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TargetHistamine H3 receptor
LigandBDBM50318666
Substrate/Competitorn/a
Meas. Tech.ChEMBL_658561 (CHEMBL1247894)
IC50>10000±n/a nM
Citation Rottmann, MMcNamara, CYeung, BKLee, MCZou, BRussell, BSeitz, PPlouffe, DMDharia, NVTan, JCohen, SBSpencer, KRGonzález-Páez, GELakshminarayana, SBGoh, ASuwanarusk, RJegla, TSchmitt, EKBeck, HPBrun, RNosten, FRenia, LDartois, VKeller, THFidock, DAWinzeler, EADiagana, TT Spiroindolones, a potent compound class for the treatment of malaria. Science329:1175-80 (2010) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histamine H3 receptor
Name:Histamine H3 receptor
Synonyms:G-protein coupled receptor 97 | GPCR97 | HH3R | HISTAMINE H3 | HRH3 | HRH3_HUMAN | Histamine H3 receptor (H3) | Histamine H3L | Histamine receptor (H3 and H4)
Type:G Protein-Coupled Receptor (GPCR)
Mol. Mass.:48691.47
Organism:Homo sapiens (Human)
Description:Binding assays were using CHO cells stably expressing hH3R receptors.
Residue:445
Sequence:
MERAPPDGPLNASGALAGEAAAAGGARGFSAAWTAVLAALMALLIVATVLGNALVMLAFV
ADSSLRTQNNFFLLNLAISDFLVGAFCIPLYVPYVLTGRWTFGRGLCKLWLVVDYLLCTS
SAFNIVLISYDRFLSVTRAVSYRAQQGDTRRAVRKMLLVWVLAFLLYGPAILSWEYLSGG
SSIPEGHCYAEFFYNWYFLITASTLEFFTPFLSVTFFNLSIYLNIQRRTRLRLDGAREAA
GPEPPPEAQPSPPPPPGCWGCWQKGHGEAMPLHRYGVGEAAVGAEAGEATLGGGGGGGSV
ASPTSSSGSSSRGTERPRSLKRGSKPSASSASLEKRMKMVSQSFTQRFRLSRDRKVAKSL
AVIVSIFGLCWAPYTLLMIIRAACHGHCVPDYWYETSFWLLWANSAVNPVLYPLCHHSFR
RAFTKLLCPQKLKIQPHSSLEHCWK
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50318666
n/a
NameBDBM50318666
Synonyms:(1R,3S)-5',7-Dichloro-6-fluoro-3-methyl-2,3,4,9-tetrahydrospiro-[beta-carboline-1,3'-indol]-2'(1'H)-one | CHEMBL1082723 | NITD609
TypeSmall organic molecule
Emp. Form.C19H14Cl2FN3O
Mol. Mass.390.238
SMILESC[C@H]1Cc2c([nH]c3cc(Cl)c(F)cc23)[C@@]2(N1)C(=O)Nc1ccc(Cl)cc21 |r|
Structure
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