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Target
Histamine H1 receptor
Ligand
BDBM87025
Substrate
n/a
Ki
10±n/a nM
Comments
PDSP_8619
Citation
 Fish, PV; Deur, C; Gan, X; Greene, K; Hoople, D; Mackenny, M; Para, KS; Reeves, K; Ryckmans, T; Stiff, C; Stobie, A; Wakenhut, F; Whitlock, GA Design and synthesis of morpholine derivatives. SAR for dual serotonin & noradrenaline reuptake inhibition. Bioorg Med Chem Lett 18:2562-6 (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:
BDBM87025
Synonyms:
(R)-2-((R)-(2,3-dihydrobenzofuran-7-yloxy)(phenyl)methyl)morpholine | (S)-2-((S)-(2,3-dihydrobenzofuran-7-yloxy)(phenyl)methyl)morpholine | CAS_44450154 | CAS_44450182 | NSC_44450154 | NSC_44450182
Type:
Small organic molecule
Emp. Form.:
C19H21NO3
Mol. Mass.:
311.3749
SMILES:
C1Cc2cccc(OC(C3CNCCO3)c3ccccc3)c2O1
Structure:
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