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Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50174737
Substrate
n/a
Meas. Tech.
ChEMBL_1579485 (CHEMBL3810554)
EC50
410±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_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:
BDBM50174737
Synonyms:
CHEMBL1357034
Type:
Small organic molecule
Emp. Form.:
C20H23N5O3S2
Mol. Mass.:
445.558
SMILES:
Cc1sc2ncnc(N3CCC(CC3)C(=O)Nc3ccc(cc3)S(N)(=O)=O)c2c1C
Structure:
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