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Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50268387
Substrate
n/a
Meas. Tech.
ChEMBL_1704900 (CHEMBL4056133)
IC50
2340±n/a nM
Citation
 Bender, AM; Weiner, RL; Luscombe, VB; Ajmera, S; Cho, HP; Chang, S; Zhan, X; Rodriguez, AL; Niswender, CM; Engers, DW; Bridges, TM; Conn, PJ; Lindsley, CW Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists. Bioorg Med Chem Lett 27:3576-3581 (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:
BDBM50268387
Synonyms:
CHEMBL4070135
Type:
Small organic molecule
Emp. Form.:
C20H26ClN5O2S
Mol. Mass.:
435.971
SMILES:
C[C@H]1CCCCN1c1ccc(nn1)N1CCN(CC1)S(=O)(=O)c1ccc(Cl)cc1 |r|
Structure:
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