Target
Histamine H1 receptor
Ligand
BDBM50155336
Substrate
n/a
Meas. Tech.
ChEMBL_302919 (CHEMBL830379)
Ki
26±n/a nM
Citation
 Lewis, TAYoung, MAArrington, MPBayless, LCai, XCollart, PEckman, JBEllis, JLEne, DGLibertine, LNicolas, JMScannell, RTWels, BFWenberg, KWypij, DM Cetirizine and loratadine-based antihistamines with 5-lipoxygenase inhibitory activity. Bioorg Med Chem Lett 14:5591-4 (2004) [PubMed]  Article 
Target
Name:
Histamine H1 receptor
Synonyms:
H1R | HH1R | HISTAMINE H1 | HRH1 | HRH1_HUMAN
Type:
G Protein-Coupled Receptor (GPCR)
Mol. Mass.:
55808.72
Organism:
Homo sapiens (Human)
Description:
Cell pellets from SK-N-MC cells transfected with human H1 receptor were used in binding assay.
Residue:
487
Sequence:
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHTVGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFILCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKCETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLRPENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKLYCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSRTDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFIMAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFKRILHIRS
  
Inhibitor
Name:
BDBM50155336
Synonyms:
1-{4-[4-(4-{4-[bis(4-fluorophenyl)methyl]piperazin-1-yl}butoxy)phenyl]but-3-yn-1-yl}-1-hydroxyurea | CHEMBL444083 | N-hydroxycarbamate derivative
Type:
Small organic molecule
Emp. Form.:
C32H36F2N4O3
Mol. Mass.:
562.65
SMILES:
NC(=O)N(O)CCC#Cc1ccc(OCCCCN2CCN(CC2)C(c2ccc(F)cc2)c2ccc(F)cc2)cc1
Structure:
Search PDB for entries with ligand similarity: