Reaction Details |
| Report a problem with these data |
Target | Muscarinic acetylcholine receptor M4 |
---|
Ligand | BDBM50268355 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_1704900 (CHEMBL4056133) |
---|
IC50 | 1600±n/a nM |
---|
Citation | Bender, AM; Weiner, RL; Luscombe, VB; Ajmera, S; Cho, HP; Chang, S; Zhan, X; Rodriguez, AL; Niswender, CM; Engers, DW; Bridges, TM; Conn, PJ; Lindsley, CW Discovery and optimization of 3-(4-aryl/heteroarylsulfonyl)piperazin-1-yl)-6-(piperidin-1-yl)pyridazines as novel, CNS penetrant pan-muscarinic antagonists. Bioorg Med Chem Lett27:3576-3581 (2017) [PubMed] Article |
---|
More Info.: | Get all data from this article, Assay Method |
---|
|
Muscarinic acetylcholine receptor M4 |
---|
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
|
|
|
BDBM50268355 |
---|
n/a |
---|
Name | BDBM50268355 |
Synonyms: | CHEMBL4088672 |
Type | Small organic molecule |
Emp. Form. | C18H27N7O2S |
Mol. Mass. | 405.518 |
SMILES | C[C@H]1CCCCN1c1ccc(nn1)N1CCN(CC1)S(=O)(=O)c1nccn1C |r| |
Structure |
|