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TargetHistamine H3 receptor
LigandBDBM50496270
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1296757 (CHEMBL3132260)
IC50 1.7±n/a nM
Citation Brown, DGBernstein, PRGriffin, AWesolowski, SLabrecque, DTremblay, MCSylvester, MMauger, REdwards, PDThroner, SRFolmer, JJCacciola, JScott, CLazor, LAPourashraf, MSanthakumar, VPotts, WMSydserff, SGiguère, PLévesque, CDasser, MGroblewski, T Discovery of spirofused piperazine and diazepane amides as selective histamine-3 antagonists with in vivo efficacy in a mouse model of cognition. J Med Chem57:733-58 (2014) [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:
BDBM50496270
n/a
NameBDBM50496270
Synonyms:CHEMBL3127679
TypeSmall organic molecule
Emp. Form.C21H37N3O2
Mol. Mass.363.5374
SMILESCC(C)N1CCN(CC1)C(=O)C1CC2(C1)CCN(CC2)C1CCOCC1
Structure
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