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Target
Histamine H1 receptor
Ligand
BDBM50261729
Substrate
n/a
Meas. Tech.
ChEMBL_514298 (CHEMBL979128)
EC50
>50000±n/a nM
Citation
 DiMauro, EF; Buchanan, JL; Cheng, A; Emkey, R; Hitchcock, SA; Huang, L; Huang, MY; Janosky, B; Lee, JH; Li, X; Martin, MW; Tomlinson, SA; White, RD; Zheng, XM; Patel, VF; Fremeau, RT Structural modifications of N-arylamide oxadiazoles: Identification of N-arylpiperidine oxadiazoles as potent and selective agonists of CB2. Bioorg Med Chem Lett 18:4267-74 (2008) [PubMed]  Article 
Target
Name:
Histamine H1 receptor
Synonyms:
H1R | HH1R | HISTAMINE H1 | HRH1 | HRH1_HUMAN
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
55808.72
Organism:
Homo sapiens (Human)
Description:
Cell pellets from SK-N-MC cells transfected with human H1 receptor were used in binding assay.
Residue:
487
Sequence:
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLRPENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKLYCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSRTDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFKRILHIRS
  
Inhibitor
Name:
BDBM50261729
Synonyms:
6-chloro-3-(4-(3-(2-chloro-4-fluorophenyl)-1,2,4-oxadiazol-5-yl)piperidin-1-yl)quinoline | CHEMBL468176
Type:
Small organic molecule
Emp. Form.:
C22H17Cl2FN4O
Mol. Mass.:
443.301
SMILES:
Fc1ccc(-c2noc(n2)C2CCN(CC2)c2cnc3ccc(Cl)cc3c2)c(Cl)c1
Structure:
Search PDB for entries with ligand similarity: