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Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50445222
Substrate
n/a
Meas. Tech.
ChEMBL_1284798 (CHEMBL3107821)
IC50
>30000±n/a nM
Citation
 Gentry, PR; Kokubo, M; Bridges, TM; Kett, NR; Harp, JM; Cho, HP; Smith, E; Chase, P; Hodder, PS; Niswender, CM; Daniels, JS; Conn, PJ; Wood, MR; Lindsley, CW Discovery of the first M5-selective and CNS penetrant negative allosteric modulator (NAM) of a muscarinic acetylcholine receptor: (S)-9b-(4-chlorophenyl)-1-(3,4-difluorobenzoyl)-2,3-dihydro-1H-imidazo[2,1-a]isoindol-5(9bH)-one (ML375). J Med Chem 56:9351-5 (2013) [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:
BDBM50445222
Synonyms:
CHEMBL3105228
Type:
Small organic molecule
Emp. Form.:
C23H15ClF2N2O2
Mol. Mass.:
424.827
SMILES:
Fc1ccc(cc1F)C(=O)N1CCN2C(=O)c3ccccc3[C@@]12c1ccc(Cl)cc1 |r|
Structure:
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