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Target
Histamine H3 receptor
Ligand
BDBM50246244
Substrate
n/a
Meas. Tech.
ChEMBL_558277 (CHEMBL956577)
IC50
0.87±n/a nM
Citation
 Mizutani, T; Nagase, T; Ito, S; Miyamoto, Y; Tanaka, T; Takenaga, N; Tokita, S; Sato, N Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists. Bioorg Med Chem Lett 18:6041-5 (2008) [PubMed]  Article 
Target
Name:
Histamine H3 receptor
Synonyms:
G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4)
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
48691.47
Organism:
Homo sapiens (Human)
Description:
Binding assays were using CHO cells stably expressing hH3R receptors.
Residue:
445
Sequence:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFVADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTSSAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGGSSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAAGPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSVASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSLAVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFRRAFTKLLCPQKLKIQPHSSLEHCWK
  
Inhibitor
Name:
BDBM50246244
Synonyms:
3-isopropyl-2-(4-(3-(piperidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-one | CHEMBL488251
Type:
Small organic molecule
Emp. Form.:
C25H31N3O2
Mol. Mass.:
405.5325
SMILES:
CC(C)n1c(nc2ccccc2c1=O)-c1ccc(OCCCN2CCCCC2)cc1
Structure:
Search PDB for entries with ligand similarity: