Reaction Details Report a problem with these data
Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50061705
Substrate
n/a
Meas. Tech.
ChEMBL_945483 (CHEMBL2343487)
EC50
5.7±n/a nM
Citation
Sumiyoshi, T; Enomoto, T; Takai, K; Takahashi, Y; Konishi, Y; Uruno, Y; Tojo, K; Suwa, A; Matsuda, H; Nakako, T; Sakai, M; Kitamura, A; Uematsu, Y; Kiyoshi, A Discovery of novel N-substituted oxindoles as selective m1 and m4 muscarinic acetylcholine receptors partial agonists. ACS Med Chem Lett 4:244-8 (2013) [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
Inhibitor
Name:
BDBM50061705
Synonyms:
(R)-1-Aza-bicyclo[2.2.2]oct-3-yl-[(Z)-methoxyimino]-acetonitrile | CHEMBL134641 | SB-202026
Type:
Small organic molecule
Emp. Form.:
C10H15N3O
Mol. Mass.:
193.2456
SMILES:
CO\N=C(/C#N)[C@H]1CN2CCC1CC2 |wU:6.5,(10.77,-7.56,;9.23,-7.56,;8.14,-8.66,;8.14,-10.2,;9.41,-10.96,;10.69,-11.69,;6.8,-10.98,;6.8,-12.53,;5.46,-13.28,;4.14,-12.53,;4.14,-10.98,;5.46,-10.2,;4.95,-11.51,;5.89,-12.1,)|