Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50253072
Substrate
n/a
Meas. Tech.
ChEBML_1685389
EC50
17±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:
BDBM50253072
Synonyms:
CHEMBL4083327
Type:
Small organic molecule
Emp. Form.:
C18H20N6O2S
Mol. Mass.:
384.455
SMILES:
COc1cncc(c1)N1CC(C1)NC(=O)c1sc2nnc(C)c(C)c2c1N
Structure:
Search PDB for entries with ligand similarity: