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Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50258656
Substrate
n/a
Meas. Tech.
ChEMBL_605047 (CHEMBL1071909)
EC50
>30000±n/a nM
Citation
 Bridges, TM; Kennedy, JP; Cho, HP; Breininger, ML; Gentry, PR; Hopkins, CR; Conn, PJ; Lindsley, CW Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorg Med Chem Lett 20:558-62 (2010) [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:
BDBM50258656
Synonyms:
1-(4-methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dione | CHEMBL466253 | VU0238429 | cid_42633508
Type:
Small organic molecule
Emp. Form.:
C17H12F3NO4
Mol. Mass.:
351.2767
SMILES:
COc1ccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc23)cc1
Structure:
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