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TargetHistamine H1 receptor
LigandBDBM35254
Substrate/Competitorn/a
Meas. Tech.ChEBML_84716
Ki 4.3±n/a nM
Citation Campiani, GButini, SFattorusso, CCatalanotti, BGemma, SNacci, VMorelli, ECagnotto, AMereghetti, IMennini, TCarli, MMinetti, PDi Cesare, MAMastroianni, DScafetta, NGalletti, BStasi, MACastorina, MPacifici, LVertechy, MDi Serio, SGhirardi, OTinti, OCarminati, P Pyrrolo[1,3]benzothiazepine-based serotonin and dopamine receptor antagonists. Molecular modeling, further structure-activity relationship studies, and identification of novel atypical antipsychotic agents. J Med Chem47:143-57 (2003) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histamine H1 receptor
Name:Histamine H1 receptor
Synonyms:HISTAMINE H1 | HRH1_RAT | Hrh1
Type:Enzyme Catalytic Domain
Mol. Mass.:55716.35
Organism:RAT
Description:HISTAMINE H1 HRH1 RAT::P31390
Residue:486
Sequence:
MSFANTSSTFEDKMCEGNRTAMASPQLLPLVVVLSSISLVTVGLNLLVLYAVHSERKLHT
VGNLYIVSLSVADLIVGAVVMPMNILYLIMTKWSLGRPLCLFWLSMDYVASTASIFSVFI
LCIDRYRSVQQPLRYLRYRTKTRASATILGAWFFSFLWVIPILGWHHFMPPAPELREDKC
ETDFYNVTWFKIMTAIINFYLPTLLMLWFYVKIYKAVRRHCQHRQLTNGSLPSFSELKLR
SDDTKEGAKKPGRESPWGVLKRPSRDPSVGLDQKSTSEDPKMTSPTVFSQEGERETRPCF
RLDIMQKQSVAEGDVRGSKANDQALSQPKMDEQSLNTCRRISETSEDQTLVDQQSFSRTT
DSDTSIEPGPGRVKSRSGSNSGLDYIKITWKRLRSHSRQYVSGLHLNRERKAAKQLGFIM
AAFILCWIPYFIFFMVIAFCKSCCSEPMHMFTIWLGYINSTLNPLIYPLCNENFKKTFKK
ILHIRS
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  Blast E-value cutoff:
BDBM35254
n/a
NameBDBM35254
Synonyms:2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine | CHEMBL715 | Olansek | US8802672, Olanzapine | Zyprexa | olanzapine
TypeSmall organic molecule
Emp. Form.C17H20N4S
Mol. Mass.312.432
SMILESCN1CCN(CC1)C1=Nc2ccccc2Nc2sc(C)cc12 |t:8|
Structure
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