Reaction Details Report a problem with these data
Target
Histamine H4 receptor
Ligand
BDBM22870
Substrate
BDBM7966
Meas. Tech.
H4R Radioligand Binding Assay
pH
7.4±n/a
Temperature
310.15±n/a K
Ki
5012±1031 nM
Comments
Analysis 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, 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
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:
BDBM22870
Synonyms:
13-chloro-10-(piperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,9,12,14-heptaene | 2-chloro-11-piperazin-1-yldibenzo[b,f][1,4]oxazepine | Amoxapine | Asendin | CHEMBL1113 | Demolox
Type:
Small organic molecule
Emp. Form.:
C17H16ClN3O
Mol. Mass.:
313.781
SMILES:
Clc1ccc2Oc3ccccc3N=C(N3CCNCC3)c2c1 |t:13|