Reaction Details Report a problem with these data
Target
Histamine H4 receptor
Ligand
BDBM22558
Substrate
BDBM7966
Meas. Tech.
Radioligand Binding Assay
pH
7.5±n/a
Temperature
298.15±n/a K
Ki
28±n/a nM
Citation
Lee-Dutra, A; Arienti, KL; Buzard, DJ; Hack, MD; Khatuya, H; Desai, PJ; Nguyen, S; Thurmond, RL; Karlsson, L; Edwards, JP; Breitenbucher, JG Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands. Bioorg Med Chem Lett 16:6043-8 (2006) [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:
BDBM22558
Synonyms:
2-arylbenzimidazole derivative, 4 | 4-{2-chloro-4-[3-(4-methylpiperazin-1-yl)propoxy]phenyl}-3,5-diazatricyclo[7.4.0.0^{2,6}]trideca-1(9),2(6),3,7,10,12-hexaene
Type:
Small organic molecule
Emp. Form.:
C25H27ClN4O
Mol. Mass.:
434.961
SMILES:
CN1CCN(CCCOc2ccc(-c3nc4c(ccc5ccccc45)[nH]3)c(Cl)c2)CC1