Ki Summary

Reaction Details

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Target

Muscarinic acetylcholine receptor M4

Ligand

BDBM50268360

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_1704900 (CHEMBL4056133)

IC50

520±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

BDBM50268360

n/a

Name

BDBM50268360

Synonyms:

CHEMBL4060443

Type

Small organic molecule

Emp. Form.

C21H26F3N5O2S

Mol. Mass.

469.524

SMILES

C[C@H]1CCCCN1c1ccc(nn1)N1CCN(CC1)S(=O)(=O)c1ccccc1C(F)(F)F |r|

Structure