| Reaction Details |
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 | Report a problem with these data |
| Target | Muscarinic acetylcholine receptor M4 |
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| Ligand | BDBM48043 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_935589 (CHEMBL2320371) |
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| EC50 | 230±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_RAT | Cholinergic, muscarinic M4 | Chrm-4 | Chrm4 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 52841.70 |
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| Organism: | RAT |
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| Description: | Cholinergic, muscarinic M4 CHRM4 RAT::P08485 |
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| Residue: | 477 |
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| Sequence: | MNFTPVNGSSANQSVRLVTAAHNHLETVEMVFIATVTGSLSLVTVVGNILVMLSIKVNRQ
LQTVNNYFLFSLGCADLIIGAFSMNLYTLYIIKGYWPLGAVVCDLWLALDYVVSNASVMN
LLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTVPD
NQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAKTL
AFLKSPLMKPSIKKPPPGGASREELRNGKLEEAPPPALPPPPRPVPDKDTSNESSSGSAT
QNTKERPPTELSTAEATTPALPAPTLQPRTLNPASKWSKIQIVTKQTGNECVTAIEIVPA
TPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMVLV
NTFCQSCIPERVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
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| BDBM48043 |
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| n/a |
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| Name | BDBM48043 |
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| Synonyms: | 3-amino-4,6-dimethyl-N-p-anisyl-thieno[2,3-b]pyridine-2-carboxamide | 3-amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethyl-2-thieno[2,3-b]pyridinecarboxamide | 3-amino-N-[(4-methoxyphenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide | 3-azanyl-N-[(4-methoxyphenyl)methyl]-4,6-dimethyl-thieno[2,3-b]pyridine-2-carboxamide | ML108 | VU0152100-1 | cid_864492 |
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| Type | Small organic molecule |
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| Emp. Form. | C18H19N3O2S |
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| Mol. Mass. | 341.427 |
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| SMILES | COc1ccc(CNC(=O)c2sc3nc(C)cc(C)c3c2N)cc1 |
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| Structure | 
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