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TargetHistamine H3 receptor
LigandBDBM50352090
Substrate/Competitorn/a
Meas. Tech.ChEMBL_766550 (CHEMBL1827031)
Ki 0.41±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:
BDBM50352090
n/a
NameBDBM50352090
Synonyms:CHEMBL1824241
TypeSmall organic molecule
Emp. Form.C24H38N2O2
Mol. Mass.386.5707
SMILESC(COc1ccc(cc1)[C@H]1CC[C@@H](CC1)N1CCOCC1)CN1CCCCC1 |r,wU:12.16,wD:9.9,(21.81,-23.48,;23.35,-23.48,;24.12,-22.15,;25.66,-22.15,;26.43,-23.49,;27.96,-23.5,;28.74,-22.17,;27.97,-20.83,;26.43,-20.82,;30.28,-22.18,;31.04,-23.52,;32.58,-23.53,;33.36,-22.21,;32.6,-20.87,;31.05,-20.85,;34.9,-22.22,;35.65,-23.56,;37.19,-23.58,;37.97,-22.26,;37.22,-20.92,;35.67,-20.9,;21.04,-22.14,;19.5,-22.14,;18.74,-23.47,;17.2,-23.47,;16.42,-22.14,;17.2,-20.8,;18.74,-20.8,)|
Structure
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