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TargetMuscarinic acetylcholine receptor M4
LigandBDBM50174738
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1579483 (CHEMBL3810552)
IC50 2400±n/a nM
Citation Wood, MRNoetzel, MJEngers, JLBollinger, KAMelancon, BJTarr, JCHan, CWest, MGregro, ARLamsal, AChang, SAjmera, SSmith, EChase, PHodder, PSBubser, MJones, CKHopkins, CREmmitte, KANiswender, CMWood, MWDuggan, MEConn, PJBridges, TMLindsley, CW Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core. Bioorg Med Chem Lett26:3029-33 (2016) [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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50174738
n/a
NameBDBM50174738
Synonyms:CHEMBL3808947
TypeSmall organic molecule
Emp. Form.C22H29N5S
Mol. Mass.395.564
SMILESCCCN(C1CCN(CC1)c1ncnc2sc(C)c(C)c12)c1ccc(C)nc1
Structure
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