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Target
Histamine H4 receptor
Ligand
BDBM50191289
Substrate
n/a
Meas. Tech.
ChEMBL_556996 (CHEMBL958182)
Ki
28.18±n/a nM
Citation
 Smits, RA; de Esch, IJ; Zuiderveld, OP; Broeker, J; Sansuk, K; Guaita, E; Coruzzi, G; Adami, M; Haaksma, E; Leurs, R Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach. J Med Chem 51:7855-65 (2008) [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:
BDBM50191289
Synonyms:
7-chloro-11-(4-methyl-piperazin-1-yl)-dibenzo[b,f][1,4]oxazepine | 7-chloro-11-(4-methylpiperazin-1-yl)-dibenzo[b,f][1,4]oxazepine | 7-chloro-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepine | CHEMBL213912 | VUF-6884
Type:
Small organic molecule
Emp. Form.:
C18H18ClN3O
Mol. Mass.:
327.808
SMILES:
CN1CCN(CC1)C1=Nc2ccc(Cl)cc2Oc2ccccc12 |t:8|
Structure:
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