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TargetHistamine H3 receptor
LigandBDBM50293632
Substrate/Competitorn/a
Meas. Tech.ChEMBL_571442 (CHEMBL1032753)
IC50 2110±n/a nM
Citation Kennedy, JPConn, PJLindsley, CW A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin. Bioorg Med Chem Lett19:3204-8 (2009) [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:
BDBM50293632
n/a
NameBDBM50293632
Synonyms:4-bromo-N-(3-bromo-4-(2-(3-fluoropyrrolidin-1-yl)ethoxy)phenethyl)-4-bromothiophene-2-carboxamide | 4-bromo-N-(3-bromo-4-(2-(3-fluoropyrrolidin-1-yl)ethoxy)phenethyl)thiophene-2-carboxamide | CHEMBL562496
TypeSmall organic molecule
Emp. Form.C19H21Br2FN2O2S
Mol. Mass.520.254
SMILESFC1CCN(CCOc2ccc(CCNC(=O)c3cc(Br)cs3)cc2Br)C1
Structure
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