Target
Histamine H1 receptor
Ligand
BDBM50240701
Substrate
n/a
Meas. Tech.
ChEBML_84431
Ki
22±n/a nM
Citation
 Calligaro, DOFairhurst, JHotten, TMMoore, NATupper, 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:
BDBM50240701
Synonyms:
2-Methyl-10-piperazin-1-yl-4H-3-thia-4,9-diaza-benzo[f]azulene | 4-Desmethylolanzapine | CHEMBL1125 | desmethylolanzapine | olanzapine, N-desmethyl
Type:
Small organic molecule
Emp. Form.:
C16H18N4S
Mol. Mass.:
298.406
SMILES:
Cc1cc2c(Nc3ccccc3N=C2N2CCNCC2)s1 |c:13|
Structure:
Search PDB for entries with ligand similarity: