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Target
Histamine H3 receptor
Ligand
BDBM50274235
Substrate
n/a
Meas. Tech.
ChEMBL_537241 (CHEMBL981856)
IC50
0.33±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 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:
BDBM50274235
Synonyms:
3-(4-[(1-Cyclobutyl-4-piperidinyl)oxy]phenyl)-2-methyl-5-(trifluoromethyl)-4(3H)-quinazolinone | CHEMBL485543
Type:
Small organic molecule
Emp. Form.:
C25H26F3N3O2
Mol. Mass.:
457.488
SMILES:
Cc1nc2cccc(c2c(=O)n1-c1ccc(OC2CCN(CC2)C2CCC2)cc1)C(F)(F)F
Structure:
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