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Target
Histamine H1 receptor
Ligand
BDBM50343584
Substrate
n/a
Meas. Tech.
ChEMBL_745951 (CHEMBL1775250)
IC50
325±n/a nM
Citation
 Kubota, K; Kurebayashi, H; Miyachi, H; Tobe, M; Onishi, M; Isobe, Y Synthesis and structure-activity relationship of tricyclic carboxylic acids as novel anti-histamines. Bioorg Med Chem 19:3005-21 (2011) [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:
BDBM50343584
Synonyms:
(Z)-11-(3-(4-(1,3-Dimethyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl)piperazin-1-yl)propylidene)-6,11-dihydrodibenzo[b,e]oxepine-2-carboxylic acid | CHEMBL1774503
Type:
Small organic molecule
Emp. Form.:
C28H30N4O5
Mol. Mass.:
502.5616
SMILES:
Cn1c(cc(=O)n(C)c1=O)N1CCN(CC\C=C2\c3ccccc3COc3ccc(cc23)C(O)=O)CC1
Structure:
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