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TargetMuscarinic acetylcholine receptor M4
LigandBDBM50423965
Substrate/Competitorn/a
Meas. Tech.ChEMBL_935591 (CHEMBL2320373)
EC50 61±n/a nM
Citation Le, UMelancon, BJBridges, TMVinson, PNUtley, TJLamsal, ARodriguez, ALVenable, DSheffler, DJJones, CKBlobaum, ALWood, MRDaniels, JSConn, PJNiswender, CMLindsley, CWHopkins, CR Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorg Med Chem Lett23:346-50 (2012) [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:
BDBM50423965
n/a
NameBDBM50423965
Synonyms:CHEMBL2313379
TypeSmall organic molecule
Emp. Form.C17H17ClN4OS
Mol. Mass.360.861
SMILESCc1cc(CNC(=O)c2sc3nc(C)c(Cl)c(C)c3c2N)ccn1
Structure
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