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TargetHistamine H3 receptor
LigandBDBM50352091
Substrate/Competitorn/a
Meas. Tech.ChEMBL_766550 (CHEMBL1827031)
Ki 0.67±n/a nM
Citation Labeeuw, OLevoin, NPoupardin-Olivier, OCalmels, TLigneau, XBerrebi-Bertrand, IRobert, PLecomte, JMSchwartz, JCCapet, M Novel and highly potent histamine H3 receptor ligands. Part 2: exploring the cyclohexylamine-based series. Bioorg Med Chem Lett21:5384-8 (2011) [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:
BDBM50352091
n/a
NameBDBM50352091
Synonyms:CHEMBL1824240
TypeSmall organic molecule
Emp. Form.C24H38N2O2
Mol. Mass.386.5707
SMILESC(COc1ccc(cc1)[C@@H]1CC[C@@H](CC1)N1CCOCC1)CN1CCCCC1 |r,wU:9.9,12.16,(-3.9,-23.3,;-2.36,-23.3,;-1.59,-21.97,;-.05,-21.97,;.71,-23.31,;2.25,-23.32,;3.03,-21.99,;2.26,-20.65,;.71,-20.64,;4.57,-22,;5.33,-23.34,;6.86,-23.36,;7.65,-22.03,;6.89,-20.69,;5.34,-20.67,;9.19,-22.04,;9.94,-23.38,;11.47,-23.4,;12.26,-22.08,;11.5,-20.74,;9.96,-20.72,;-4.67,-21.96,;-6.21,-21.96,;-6.98,-23.29,;-8.52,-23.29,;-9.29,-21.96,;-8.52,-20.63,;-6.98,-20.63,)|
Structure
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