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TargetHistamine H4 receptor
LigandBDBM22889
Substrate/CompetitorBDBM7966
Meas. Tech.H4R Radioligand Binding Assay
pH7.4±n/a
Temperature310.15±n/a K
Ki>10000±n/a nM
CommentsAnalysis of the [3H]histamine saturation binding yielded a Kd value of 11 +/- 1 and a Bmax value of 1.8 +/- 0.4 pmol/mg protein.
Citation Lim HDvan Rijn RMLing PBakker RAThurmond RLLeurs R Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist. J Pharmacol Exp Ther 314:1310-21 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   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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BDBM22889
BDBM7966
NameBDBM22889
Synonyms:(Cimetidine) N-Methyl-N''''-[2-(5-methyl-1H-imidazol-4-ylmethylsulfanyl)-ethyl]-guanidine,cyanide | (Cimetidine)N-methyl-N-[2-(5-methyl-1H-4-imidazolylmethylsulfanyl)ethyl]cyanomethyliminomethanediamine | (cimetidine) N-methyl-N-[2-(5-methyl-1H-4-imidazolylmethylsulfanyl)ethyl]cyanoiminomethanediamine | 1-cyano-2-methyl-3-(2-((5-methyl-1H-imidazol-4-yl)methylthio)ethyl)guanidine | 1-cyano-2-methyl-3-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]sulfanyl}ethyl)guanidine | 2-Chloro-5-(1-hydroxy-3-oxo-2,3-dihydro-1H-isoindol-1-yl)-benzenesulfonamide(Cimetidine) | 2-Methyl-8-phenethyl-imidazo[1,2-a]pyridine-3-carboxylic acid methyl ester(cimetidine) | 2-methylamino-2-[2-(4-methyl-1H-5-imidazolylmethylsulfanyl)ethylamino]-(E)-1-imino cyanide | 2-methylamino-2-[2-(5-methyl-1H-4-imidazolylmethylsulfanyl)ethylamino]-(Z)-1-imino cyanide(cimetidine) | ; N''''''''-cyano-N-methyl-N''''-(2-(((5-methyl-1H-imidazol-4-yl)methyl)thio)-ethyl)guanidine | CHEMBL30 | CIMETIDINE | Cimetidine | Eureceptor | N''''''''''''''''-cyano-N-methyl-N''''''''-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]thio}ethyl)guanidine | N''''''''-cyano-N-methyl-N''''-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]-lambda~4~-sulfanyl}ethyl)guanidine | N''''''''-cyano-N-methyl-N''''-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]thio}ethyl)guanidine | N''''''''-cyano-N-methyl-N''''-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]thio}ethyl)guanidine (Cimetidine) | N''''''''-cyano-N-methyl-N''''-(2-{[(5-methyl-1H-imidazol-4-yl)methyl]thio}ethyl)guanidine(cimetidine) | N''''''''-cyano-N-methyl-N''''-({[(5-methyl-1H-imidazol-4-yl)methyl]thio}methyl)guanidine(cimetidine) | N-Cyano-N''''-methyl-N''''''''-(2-(((5-methyl-1H-imidazol-4-yl) methyl)thio)ethyl)guanidine(Cimetidine) | N-Methyl-N''''-[2-(5-methyl-1H-imidazol-4-ylmethylsulfanyl)-ethyl]-N''''''''-Cyano-guanidine | N-Methyl-N''''-[2-(5-methyl-1H-imidazol-4-ylmethylsulfanyl)-ethyl]-N''''''''-cyano-guanidine(Cimetidine) | N-Methyl-N''''-[2-(5-methyl-1H-imidazol-4-ylmethylsulfanyl)-ethyl]-cyanoguanidine(cimetidine) | N-cyanomethyl-N''''-methyl-N''''''''-[2-(5-methyl-1H-imidazol-4-ylmethylsulfanyl)-ethyl]-guanidine ( Cimetidine) | N-methyl-N''''-cyano-N''''''''-[2-(5-methyl-1H-imidazol-4-ylmethylsulfanyl)-ethyl]-guanidine | N-methyl-N-[2-(5-methyl-1H-4-imidazolylmethylsulfanyl)ethyl]-1-cyanoiminomethanediamine | N-methyl-N-[2-(5-methyl-1H-4-imidazolylmethylsulfanyl)ethyl]cyanoiminomethanediamine (cimetidine) | N-methyl-N-[2-(5-methyl-1H-4-imidazolylmethylsulfanyl)ethyl]imino(-N-cyano)methanediaminem | N-tert-Butyl-N''''-[4-(1H-imidazol-4-yl)-phenyl]-formamidine(cimetidine) | Tagamet | Tagamet HB | Tagamet hb 200 | cemitidine
TypeSmall organic molecule
Emp. Form.C10H16N6S
Mol. Mass.252.339
SMILESCNC(NC#N)=NCCSCc1[nH]cnc1C |w:6.6|
Structure
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