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Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50174736
Substrate
n/a
Meas. Tech.
ChEMBL_1579487 (CHEMBL3810685)
EC50
950±n/a nM
Citation
 Wood, MR; Noetzel, MJ; Engers, JL; Bollinger, KA; Melancon, BJ; Tarr, JC; Han, C; West, M; Gregro, AR; Lamsal, A; Chang, S; Ajmera, S; Smith, E; Chase, P; Hodder, PS; Bubser, M; Jones, CK; Hopkins, CR; Emmitte, KA; Niswender, CM; Wood, MW; Duggan, ME; Conn, PJ; Bridges, TM; Lindsley, CW Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core. Bioorg Med Chem Lett 26:3029-33 (2016) [PubMed]  Article 
Target
Name:
Muscarinic acetylcholine receptor M4
Synonyms:
ACM4_RAT | Cholinergic, muscarinic M4 | Chrm-4 | Chrm4
Type:
Enzyme Catalytic Domain
Mol. Mass.:
52841.70
Organism:
RAT
Description:
Cholinergic, muscarinic M4 CHRM4 RAT::P08485
Residue:
477
Sequence:
MNFTPVNGSSANQSVRLVTAAHNHLETVEMVFIATVTGSLSLVTVVGNILVMLSIKVNRQLQTVNNYFLFSLGCADLIIGAFSMNLYTLYIIKGYWPLGAVVCDLWLALDYVVSNASVMNLLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTVPDNQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAKTLAFLKSPLMKPSIKKPPPGGASREELRNGKLEEAPPPALPPPPRPVPDKDTSNESSSGSATQNTKERPPTELSTAEATTPALPAPTLQPRTLNPASKWSKIQIVTKQTGNECVTAIEIVPATPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMVLVNTFCQSCIPERVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
  
Inhibitor
Name:
BDBM50174736
Synonyms:
CHEMBL3808485
Type:
Small organic molecule
Emp. Form.:
C19H19FN4O
Mol. Mass.:
338.3788
SMILES:
Cc1ccc(OC2CCN(CC2)c2ncnc3ccc(F)cc23)cn1
Structure:
Search PDB for entries with ligand similarity: