Reaction Details |
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Target | Muscarinic acetylcholine receptor M4 |
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Ligand | BDBM50240552 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1704863 (CHEMBL4056096) |
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Ki | 0.640000±n/a nM |
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Citation | Bender, AM; Weiner, RL; Luscombe, VB; Ajmera, S; Cho, HP; Chang, S; Zhan, X; Rodriguez, AL; Niswender, CM; Engers, DW; Bridges, TM; Conn, PJ; Lindsley, CW Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists. Bioorg Med Chem Lett27:3576-3581 (2017) [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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BDBM50240552 |
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n/a |
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Name | BDBM50240552 |
Synonyms: | CHEMBL195 |
Type | Small organic molecule |
Emp. Form. | C17H23NO3 |
Mol. Mass. | 289.3694 |
SMILES | [H][C@@]12CC[C@]([H])(CC(C1)OC(=O)C(CO)c1ccccc1)N2C |r,@@:7,TLB:9:7:21:2.3| |
Structure |
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