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TargetHistamine H4 receptor
LigandBDBM26395
Substrate/CompetitorBDBM7966
Meas. Tech.Radioligand Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 71±15 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:AXOR35 | G-protein coupled receptor 105 | GPRv53 | HH4R | HISTAMINE H4 | 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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BDBM26395
BDBM7966
NameBDBM26395
Synonyms:2,4-diamino-5,6-disubstituted pyrimidine, 9 | 6-(piperazin-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
SMILESNc1nc(N2CCNCC2)c2CCCc3ccccc3-c2n1
Structure
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