Target
Histamine H1 receptor
Ligand
BDBM50035398
Substrate
n/a
Ki
>10000±n/a nM
Comments
PDSP_222
Citation
 Arneric, SPSullivan, JPBriggs, CADonnelly-Roberts, DAnderson, DJRaszkiewicz, JLHughes, MLCadman, EDAdams, PGarvey, DS (S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization. J Pharmacol Exp Ther 270:310-8 (1994) [PubMed] 
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:
BDBM50035398
Synonyms:
(S)-1-Methyl-2-(3-methyl-isoxazol-5-yl)-pyrrolidinium | (S)-3-methyl-5-(1-methylpyrrolidin-2-yl)isoxazole | 3-Methyl-5-((S)-1-methyl-pyrrolidin-2-yl)-isoxazole | ABT-418 | CHEMBL274525
Type:
Small organic molecule
Emp. Form.:
C9H14N2O
Mol. Mass.:
166.2203
SMILES:
CN1CCC[C@H]1c1cc(C)no1 |r|
Structure:
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