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Target
Histamine H1 receptor
Ligand
BDBM50274692
Substrate
n/a
Meas. Tech.
ChEMBL_537282 (CHEMBL985378)
IC50
>10000±n/a nM
Citation
 Nagase, T; Mizutani, T; Sekino, E; Ishikawa, S; Ito, S; Mitobe, Y; Miyamoto, Y; Yoshimoto, R; Tanaka, T; Ishihara, A; Takenaga, N; Tokita, S; Sato, N Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists. J Med Chem 51:6889-901 (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:
BDBM50274692
Synonyms:
3-(4-[(1-Cyclobutyl-4-piperidinyl)oxy]phenyl)-5-fluoro-2-methyl-4(3H)-quinazolinone | CHEMBL483400
Type:
Small organic molecule
Emp. Form.:
C24H26FN3O2
Mol. Mass.:
407.4805
SMILES:
Cc1nc2cccc(F)c2c(=O)n1-c1ccc(OC2CCN(CC2)C2CCC2)cc1
Structure:
Search PDB for entries with ligand similarity: