Target
Muscarinic acetylcholine receptor M5
Ligand
BDBM50268343
Substrate
n/a
Meas. Tech.
ChEMBL_1704880 (CHEMBL4056113)
IC50
>10000±n/a nM
Citation
 Bender, AMWeiner, RLLuscombe, VBAjmera, SCho, HPChang, SZhan, XRodriguez, ALNiswender, CMEngers, DWBridges, TMConn, PJLindsley, 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 Lett 27:3576-3581 (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:
BDBM50268343
Synonyms:
CHEMBL4096727
Type:
Small organic molecule
Emp. Form.:
C20H26ClN5O2S
Mol. Mass.:
435.971
SMILES:
C[C@H]1CCCCN1c1ccc(nn1)N1CCN(CC1)S(=O)(=O)c1ccccc1Cl |r|
Structure:
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