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Target
Histamine H1 receptor
Ligand
BDBM27213
Substrate
n/a
Meas. Tech.
ChEMBL_1280381 (CHEMBL3095541)
Ki
>2512±n/a nM
Citation
 Wilson, DM; Apps, J; Bailey, N; Bamford, MJ; Beresford, IJ; Briggs, MA; Calver, AR; Crook, B; Davis, RP; Davis, S; Dean, DK; Harris, L; Heightman, TD; Panchal, T; Parr, CA; Quashie, N; Steadman, JG; Schogger, J; Sehmi, SS; Stean, TO; Takle, AK; Trail, BK; White, T; Witherington, J; Worby, A; Medhurst, AD The discovery of the benzazepine class of histamine H3 receptor antagonists. Bioorg Med Chem Lett 23:6897-901 (2013) [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:
BDBM27213
Synonyms:
4-[3-(4-cyclopropanecarbonylphenoxy)propyl]-1H-imidazole | CHEMBL14638 | CHEMBL1795025 | Ciproxifan
Type:
Small organic molecule
Emp. Form.:
C16H18N2O2
Mol. Mass.:
270.3263
SMILES:
O=C(C1CC1)c1ccc(OCCCc2cnc[nH]2)cc1
Structure:
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