:
MANFTPVNGSSGNQSVRLVTSSSHNRYETVEMVFIATVTGSLSLVTVVGNILVMLSIKVN
RQLQTVNNYFLFSLACADLIIGAFSMNLYTVYIIKGYWPLGAVVCDLWLALDYVVSNASV
MNLLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTV
PDNQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAK
TLAFLKSPLMKQSVKKPPPGEAAREELRNGKLEEAPPPALPPPPRPVADKDTSNESSSGS
ATQNTKERPATELSTTEATTPAMPAPPLQPRALNPASRWSKIQIVTKQTGNECVTAIEIV
PATPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMV
LVNTFCQSCIPDTVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
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  Blast E-value cutoff:
BDBM50521763
n/a
NameBDBM50521763
Synonyms:CHEMBL4579086
TypeSmall organic molecule
Emp. Form.C20H18ClN5OS
Mol. Mass.411.908
SMILESCc1nnc2c(Cl)c(C)c3c(N)c(sc3n12)C(=O)NC1Cc2ccccc2C1
Structure
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