Ki Summary

Reaction Details

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Target

Muscarinic acetylcholine receptor M4

Ligand

BDBM50382119

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_815545 (CHEMBL2025074)

IC50

>10000±n/a nM

Citation

Melancon, BJ; Gogliotti, RD; Tarr, JC; Saleh, SA; Chauder, BA; Lebois, EP; Cho, HP; Utley, TJ; Sheffler, DJ; Bridges, TM; Morrison, RD; Daniels, JS; Niswender, CM; Conn, PJ; Lindsley, CW; Wood, MR Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor. Bioorg Med Chem Lett22:3467-72 (2012) [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

BDBM50382119

n/a

Name

BDBM50382119

Synonyms:

CHEMBL2022952

Type

Small organic molecule

Emp. Form.

C19H26ClN3O3

Mol. Mass.

379.881

SMILES

CCOC(=O)N1C[C@@H]2CC[C@@H](C1)C2NCCNC(=O)c1cccc(Cl)c1 |r,TLB:3:5:12:8.9,THB:13:12:5.6.11:8.9|

Structure