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Target
Histamine H3 receptor
Ligand
BDBM50325087
Substrate
n/a
Meas. Tech.
ChEMBL_651627 (CHEMBL1228010)
IC50
0.5±n/a nM
Citation
 Davenport, AJ; Stimson, CC; Corsi, M; Vaidya, D; Glenn, E; Jones, TD; Bailey, S; Gemkow, MJ; Fritz, U; Hallett, DJ Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists. Bioorg Med Chem Lett 20:5165-9 (2010) [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:
BDBM50325087
Synonyms:
1-((1-benzyl-1H-tetrazol-5-yl)(4-(4-methylpiperazin-1-yl)phenyl)methyl)-4-cyclobutyl-1,4-diazepane | CHEMBL1222434
Type:
Small organic molecule
Emp. Form.:
C29H40N8
Mol. Mass.:
500.6815
SMILES:
CN1CCN(CC1)c1ccc(cc1)C(N1CCCN(CC1)C1CCC1)c1nnnn1Cc1ccccc1
Structure:
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