Target
Histamine H4 receptor
Ligand
BDBM50315346
Substrate
n/a
Meas. Tech.
ChEMBL_625969 (CHEMBL1103488)
IC50
1000±n/a nM
Citation
 Cramp, SDyke, HJHiggs, CClark, DEGill, MSavy, PJennings, NPrice, SLockey, PMNorman, DPorres, SWilson, FJones, ARamsden, NMangano, RLeggate, DAndersson, MHale, R Identification and hit-to-lead exploration of a novel series of histamine H4 receptor inverse agonists. Bioorg Med Chem Lett 20:2516-9 (2010) [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:
BDBM50315346
Synonyms:
8-chloro-4-(4-methylpiperazin-1-yl)benzofuro[3,2-d]pyrimidin-2-ol | CHEMBL1093438
Type:
Small organic molecule
Emp. Form.:
C15H15ClN4O2
Mol. Mass.:
318.758
SMILES:
CN1CCN(CC1)c1[nH]c(=O)nc2c3cc(Cl)ccc3oc12
Structure:
Search PDB for entries with ligand similarity: