Reaction Details |
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Target | Muscarinic acetylcholine receptor M4 |
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Ligand | BDBM50423960 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_935591 (CHEMBL2320373) |
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EC50 | 128±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 |
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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BDBM50423960 |
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n/a |
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Name | BDBM50423960 |
Synonyms: | CHEMBL2313384 |
Type | Small organic molecule |
Emp. Form. | C17H17ClN4OS |
Mol. Mass. | 360.861 |
SMILES | Cc1nc2sc(C(=O)NCCc3ccncc3)c(N)c2c(C)c1Cl |
Structure |
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