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Target
Histamine H1 receptor
Ligand
BDBM50295719
Substrate
n/a
Meas. Tech.
ChEMBL_577959 (CHEMBL1059632)
IC50
>1000±n/a nM
Citation
 Kubota, K; Kurebayashi, H; Miyachi, H; Tobe, M; Onishi, M; Isobe, Y Synthesis and structure-activity relationships of phenothiazine carboxylic acids having pyrimidine-dione as novel histamine H(1) antagonists. Bioorg Med Chem Lett 19:2766-71 (2009) [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:
BDBM50295719
Synonyms:
5-chloro-2-(1-(3-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-ylamino)propyl)piperidin-4-yloxy)benzoic acid | CHEMBL562638
Type:
Small organic molecule
Emp. Form.:
C21H27ClN4O5
Mol. Mass.:
450.916
SMILES:
Cn1c(NCCCN2CCC(CC2)Oc2ccc(Cl)cc2C(O)=O)cc(=O)n(C)c1=O
Structure:
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