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TargetHistamine H3 receptor
LigandBDBM27201
Substrate/CompetitorBDBM22530
Meas. Tech.Radioligand Binding Assay
pH7.4±n/a
Temperature298.15±n/a K
Ki 1.66±n/a nM
Citation Zhao, CSun, MBennani, YLGopalakrishnan, SMWitte, DGMiller, TRKrueger, KMBrowman, KEThiffault, CWetter, JMarsh, KCHancock, AAEsbenshade, TACowart, MD The alkaloid conessine and analogues as potent histamine H3 receptor antagonists. J Med Chem51:5423-30 (2008) [PubMed]  Article
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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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BDBM27201
BDBM22530
NameBDBM27201
Synonyms:4-{methyl[(1R,2S,5S,6S,9R,12S,13R,16S)-6,7,13-trimethyl-7-azapentacyclo[10.8.0.0^{2,9}.0^{5,9}.0^{13,18}]icos-18-en-16-yl]amino}benzonitrile | Conessine analogue, 12g
TypeSmall organic molecule
Emp. Form.C30H41N3
Mol. Mass.443.6666
SMILES[H][C@@]1(C)N(C)C[C@]23CC[C@@]4([H])[C@@]([H])(CC=C5C[C@H](CC[C@]45C)N(C)c4ccc(cc4)C#N)[C@]2([H])CC[C@]13[H] |r,t:14|
Structure
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