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Target
Muscarinic acetylcholine receptor M5
Ligand
BDBM50023229
Substrate
n/a
Meas. Tech.
ChEMBL_1457828 (CHEMBL3370306)
EC50
610±n/a nM
Citation
 Gentry, PR; Kokubo, M; Bridges, TM; Noetzel, MJ; Cho, HP; Lamsal, A; Smith, E; Chase, P; Hodder, PS; Niswender, CM; Daniels, JS; Conn, PJ; Lindsley, CW; Wood, MR Development of a highly potent, novel M5 positive allosteric modulator (PAM) demonstrating CNS exposure: 1-((1H-indazol-5-yl)sulfoneyl)-N-ethyl-N-(2-(trifluoromethyl)benzyl)piperidine-4-carboxamide (ML380). J Med Chem 57:7804-10 (2014) [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:
BDBM50023229
Synonyms:
CHEMBL3329755
Type:
Small organic molecule
Emp. Form.:
C23H25F3N4O3S
Mol. Mass.:
494.53
SMILES:
CCN(Cc1ccccc1C(F)(F)F)C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2[nH]ncc2c1
Structure:
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