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Reaction Details
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TargetHistamine H3 receptor
LigandBDBM50361224
Substrate/Competitorn/a
Meas. Tech.ChEMBL_794859 (CHEMBL1936095)
Ki 1.3±n/a nM
Citation Semple, GSantora, VJSmith, JMCovel, JAHayashi, RGallardo, CIbarra, JBSchultz, JAPark, DMEstrada, SAHofilena, BJSmith, BMRen, ASuarez, MFrazer, JEdwards, JEHart, RHauser, EKLorea, JGrottick, AJ Identification of biaryl sulfone derivatives as antagonists of the histamine H3 receptor: discovery of (R)-1-(2-(4'-(3-methoxypropylsulfonyl)biphenyl-4-yl)ethyl)-2-methylpyrrolidine (APD916). Bioorg Med Chem Lett22:71-5 (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:
BDBM50361224
n/a
NameBDBM50361224
Synonyms:CHEMBL1934354
TypeSmall organic molecule
Emp. Form.C20H25NO2S
Mol. Mass.343.483
SMILESC[C@@H]1CCCN1CCc1ccc(cc1)-c1ccc(cc1)S(C)(=O)=O |r|
Structure
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