Ki Summary

Reaction Details

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Target

Muscarinic acetylcholine receptor M4

Ligand

BDBM50577263

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_2129874 (CHEMBL4839303)

IC50

4.1±n/a nM

Citation

Spock, M; Carter, TR; Bollinger, KA; Han, C; Baker, LA; Rodriguez, AL; Peng, L; Dickerson, JW; Qi, A; Rook, JM; O'Neill, JC; Watson, KJ; Chang, S; Bridges, TM; Engers, JL; Engers, DW; Niswender, CM; Conn, PJ; Lindsley, CW; Bender, AM Discovery of VU6028418: A Highly Selective and Orally Bioavailable M ACS Med Chem Lett12:1342-1349 (2021) [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

BDBM50577263

n/a

Name

BDBM50577263

Synonyms:

CHEMBL4850236

Type

Small organic molecule

Emp. Form.

C23H27F3N4O

Mol. Mass.

432.4819

SMILES

[H][C@@]12C[C@H](C[C@]1([H])CN(CC1CCOCC1)C2)Nc1ccc(nn1)-c1cc(F)cc(F)c1F |r|

Structure