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Target
Histamine H4 receptor
Ligand
BDBM22541
Substrate
BDBM7966
Meas. Tech.
H4R Radioligand Binding Assay
Ki
8±n/a nM
Citation
Lim, HD; van Rijn, RM; Ling, P; Bakker, RA; Thurmond, RL; Leurs, 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.:
Target
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:
MPDTNSTINLSLSTRVTLAFFMSLVAFAIMLGNALVILAFVVDKNLRHRSSYFFLNLAISDFFVGVISIPLYIPHTLFEWDFGKEICVFWLTTDYLLCTASVYNIVLISYDRYLSVSNAVSYRTQHTGVLKIVTLMVAVWVLAFLVNGPMILVSESWKDEGSECEPGFFSEWYILAITSFLEFVIPVILVAYFNMNIYWSLWKRDHLSRCQSHPGLTAVSSNICGHSFRGRLSSRRSLSASTEVPASFHSERQRRKSSLMFSSRTKMNSNTIASKMGSFSQSDSVALHQREHVELLRARRLAKSLAILLGVFAVCWAPYSLFTIVLSFYSSATGPKSVWYRIAFWLQWFNSFVNPLLYPLCHKRFQKAFLKIFCIKKQPLPSQHSRSVSS
Inhibitor
Name:
BDBM22541
Synonyms:
Clobenpropit | N''-[(4-chlorophenyl)methyl]{[3-(1H-imidazol-5-yl)propyl]sulfanyl}methanimidamide | VUF 9153 | VUF-9153 | VUF9153
Type:
Small organic molecule
Emp. Form.:
C14H17ClN4S
Mol. Mass.:
308.83
SMILES:
NC(SCCCc1cnc[nH]1)=NCc1ccc(Cl)cc1 |w:11.12|