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Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50342538
Substrate
n/a
Meas. Tech.
ChEMBL_744889 (CHEMBL1772910)
IC50
6800±n/a nM
Citation
Andrews, MD; Fish, PV; Blagg, J; Brabham, TK; Brennan, PE; Bridgeland, A; Brown, AD; Bungay, PJ; Conlon, KM; Edmunds, NJ; af Forselles, K; Gibbons, CP; Green, MP; Hanton, G; Holbrook, M; Jessiman, AS; McIntosh, K; McMurray, G; Nichols, CL; Root, JA; Storer, RI; Sutton, MR; Ward, RV; Westbrook, D; Whitlock, GA Pyrimido[4,5-d]azepines as potent and selective 5-HT2C receptor agonists: design, synthesis, and evaluation of PF-3246799 as a treatment for urinary incontinence. Bioorg Med Chem Lett 21:2715-20 (2011) [PubMed] Article
More Info.:
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