Reaction Details Report a problem with these data
Target
Histamine H1 receptor
Ligand
BDBM50262939
Substrate
n/a
Meas. Tech.
ChEMBL_489018 (CHEMBL986359)
IC50
>10000±n/a nM
Citation
 Nagase, T; Mizutani, T; Ishikawa, S; Sekino, E; Sasaki, T; Fujimura, T; Ito, S; Mitobe, Y; Miyamoto, Y; Yoshimoto, R; Tanaka, T; Ishihara, A; Takenaga, N; Tokita, S; Fukami, T; Sato, N Synthesis, structure-activity relationships, and biological profiles of a quinazolinone class of histamine H3 receptor inverse agonists. J Med Chem 51:4780-9 (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:
BDBM50262939
Synonyms:
2-Methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-5-(trifluoromethyl)-4(3H)-quinazolinone | CHEMBL476323
Type:
Small organic molecule
Emp. Form.:
C23H24F3N3O2
Mol. Mass.:
431.4508
SMILES:
Cc1nc2cccc(c2c(=O)n1-c1ccc(OCCCN2CCCC2)cc1)C(F)(F)F
Structure:
Search PDB for entries with ligand similarity: