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TargetHistamine H4 Receptor
LigandBDBM26398
Substrate/CompetitorBDBM7966
Meas. Tech.Radioligand Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 3.6±0.6 nM
Citation Cowart MDAltenbach RJLiu HHsieh GCDrizin IMilicic IMiller TRWitte DGWishart NFix-Stenzel SRMcPherson MJAdair RMWetter JMBettencourt BMMarsh KCSullivan JPHonore PEsbenshade TABrioni JD Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models. J Med Chem 51:6547-57 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Histamine H4 Receptor
Name:Histamine H4 Receptor
Synonyms:HH4R
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:
BDBM26398
BDBM7966
NameBDBM26398
Synonyms:2,4-diamino-5,6-disubstituted pyrimidine, 12 | 6-[3-(methylamino)azetidin-1-yl]-3,5-diazatricyclo[9.4.0.0^{2,7}]pentadeca-1(15),2(7),3,5,11,13-hexaen-4-amine
TypeSmall organic molecule
Emp. Form.C17H21N5
Mol. Mass.295.3821
SMILESCNC1CN(C1)c1nc(N)nc-2c1CCCc1ccccc-21
Structure
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