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Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50240548
Substrate
n/a
Meas. Tech.
ChEMBL_1668370 (CHEMBL4018258)
IC50
100±n/a nM
Citation
 Bender, AM; Weiner, RL; Luscombe, VB; Cho, HP; Niswender, CM; Engers, DW; Bridges, TM; Conn, PJ; Lindsley, CW Synthesis and evaluation of 4,6-disubstituted pyrimidines as CNS penetrant pan-muscarinic antagonists with a novel chemotype. Bioorg Med Chem Lett 27:2479-2483 (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:
BDBM50240548
Synonyms:
CHEMBL4059829
Type:
Small organic molecule
Emp. Form.:
C25H24F2N4O2
Mol. Mass.:
450.4805
SMILES:
Fc1ccc(Oc2cc(ncn2)N2CCC(CC2)C(=O)N2CCc3ccccc3C2)c(F)c1
Structure:
Search PDB for entries with ligand similarity: