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TargetHistamine H3 receptor
LigandBDBM50352087
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
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  Blast E-value cutoff:
BDBM50352087
n/a
NameBDBM50352087
Synonyms:CHEMBL1824244
TypeSmall organic molecule
Emp. Form.C28H38N2O
Mol. Mass.418.6141
SMILESC(COc1ccc(cc1)[C@@H]1CC[C@@H](CC1)N1Cc2ccccc2C1)CN1CCCCC1 |r,wU:9.9,12.16,(-4.94,-32.61,;-3.4,-32.61,;-2.63,-31.28,;-1.09,-31.28,;-.33,-32.62,;1.2,-32.63,;1.98,-31.3,;1.22,-29.96,;-.33,-29.95,;3.53,-31.31,;4.29,-32.65,;5.82,-32.67,;6.61,-31.34,;5.84,-30,;4.3,-29.98,;8.15,-31.35,;9.04,-32.61,;10.5,-32.14,;11.83,-32.92,;13.17,-32.17,;13.18,-30.62,;11.85,-29.85,;10.52,-30.6,;9.06,-30.11,;-5.71,-31.27,;-7.25,-31.27,;-8.02,-32.6,;-9.56,-32.6,;-10.33,-31.27,;-9.56,-29.94,;-8.02,-29.94,)|
Structure
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