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TargetHistamine H1 receptor
LigandBDBM50131346
Substrate/Competitorn/a
Meas. Tech.ChEMBL_303340 (CHEMBL840156)
Ki 113±n/a nM
Citation Andrés, JIAlcázar, JAlonso, JMAlvarez, RMBakker, MHBiesmans, ICid, JMDe Lucas, AIFernández, JFont, LMHens, KAIturrino, LLenaerts, IMartínez, SMegens, AAPastor, JVermote, PCSteckler, T Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity. J Med Chem48:2054-71 (2005) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histamine H1 receptor
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:
MSLPNSSCLLEDKMCEGNKTTMASPQLMPLVVVLSTICLVTVGLNLLVLYAVRSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLLMSKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLKYRTKTRASATILGAWFLSFLWVIPILGWNHFMQQTSVRREDKC
ETDFYDVTWFKVMTAIINFYLPTLLMLWFYAKIYKAVRQHCQHRELINRSLPSFSEIKLR
PENPKGDAKKPGKESPWEVLKRKPKDAGGGSVLKSPSQTPKEMKSPVVFSQEDDREVDKL
YCFPLDIVHMQAAAEGSSRDYVAVNRSHGQLKTDEQGLNTHGASEISEDQMLGDSQSFSR
TDSDTTTETAPGKGKLRSGSNTGLDYIKFTWKRLRSHSRQYVSGLHMNRERKAAKQLGFI
MAAFILCWIPYFIFFMVIAFCKNCCNEHLHMFTIWLGYINSTLNPLIYPLCNENFKKTFK
RILHIRS
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  Blast E-value cutoff:
BDBM50131346
n/a
NameBDBM50131346
Synonyms:(3R,3aS)-7,8-Dimethoxy-3-[4-((E)-2-methyl-3-phenyl-allyl)-piperazin-1-ylmethyl]-3a,4-dihydro-3H-chromeno[4,3-c]isoxazole | (3R,3aS)-7,8-Dimethoxy-3-[4-(2-methyl-3-phenyl-allyl)-piperazin-1-ylmethyl]-3a,4-dihydro-3H-chromeno[4,3-c]isoxazole | CHEMBL91157
TypeSmall organic molecule
Emp. Form.C27H33N3O4
Mol. Mass.463.5686
SMILESCOc1cc2OC[C@H]3[C@H](CN4CCN(C\C(C)=C\c5ccccc5)CC4)ON=C3c2cc1OC |c:29|
Structure
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