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TargetHistamine receptor (H3)
LigandBDBM50401006
Substrate/Competitorn/a
Meas. Tech.ChEMBL_879383
Ki 12±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 receptor (H3)
Name:Histamine receptor (H3 and H4)
Synonyms:G-protein coupled receptor 97 | HH3R | HISTAMINE H3 | HRH3 | Histamine H3 Receptor | 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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BDBM50401006
NameBDBM50401006
Synonyms:CHEMBL2206289
TypeSmall organic molecule
Emp. Form.C20H25N3O
Mol. Mass.323.432
SMILESC(Oc1ncccn1)[C@H]1C[C@@H](C1)c1ccc(CN2CCCC2)cc1 |r,wU:10.13,wD:8.8,(11.52,-15.55,;10.75,-14.22,;9.21,-14.22,;8.44,-15.55,;6.9,-15.55,;6.13,-14.22,;6.9,-12.88,;8.44,-12.88,;13.06,-15.55,;14.15,-16.64,;15.24,-15.55,;14.15,-14.46,;16.78,-15.55,;17.55,-14.22,;19.09,-14.22,;19.86,-15.55,;21.4,-15.55,;22.17,-16.88,;23.7,-17.04,;24.02,-18.55,;22.68,-19.32,;21.54,-18.29,;19.09,-16.88,;17.55,-16.88,)|
Structure
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