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TargetHistamine H3 receptor
LigandBDBM50346209
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1277742 (CHEMBL3097342)
Ki 0.832000±n/a nM
Citation Wilson, DMApps, JBailey, NBamford, MJBeresford, IJBrackenborough, KBriggs, MABrough, SCalver, ARCrook, BDavis, RKDavis, RPDavis, SDean, DKHarris, LHeslop, THolland, VJeffrey, PPanchal, TAParr, CAQuashie, NSchogger, JSehmi, SSStean, TOSteadman, JGTrail, BWald, JWorby, ATakle, AKWitherington, JMedhurst, AD Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists. Bioorg Med Chem Lett23:6890-6 (2013) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histamine H3 receptor
Name:Histamine H3 receptor
Synonyms:HH3R | HRH3_RAT | Hrh3
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:48607.98
Organism:Rattus norvegicus (rat)
Description:n/a
Residue:445
Sequence:
MERAPPDGLMNASGTLAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCAS
SVFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMALVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGGREAG
PEPPPDAQPSPPPAPPSCWGCWPKGHGEAMPLHRYGVGEAGPGVEAGEAALGGGSGGGAA
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSITQRFRLSRDKKVAKSL
AIIVSIFGLCWAPYTLLMIIRAACHGRCIPDYWYETSFWLLWANSAVNPVLYPLCHYSFR
RAFTKLLCPQKLKVQPHGSLEQCWK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50346209
n/a
NameBDBM50346209
Synonyms:5-(3-cyclobutyl-2,3,4,5-tetrahydro-1H-benzo[d]azepin-7-yloxy)-N-methylpyrazine-2-carboxamide | CHEMBL1783890
TypeSmall organic molecule
Emp. Form.C20H24N4O2
Mol. Mass.352.4302
SMILESCNC(=O)c1cnc(Oc2ccc3CCN(CCc3c2)C2CCC2)cn1
Structure
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