Reaction Details |
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Target | Muscarinic acetylcholine receptor M4 |
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Ligand | BDBM50174738 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1579483 (CHEMBL3810552) |
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IC50 | 2400±n/a nM |
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Citation | Wood, MR; Noetzel, MJ; Engers, JL; Bollinger, KA; Melancon, BJ; Tarr, JC; Han, C; West, M; Gregro, AR; Lamsal, A; Chang, S; Ajmera, S; Smith, E; Chase, P; Hodder, PS; Bubser, M; Jones, CK; Hopkins, CR; Emmitte, KA; Niswender, CM; Wood, MW; Duggan, ME; Conn, PJ; Bridges, TM; Lindsley, CW Discovery and optimization of a novel series of highly CNS penetrant M4 PAMs based on a 5,6-dimethyl-4-(piperidin-1-yl)thieno[2,3-d]pyrimidine core. Bioorg Med Chem Lett26:3029-33 (2016) [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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BDBM50174738 |
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n/a |
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Name | BDBM50174738 |
Synonyms: | CHEMBL3808947 |
Type | Small organic molecule |
Emp. Form. | C22H29N5S |
Mol. Mass. | 395.564 |
SMILES | CCCN(C1CCN(CC1)c1ncnc2sc(C)c(C)c12)c1ccc(C)nc1 |
Structure |
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