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Target
Histamine H1 receptor
Ligand
BDBM50371974
Substrate
n/a
Meas. Tech.
ChEMBL_464412 (CHEMBL931079)
Ki
18.3±n/a nM
Citation
 Peters, JU; Lübbers, T; Alanine, A; Kolczewski, S; Blasco, F; Steward, L Cyclic guanidines as dual 5-HT5A/5-HT7 receptor ligands: optimising brain penetration. Bioorg Med Chem Lett 18:262-6 (2008) [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:
BDBM50371974
Synonyms:
CHEMBL256047
Type:
Small organic molecule
Emp. Form.:
C11H11Cl2F2N3
Mol. Mass.:
294.128
SMILES:
C[C@H]1NC(NCC(F)F)=Nc2ccc(Cl)c(Cl)c12 |c:8|
Structure:
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