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TargetHistamine H3 receptor
LigandBDBM50325051
Substrate/Competitorn/a
Meas. Tech.ChEMBL_651627 (CHEMBL1228010)
IC50 2.2±n/a nM
Citation Davenport, AJStimson, CCCorsi, MVaidya, DGlenn, EJones, TDBailey, SGemkow, MJFritz, UHallett, DJ Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists. Bioorg Med Chem Lett20:5165-9 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histamine H3 receptor
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:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50325051
n/a
NameBDBM50325051
Synonyms:(2R)-4-((1-benzyl-1H-tetrazol-5-yl)(4-fluorophenyl)methyl)-1-cyclobutyl-2-methylpiperazine | CHEMBL1222946
TypeSmall organic molecule
Emp. Form.C24H29FN6
Mol. Mass.420.5257
SMILESC[C@@H]1CN(CCN1C1CCC1)C(c1nnnn1Cc1ccccc1)c1ccc(F)cc1 |r|
Structure
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