Target
Muscarinic acetylcholine receptor M5
Ligand
BDBM50207463
Substrate
n/a
Meas. Tech.
ChEMBL_1632016 (CHEMBL3874722)
EC50
>30000±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 M5
Synonyms:
ACM5_RAT | Cholinergic, muscarinic M5 | Chrm-5 | Chrm5 | Muscarinic acetylcholine receptor | Muscarinic acetylcholine receptor M5
Type:
Enzyme Catalytic Domain
Mol. Mass.:
60161.80
Organism:
RAT
Description:
Cholinergic, muscarinic M5 CHRM5 RAT::P08911
Residue:
531
Sequence:
MEGESYNESTVNGTPVNHQALERHGLWEVITIAVVTAVVSLMTIVGNVLVMISFKVNSQLKTVNNYYLLSLACADLIIGIFSMNLYTTYILMGRWVLGSLACDLWLALDYVASNASVMNLLVISFDRYFSITRPLTYRAKRTPKRAGIMIGLAWLVSFILWAPAILCWQYLVGKRTVPPDECQIQFLSEPTITFGTAIAAFYIPVSVMTILYCRIYRETEKRTKDLADLQGSDSVAEAKKREPAQRTLLRSFFSCPRPSLAQRERNQASWSSSRRSTSTTGKTTQATDLSADWEKAEQVTTCSSYPSSEDEAKPTTDPVFQMVYKSEAKESPGKESNTQETKETVVNTRTENSDYDTPKYFLSPAAAHRLKSQKCVAYKFRLVVKADGTQETNNGCRKVKIMPCSFPVSKDPSTKGPDPNLSHQMTKRKRMVLVKERKAAQTLSAILLAFIITWTPYNIMVLVSTFCDKCVPVTLWHLGYWLCYVNSTINPICYALCNRTFRKTFKLLLLCRWKKKKVEEKLYWQGNSKLP
  
Inhibitor
Name:
BDBM50207463
Synonyms:
CHEMBL3963788
Type:
Small organic molecule
Emp. Form.:
C17H16F2N4O3S2
Mol. Mass.:
426.461
SMILES:
Cc1nnc2sc(C(=O)NCc3ccc(cc3)S(=O)(=O)C(F)F)c(N)c2c1C
Structure:
Search PDB for entries with ligand similarity: