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TargetHistamine H4 receptor
LigandBDBM26391
Substrate/CompetitorBDBM7966
Meas. Tech.Radioligand Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 4±1 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 Chem51:6547-57 (2008) [PubMed]  Article
More Info.:Get all data from this article,   Solution Info,  Assay Method
 
Histamine H4 receptor
Name:Histamine H4 receptor
Synonyms:HH4R | 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:
BDBM26391
BDBM7966
NameBDBM26391
Synonyms:5-chloro-2-(piperazin-1-ylcarbonyl)-1H-indole | JNJ 7777120 analogue, 4
TypeSmall organic molecule
Emp. Form.C13H14ClN3O
Mol. Mass.263.723
SMILESClc1ccc2[nH]c(cc2c1)C(=O)N1CCNCC1
Structure
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