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Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM48056
Substrate
n/a
Meas. Tech.
ChEMBL_987752 (CHEMBL2439843)
EC50
105±n/a nM
Citation
 Huynh, T; Valant, C; Crosby, IT; Sexton, PM; Christopoulos, A; Capuano, B Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor. J Med Chem 56:8196-200 (2013) [PubMed]  Article
Target
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:
MANFTPVNGSSGNQSVRLVTSSSHNRYETVEMVFIATVTGSLSLVTVVGNILVMLSIKVNRQLQTVNNYFLFSLACADLIIGAFSMNLYTVYIIKGYWPLGAVVCDLWLALDYVVSNASVMNLLIISFDRYFCVTKPLTYPARRTTKMAGLMIAAAWVLSFVLWAPAILFWQFVVGKRTVPDNQCFIQFLSNPAVTFGTAIAAFYLPVVIMTVLYIHISLASRSRVHKHRPEGPKEKKAKTLAFLKSPLMKQSVKKPPPGEAAREELRNGKLEEAPPPALPPPPRPVADKDTSNESSSGSATQNTKERPATELSTTEATTPAMPAPPLQPRALNPASRWSKIQIVTKQTGNECVTAIEIVPATPAGMRPAANVARKFASIARNQVRKKRQMAARERKVTRTIFAILLAFILTWTPYNVMVLVNTFCQSCIPDTVWSIGYWLCYVNSTINPACYALCNATFKKTFRHLLLCQYRNIGTAR
  
Inhibitor
Name:
BDBM48056
Synonyms:
3-amino-N-(2,3-difluorobenzyl)-4,6-dimethyl-thieno[2,3-b]pyridine-2-carboxamide | 3-amino-N-[(2,3-difluorophenyl)methyl]-4,6-dimethyl-2-thieno[2,3-b]pyridinecarboxamide | 3-amino-N-[(2,3-difluorophenyl)methyl]-4,6-dimethylthieno[2,3-b]pyridine-2-carboxamide | 3-azanyl-N-[[2,3-bis(fluoranyl)phenyl]methyl]-4,6-dimethyl-thieno[2,3-b]pyridine-2-carboxamide | VU0402483-1 | cid_44176134
Type:
Small organic molecule
Emp. Form.:
C17H15F2N3OS
Mol. Mass.:
347.382
SMILES:
Cc1cc(C)c2c(N)c(sc2n1)C(=O)NCc1cccc(F)c1F
Structure:
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