Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50253109
Substrate
n/a
Meas. Tech.
ChEBML_1685389
EC50
8.1±n/a nM
Citation
 Tarr, JCWood, MRNoetzel, MJBertron, JLWeiner, RLRodriguez, ALLamsal, AByers, FWChang, SCho, HPJones, CKNiswender, CMWood, MWBrandon, NJDuggan, MEConn, PJBridges, TMLindsley, CW Challenges in the development of an M Bioorg Med Chem Lett 27:2990-2995 (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:
BDBM50253109
Synonyms:
CHEMBL4066508
Type:
Small organic molecule
Emp. Form.:
C17H17ClN6OS
Mol. Mass.:
388.874
SMILES:
Cc1nnc2sc(C(=O)NC3CN(C3)c3ccncc3Cl)c(N)c2c1C
Structure:
Search PDB for entries with ligand similarity: