Reaction Details |
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Target | Muscarinic acetylcholine receptor M4 |
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Ligand | BDBM50258656 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_605047 (CHEMBL1071909) |
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EC50 | >30000±n/a nM |
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Citation | Bridges, TM; Kennedy, JP; Cho, HP; Breininger, ML; Gentry, PR; Hopkins, CR; Conn, PJ; Lindsley, CW Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorg Med Chem Lett20:558-62 (2010) [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_RAT | Cholinergic, muscarinic M4 | Chrm-4 | Chrm4 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 52841.70 |
Organism: | RAT |
Description: | Cholinergic, muscarinic M4 CHRM4 RAT::P08485 |
Residue: | 477 |
Sequence: | MNFTPVNGSSANQSVRLVTAAHNHLETVEMVFIATVTGSLSLVTVVGNILVMLSIKVNRQ
LQTVNNYFLFSLGCADLIIGAFSMNLYTLYIIKGYWPLGAVVCDLWLALDYVVSNASVMN
LLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTVPD
NQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAKTL
AFLKSPLMKPSIKKPPPGGASREELRNGKLEEAPPPALPPPPRPVPDKDTSNESSSGSAT
QNTKERPPTELSTAEATTPALPAPTLQPRTLNPASKWSKIQIVTKQTGNECVTAIEIVPA
TPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMVLV
NTFCQSCIPERVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
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BDBM50258656 |
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n/a |
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Name | BDBM50258656 |
Synonyms: | 1-(4-methoxybenzyl)-5-(trifluoromethoxy)indoline-2,3-dione | CHEMBL466253 | VU0238429 | cid_42633508 |
Type | Small organic molecule |
Emp. Form. | C17H12F3NO4 |
Mol. Mass. | 351.2767 |
SMILES | COc1ccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc23)cc1 |
Structure |
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