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TargetHistamine H4 receptor
LigandBDBM26390
Substrate/CompetitorBDBM7966
Meas. Tech.Radioligand Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 5±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:AXOR35 | G-protein coupled receptor 105 | GPCR105 | GPRv53 | HH4R | HISTAMINE H4 | HRH4 | HRH4_HUMAN | Histamine H4 receptor | Histamine H4 receptor (H4R) | Histamine receptor (H3 and H4) | Pfi-013 | SP9144
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:44517.02
Organism:Homo sapiens (Human)
Description:Binding assays were using CHO cells stably expressing hH4R receptors.
Residue:390
Sequence:
MPDTNSTINLSLSTRVTLAFFMSLVAFAIMLGNALVILAFVVDKNLRHRSSYFFLNLAIS
DFFVGVISIPLYIPHTLFEWDFGKEICVFWLTTDYLLCTASVYNIVLISYDRYLSVSNAV
SYRTQHTGVLKIVTLMVAVWVLAFLVNGPMILVSESWKDEGSECEPGFFSEWYILAITSF
LEFVIPVILVAYFNMNIYWSLWKRDHLSRCQSHPGLTAVSSNICGHSFRGRLSSRRSLSA
STEVPASFHSERQRRKSSLMFSSRTKMNSNTIASKMGSFSQSDSVALHQREHVELLRARR
LAKSLAILLGVFAVCWAPYSLFTIVLSFYSSATGPKSVWYRIAFWLQWFNSFVNPLLYPL
CHKRFQKAFLKIFCIKKQPLPSQHSRSVSS
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  Blast E-value cutoff:
BDBM26390
BDBM7966
NameBDBM26390
Synonyms:4-(4-methylpiperazin-1-yl)-6-phenylpyrimidin-2-amine | 6-aryl-2-aminopyrimidine, 3
TypeSmall organic molecule
Emp. Form.C15H19N5
Mol. Mass.269.3449
SMILESCN1CCN(CC1)c1cc(nc(N)n1)-c1ccccc1
Structure
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