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TargetHistamine H1 receptor
LigandBDBM50001884
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1339952 (CHEMBL3243859)
Ki 1.000000±n/a nM
Citation Li, PZhang, QRobichaud, AJLee, TTomesch, JYao, WBeard, JDSnyder, GLZhu, HPeng, YHendrick, JPVanover, KEDavis, REMates, SWennogle, LP Discovery of a tetracyclic quinoxaline derivative as a potent and orally active multifunctional drug candidate for the treatment of neuropsychiatric and neurological disorders. J Med Chem57:2670-82 (2014) [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:
BDBM50001884
n/a
NameBDBM50001884
Synonyms:2-[4-(4-Methyl-benzyl)-piperazin-1-yl]-1-(2-methyl-2,3-dihydro-indol-1-yl)-ethanone | 3-Hydroxy-2-phenyl-propionic acid 8-methyl-8-aza-bicyclo[3.2.1]oct-3-yl ester | 3-chloro-6-(4-methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine | 8-Chloro-11-(4-methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine (Clozapine) | 8-Chloro-11-(4-methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine( Clozepine ) | 8-Chloro-11-(4-methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine(Ciozapine) | 8-Chloro-11-(4-methyl-piperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine(Clopazine) | 8-chloro-11-(4-methyl-piperazin-1-yl)-10H-dibenzo[b,e][1,4]diazepine | 8-chloro-11-(4-methylpiperazin-1-yl)-5H-dibenzo[b,e][1,4]diazepine | CHEMBL42 | CHEMBL538973 | CLOZAPINE | CLOZAPINE, 8-CHLORO-11-(4-METHYL-PIPERAZIN-1-YL)-5H-DIBENZO[B,E][1,4]DIAZEPINE | CLOZARIL | HF 1854 | US10167256, Clozapine | US10752588, Compound Clozapine | US11498896, Compound Clozapine
TypeSmall organic molecule
Emp. Form.C18H19ClN4
Mol. Mass.326.823
SMILESCN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2ccccc12 |t:8|
Structure
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