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TargetHistamine H4 receptor
LigandBDBM26226
Substrate/CompetitorBDBM7966
Meas. Tech.Radioligand Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 3.4±n/a nM
Citation Liu, HAltenbach, RJCarr, TLChandran, PHsieh, GCLewis, LGManelli, AMMilicic, IMarsh, KCMiller, TRStrakhova, MIVortherms, TAWakefield, BDWetter, JMWitte, DGHonore, PEsbenshade, TABrioni, JDCowart, MD cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia. J Med Chem51:7094-8 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Histamine H4 receptor
Name:Histamine H4 receptor
Synonyms:HH4R | HRH4_RAT | Hrh4
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:44045.07
Organism:Rattus norvegicus (rat)
Description:Cell pellets from SK-N-MC cells transfected with rat H4 receptor were used in binding assay.
Residue:391
Sequence:
MSESNGTDVLPLTAQVPLAFLMSLLAFAITIGNAVVILAFVADRNLRHRSNYFFLNLAIS
DFFVGVISIPLYIPHTLFNWNFGSGICMFWLITDYLLCTASVYSIVLISYDRYQSVSNAV
RYRAQHTGILKIVAQMVAVWILAFLVNGPMILASDSWKNSTNTEECEPGFVTEWYILAIT
AFLEFLLPVSLVVYFSVQIYWSLWKRGSLSRCPSHAGFIATSSRGTGHSRRTGLACRTSL
PGLKEPAASLHSESPRGKSSLLVSLRTHMSGSIIAFKVGSFCRSESPVLHQREHVELLRG
RKLARSLAVLLSAFAICWAPYCLFTIVLSTYRRGERPKSIWYSIAFWLQWFNSLINPFLY
PLCHRRFQKAFWKILCVTKQPAPSQTQSVSS
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  Blast E-value cutoff:
BDBM26226
BDBM7966
NameBDBM26226
Synonyms:(12S,17S)-6-(piperazin-1-yl)-11-oxa-3,5-diazatetracyclo[8.7.0.0^{2,7}.0^{12,17}]heptadeca-1(10),2(7),3,5-tetraen-4-amine | A-987306
TypeSmall organic molecule
Emp. Form.C18H25N5O
Mol. Mass.327.424
SMILES[H][C@]12CCCC[C@@]1([H])C1=C(CCc3c(nc(N)nc13)N1CCNCC1)O2 |r,t:9|
Structure
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