Target
Muscarinic acetylcholine receptor M4
Ligand
BDBM50207517
Substrate
n/a
Meas. Tech.
ChEMBL_1631989 (CHEMBL3874695)
EC50
631±n/a nM
Citation
 Wood, MRNoetzel, MJPoslusney, MSMelancon, BJTarr, JCLamsal, AChang, SLuscombe, VBWeiner, RLCho, HPBubser, MJones, CKNiswender, CMWood, MWEngers, DWBrandon, NJDuggan, MEConn, PJBridges, TMLindsley, CW Challenges in the development of an M Bioorg Med Chem Lett 27:171-175 (2017) [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:
BDBM50207517
Synonyms:
CHEMBL3915634
Type:
Small organic molecule
Emp. Form.:
C17H15F3N4O3S2
Mol. Mass.:
444.451
SMILES:
Cc1nnc2sc(C(=O)NCc3ccc(cc3)S(=O)(=O)C(F)(F)F)c(N)c2c1C
Structure:
Search PDB for entries with ligand similarity: