Reaction Details |
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Target | Muscarinic acetylcholine receptor M4 |
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Ligand | BDBM50521777 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1885222 (CHEMBL4386804) |
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EC50 | 120±n/a nM |
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Citation | Chopko, TC; Han, C; Gregro, AR; Engers, DW; Felts, AS; Poslusney, MS; Bollinger, KA; Morrison, RD; Bubser, M; Lamsal, A; Luscombe, VB; Cho, HP; Schnetz-Boutaud, NC; Rodriguez, AL; Chang, S; Daniels, JS; Stec, DF; Niswender, CM; Jones, CK; Wood, MR; Wood, MW; Duggan, ME; Brandon, NJ; Conn, PJ; Bridges, TM; Lindsley, CW; Melancon, BJ SAR inspired by aldehyde oxidase (AO) metabolism: Discovery of novel, CNS penetrant tricyclic M Bioorg Med Chem Lett29:2224-2228 (2019) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Muscarinic acetylcholine receptor M4 |
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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: | MANFTPVNGSSGNQSVRLVTSSSHNRYETVEMVFIATVTGSLSLVTVVGNILVMLSIKVN
RQLQTVNNYFLFSLACADLIIGAFSMNLYTVYIIKGYWPLGAVVCDLWLALDYVVSNASV
MNLLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTV
PDNQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAK
TLAFLKSPLMKQSVKKPPPGEAAREELRNGKLEEAPPPALPPPPRPVADKDTSNESSSGS
ATQNTKERPATELSTTEATTPAMPAPPLQPRALNPASRWSKIQIVTKQTGNECVTAIEIV
PATPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMV
LVNTFCQSCIPDTVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
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BDBM50521777 |
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n/a |
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Name | BDBM50521777 |
Synonyms: | CHEMBL4558206 |
Type | Small organic molecule |
Emp. Form. | C21H22N8OS |
Mol. Mass. | 434.517 |
SMILES | Cc1nc2cc(C)c3c(N)c(sc3n2n1)C(=O)NC1CN(C1)c1cnc(nc1)C1CC1 |
Structure |
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