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TargetHistamine H3 receptor
LigandBDBM50352080
Substrate/Competitorn/a
Meas. Tech.ChEMBL_766550 (CHEMBL1827031)
Ki 0.53±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
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  Blast E-value cutoff:
BDBM50352080
n/a
NameBDBM50352080
Synonyms:CHEMBL1824248
TypeSmall organic molecule
Emp. Form.C24H40N2O
Mol. Mass.372.5872
SMILESCCCCN[C@H]1CC[C@H](CC1)c1ccc(OCCCN2CCCCC2)cc1 |r,wU:8.11,5.4,(13.77,-38.89,;12.23,-38.87,;11.45,-40.2,;9.91,-40.18,;9.13,-41.51,;7.59,-41.5,;6.8,-42.82,;5.27,-42.81,;4.51,-41.47,;5.28,-40.14,;6.82,-40.16,;2.96,-41.46,;2.18,-42.79,;.65,-42.78,;-.11,-41.44,;-1.65,-41.43,;-2.42,-42.77,;-3.96,-42.76,;-4.73,-41.43,;-6.27,-41.43,;-7.04,-42.75,;-8.58,-42.75,;-9.35,-41.43,;-8.58,-40.09,;-7.04,-40.09,;.65,-40.11,;2.2,-40.12,)|
Structure
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