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TargetMuscarinic acetylcholine receptor M5
LigandBDBM50023269
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1457820 (CHEMBL3370062)
EC50 120±n/a nM
Citation Gentry, PRKokubo, MBridges, TMNoetzel, MJCho, HPLamsal, ASmith, EChase, PHodder, PSNiswender, CMDaniels, JSConn, PJLindsley, CWWood, 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 Chem57:7804-10 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Muscarinic acetylcholine receptor M5
Name:Muscarinic acetylcholine receptor M5
Synonyms:ACM5_HUMAN | CHRM5
Type:PROTEIN
Mol. Mass.:60102.35
Organism:Homo sapiens (Human)
Description:ChEMBL_1517990
Residue:532
Sequence:
MEGDSYHNATTVNGTPVNHQPLERHRLWEVITIAAVTAVVSLITIVGNVLVMISFKVNSQ
LKTVNNYYLLSLACADLIIGIFSMNLYTTYILMGRWALGSLACDLWLALDYVASNASVMN
LLVISFDRYFSITRPLTYRAKRTPKRAGIMIGLAWLISFILWAPAILCWQYLVGKRTVPL
DECQIQFLSEPTITFGTAIAAFYIPVSVMTILYCRIYRETEKRTKDLADLQGSDSVTKAE
KRKPAHRALFRSCLRCPRPTLAQRERNQASWSSSRRSTSTTGKPSQATGPSANWAKAEQL
TTCSSYPSSEDEDKPATDPVLQVVYKSQGKESPGEEFSAEETEETFVKAETEKSDYDTPN
YLLSPAAAHRPKSQKCVAYKFRLVVKADGNQETNNGCHKVKIMPCPFPVAKEPSTKGLNP
NPSHQMTKRKRVVLVKERKAAQTLSAILLAFIITWTPYNIMVLVSTFCDKCVPVTLWHLG
YWLCYVNSTVNPICYALCNRTFRKTFKMLLLCRWKKKKVEEKLYWQGNSKLP
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50023269
n/a
NameBDBM50023269
Synonyms:CHEMBL3329765
TypeSmall organic molecule
Emp. Form.C25H27F3N4O3S
Mol. Mass.520.567
SMILESFC(F)(F)c1ccccc1CN(CC1CC1)C(=O)C1CCN(CC1)S(=O)(=O)c1ccc2[nH]ncc2c1
Structure
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