Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50249433
Substrate
n/a
Meas. Tech.
ChEMBL_1679899 (CHEMBL4030176)
EC50
776±n/a nM
Citation
 Melancon, BJWood, MRNoetzel, MJNance, KDEngelberg, EMHan, CLamsal, AChang, SCho, HPByers, FWBubser, MJones, CKNiswender, CMWood, MWEngers, DWWu, DBrandon, NJDuggan, MEConn, PJBridges, TMLindsley, CW Optimization of M Bioorg Med Chem Lett 27:2296-2301 (2017) [PubMed]  Article 
Target
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:
MANFTPVNGSSGNQSVRLVTSSSHNRYETVEMVFIATVTGSLSLVTVVGNILVMLSIKVNRQLQTVNNYFLFSLACADLIIGAFSMNLYTVYIIKGYWPLGAVVCDLWLALDYVVSNASVMNLLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTVPDNQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAKTLAFLKSPLMKQSVKKPPPGEAAREELRNGKLEEAPPPALPPPPRPVADKDTSNESSSGSATQNTKERPATELSTTEATTPAMPAPPLQPRALNPASRWSKIQIVTKQTGNECVTAIEIVPATPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMVLVNTFCQSCIPDTVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
  
Inhibitor
Name:
BDBM50249433
Synonyms:
CHEMBL4064060
Type:
Small organic molecule
Emp. Form.:
C22H20FN5OS
Mol. Mass.:
421.491
SMILES:
Cc1cc(cnc1F)-c1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1
Structure:
Search PDB for entries with ligand similarity: