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TargetHistamine H3 receptor
LigandBDBM50321499
Substrate/Competitorn/a
Meas. Tech.ChEMBL_640775 (CHEMBL1175767)
Ki 5.5±n/a nM
Citation Letavic, MAAluisio, LAtack, JRBonaventure, PCarruthers, NIDugovic, CEverson, AFeinstein, MAFraser, ICHoey, KJiang, XKeith, JMKoudriakova, TLeung, PLord, BLovenberg, TWLy, KSMorton, KLMotley, STNepomuceno, DRizzolio, MRynberg, RSepassi, KShelton, J Pre-clinical characterization of aryloxypyridine amides as histamine H3 receptor antagonists: identification of candidates for clinical development. Bioorg Med Chem Lett20:4210-4 (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:
BDBM50321499
n/a
NameBDBM50321499
Synonyms:(4-cyclobutyl-1,4-diazepan-1-yl)(5-(3-fluorophenoxy)pyridin-2-yl)methanone | CHEMBL1171154
TypeSmall organic molecule
Emp. Form.C21H24FN3O2
Mol. Mass.369.4326
SMILESFc1cccc(Oc2ccc(nc2)C(=O)N2CCCN(CC2)C2CCC2)c1
Structure
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