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Target
Muscarinic acetylcholine receptor M5
Ligand
BDBM50305822
Substrate
n/a
Meas. Tech.
ChEMBL_605048 (CHEMBL1071910)
EC50
3300±n/a nM
Citation
 Bridges, TM; Kennedy, JP; Cho, HP; Breininger, ML; Gentry, PR; Hopkins, CR; Conn, PJ; Lindsley, CW Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM. Bioorg Med Chem Lett 20:558-62 (2010) [PubMed]  Article 
Target
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:
MEGDSYHNATTVNGTPVNHQPLERHRLWEVITIAAVTAVVSLITIVGNVLVMISFKVNSQLKTVNNYYLLSLACADLIIGIFSMNLYTTYILMGRWALGSLACDLWLALDYVASNASVMNLLVISFDRYFSITRPLTYRAKRTPKRAGIMIGLAWLISFILWAPAILCWQYLVGKRTVPLDECQIQFLSEPTITFGTAIAAFYIPVSVMTILYCRIYRETEKRTKDLADLQGSDSVTKAEKRKPAHRALFRSCLRCPRPTLAQRERNQASWSSSRRSTSTTGKPSQATGPSANWAKAEQLTTCSSYPSSEDEDKPATDPVLQVVYKSQGKESPGEEFSAEETEETFVKAETEKSDYDTPNYLLSPAAAHRPKSQKCVAYKFRLVVKADGNQETNNGCHKVKIMPCPFPVAKEPSTKGLNPNPSHQMTKRKRVVLVKERKAAQTLSAILLAFIITWTPYNIMVLVSTFCDKCVPVTLWHLGYWLCYVNSTVNPICYALCNRTFRKTFKMLLLCRWKKKKVEEKLYWQGNSKLP
  
Inhibitor
Name:
BDBM50305822
Synonyms:
1-(4-(1-methyl-1H-pyrazol-4-yl)benzyl)-5-(trifluoromethoxy)indoline-2,3-dione | CHEMBL596510
Type:
Small organic molecule
Emp. Form.:
C20H14F3N3O3
Mol. Mass.:
401.3387
SMILES:
Cn1cc(cn1)-c1ccc(CN2C(=O)C(=O)c3cc(OC(F)(F)F)ccc23)cc1
Structure:
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