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TargetHistamine H3 receptor
LigandBDBM50401005
Substrate/Competitorn/a
Meas. Tech.ChEMBL_879383 (CHEMBL2208781)
Ki 3.31±n/a nM
Citation Wager, TTPettersen, BASchmidt, AWSpracklin, DKMente, SButler, TWHoward, HLettiere, DJRubitski, DMWong, DFNedza, FMNelson, FRRollema, HRaggon, JWAubrecht, JFreeman, JKMarcek, JMCianfrogna, JCook, KWJames, LCChatman, LAIredale, PABanker, MJHomiski, MLMunzner, JBChandrasekaran, RY Discovery of two clinical histamine H(3) receptor antagonists: trans-N-ethyl-3-fluoro-3-[3-fluoro-4-(pyrrolidinylmethyl)phenyl]cyclobutanecarboxamide (PF-03654746) and trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-N-(2-methylpropyl)cyclobutanecarboxamide (PF-03654764). J Med Chem54:7602-20 (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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BDBM50401005
n/a
NameBDBM50401005
Synonyms:CHEMBL2206290
TypeSmall organic molecule
Emp. Form.C19H27ClN2O
Mol. Mass.334.883
SMILESCN(C[C@H]1C[C@@H](C1)c1ccc(CN2CCCC2)c(Cl)c1)C(C)=O |r,wU:5.7,wD:3.2,(8.86,-17.88,;8.17,-16.51,;9.01,-15.22,;10.55,-15.3,;11.58,-16.45,;12.72,-15.42,;11.7,-14.28,;14.26,-15.51,;14.96,-16.88,;16.49,-16.97,;17.34,-15.68,;18.87,-15.77,;19.57,-17.14,;21.09,-17.39,;21.33,-18.91,;19.95,-19.6,;18.87,-18.51,;16.64,-14.31,;17.49,-13.02,;15.1,-14.22,;6.63,-16.42,;5.94,-15.05,;5.79,-17.71,)|
Structure
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