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TargetHistamine H4 Receptor
LigandBDBM26399
Substrate/CompetitorBDBM7966
Meas. Tech.Radioligand Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 1.45±0.1 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
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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BDBM26399
NameBDBM26399
Synonyms:14-fluoro-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 | 2,4-diamino-5,6-disubstituted pyrimidine, 13
TypeSmall organic molecule
Emp. Form.C17H20FN5
Mol. Mass.313.3726
SMILESNc1nc(N2CCNCC2)c2CCCc3ccc(F)cc3-c2n1
Structure
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BDBM7966
NameBDBM7966
Synonyms:2-(1H-imidazol-4-yl)ethan-1-amine | CHEMBL544208 | CHEMBL90 | Ceplene | Ergotidine | HISTAMINE | HISTAMINE DIHYDROCHLORIDE | Histamine | L-histamine | Peremin | [3H]histamine
TypeSmall organic molecule
Emp. Form.C5H9N3
Mol. Mass.111.1451
SMILESNCCc1cnc[nH]1
Structure
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