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TargetHistamine H3 receptor
LigandBDBM50401001
Substrate/Competitorn/a
Meas. Tech.ChEMBL_879384 (CHEMBL2208782)
Ki 3.55±n/a nM
Citation Wager, TTPettersen, BASchmidt, AWSpracklin, DKMente, SButler, TWHoward, HLettiere, DJRubitski, DMWong, DFNedza, FMNelson, FRRollema, HRaggon, JWAubrecht, JFreeman, JKMarcek, JMCianfrogna, JCook, KWJames, LCChatman, LAIredale, PABanker, MJHomiski, MLMunzner, JBChandrasekaran, RY Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764). J Med Chem54:7602-20 (2011) [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:
BDBM50401001
n/a
NameBDBM50401001
Synonyms:CHEMBL2206288
TypeSmall organic molecule
Emp. Form.C20H30N2O
Mol. Mass.314.465
SMILESC([C@H]1C[C@H](C1)c1ccc(CN2CCCC2)cc1)N1CCOCC1 |r,wU:3.5,1.0,(12.44,-17.63,;13.93,-17.23,;14.7,-15.89,;16.03,-16.66,;15.26,-18,;17.52,-16.26,;18.61,-17.35,;20.1,-16.95,;20.5,-15.47,;21.98,-15.07,;23.07,-16.16,;22.83,-17.68,;24.2,-18.38,;25.29,-17.29,;24.59,-15.92,;19.41,-14.38,;17.92,-14.78,;11.35,-16.54,;11.75,-15.05,;10.66,-13.96,;9.18,-14.36,;8.78,-15.85,;9.87,-16.93,)|
Structure
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