Reaction Details |
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Target | Muscarinic acetylcholine receptor M4 |
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Ligand | BDBM50023230 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1457824 (CHEMBL3370066) |
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EC50 | >30000±n/a nM |
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Citation | Gentry, PR; Kokubo, M; Bridges, TM; Noetzel, MJ; Cho, HP; Lamsal, A; Smith, E; Chase, P; Hodder, PS; Niswender, CM; Daniels, JS; Conn, PJ; Lindsley, CW; Wood, MR Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380). J Med Chem57:7804-10 (2014) [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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BDBM50023230 |
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n/a |
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Name | BDBM50023230 |
Synonyms: | CHEMBL1602658 |
Type | Small organic molecule |
Emp. Form. | C23H28N2O5S |
Mol. Mass. | 444.544 |
SMILES | CCN(Cc1ccccc1)C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2OCCOc2c1 |
Structure |
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