Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50207523
Substrate
n/a
Meas. Tech.
ChEMBL_1631989 (CHEMBL3874695)
EC50
60±n/a nM
Citation
 Wood, MRNoetzel, MJPoslusney, MSMelancon, BJTarr, JCLamsal, AChang, SLuscombe, VBWeiner, RLCho, HPBubser, MJones, CKNiswender, CMWood, MWEngers, DWBrandon, NJDuggan, MEConn, PJBridges, TMLindsley, CW Challenges in the development of an M Bioorg Med Chem Lett 27:171-175 (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:
BDBM50207523
Synonyms:
CHEMBL3982695
Type:
Small organic molecule
Emp. Form.:
C17H18N4OS2
Mol. Mass.:
358.481
SMILES:
CSc1ccc(CNC(=O)c2sc3nnc(C)c(C)c3c2N)cc1
Structure:
Search PDB for entries with ligand similarity: