| Reaction Details |
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 | Report a problem with these data |
| Target | Muscarinic acetylcholine receptor M4 |
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| Ligand | BDBM50423953 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_935591 (CHEMBL2320373) |
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| EC50 | 80±n/a nM |
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| Citation |  Le, U; Melancon, BJ; Bridges, TM; Vinson, PN; Utley, TJ; Lamsal, A; Rodriguez, AL; Venable, D; Sheffler, DJ; Jones, CK; Blobaum, AL; Wood, MR; Daniels, JS; Conn, PJ; Niswender, CM; Lindsley, CW; Hopkins, CR Discovery of a selective M4 positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorg Med Chem Lett23:346-50 (2012) [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 |
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| Synonyms: | ACM4_HUMAN | CHRM4 | Cholinergic, muscarinic M4 | Muscarinic acetylcholine receptor | Muscarinic acetylcholine receptor M2 and M4 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 53079.31 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Cholinergic, muscarinic M4 CHRM4 HUMAN M3::P08173 |
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| Residue: | 479 |
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| Sequence: | MANFTPVNGSSGNQSVRLVTSSSHNRYETVEMVFIATVTGSLSLVTVVGNILVMLSIKVN
RQLQTVNNYFLFSLACADLIIGAFSMNLYTVYIIKGYWPLGAVVCDLWLALDYVVSNASV
MNLLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTV
PDNQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAK
TLAFLKSPLMKQSVKKPPPGEAAREELRNGKLEEAPPPALPPPPRPVADKDTSNESSSGS
ATQNTKERPATELSTTEATTPAMPAPPLQPRALNPASRWSKIQIVTKQTGNECVTAIEIV
PATPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMV
LVNTFCQSCIPDTVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
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| BDBM50423953 |
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| n/a |
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| Name | BDBM50423953 |
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| Synonyms: | CHEMBL2313391 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H16ClN3O3S |
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| Mol. Mass. | 389.856 |
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| SMILES | Cc1nc2sc(C(=O)NCc3ccc4OCOc4c3)c(N)c2c(C)c1Cl |
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| Structure | 
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