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Target
Histamine H1 receptor
Ligand
BDBM35254
Substrate
n/a
Meas. Tech.
ChEBML_84431
Ki
7±n/a nM
Citation
 Calligaro, DO; Fairhurst, J; Hotten, TM; Moore, NA; Tupper, DE The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053) Bioorg Med Chem Lett 7:25-30 (1997)    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:
BDBM35254
Synonyms:
2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine | CHEMBL715 | Olansek | US8802672, Olanzapine | Zyprexa | olanzapine
Type:
Small organic molecule
Emp. Form.:
C17H20N4S
Mol. Mass.:
312.432
SMILES:
CN1CCN(CC1)C1=Nc2ccccc2Nc2sc(C)cc12 |t:8|
Structure:
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