Reaction Details Report a problem with these data
Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50261446
Substrate
n/a
Meas. Tech.
ChEMBL_1696020 (CHEMBL4046910)
EC50
490±n/a nM
Citation
 Bewley, BR; Spearing, PK; Weiner, RL; Luscombe, VB; Zhan, X; Chang, S; Cho, HP; Rodriguez, AL; Niswender, CM; Conn, PJ; Bridges, TM; Engers, DW; Lindsley, CW Discovery of a novel, CNS penetrant M Bioorg Med Chem Lett 27:4274-4279 (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:
BDBM50261446
Synonyms:
CHEMBL4079953
Type:
Small organic molecule
Emp. Form.:
C20H16F2N4O
Mol. Mass.:
366.364
SMILES:
Fc1ccc2ncc(C#N)c(N3CCC(CC3)Oc3ccc(F)nc3)c2c1
Structure:
Search PDB for entries with ligand similarity: