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Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50122054
Substrate
n/a
Meas. Tech.
ChEMBL_2107608 (CHEMBL4816283)
EC50
>10000±n/a nM
Citation
 Watanabe, H; Ishida, K; Yamamoto, M; Nakako, T; Horiguchi, M; Isobe, Y Identification of 2-fluoro-8-methyl-11-(1-methyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepine with clozapine-like mixed activities at muscarinic acetylcholine, dopamine, and serotonin receptors. Bioorg Med Chem Lett 40:0 (2021) [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:
BDBM50122054
Synonyms:
8-Chloro-11-piperazin-1-yl-5H-dibenzo[b,e][1,4]diazepine | CHEMBL845 | N-Demethylclozapine | N-desmethyl-Clozapine | USRE49340, Rank 7
Type:
Small organic molecule
Emp. Form.:
C17H17ClN4
Mol. Mass.:
312.797
SMILES:
Clc1ccc2Nc3ccccc3C(=Nc2c1)N1CCNCC1 |c:13|
Structure:
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