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TargetHistamine receptor (H3)
LigandBDBM50401001
Substrate/Competitorn/a
Meas. Tech.ChEMBL_879381
Ki 2.19±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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BDBM50401001
NameBDBM50401001
Synonyms:CHEMBL2206288
TypeSmall organic molecule
Emp. Form.C20H30N2O
Mol. Mass.314.465
SMILESC([C@H]1C[C@H](C1)c1ccc(CN2CCCC2)cc1)N1CCOCC1 |r,wU:3.5,1.0,(12.44,-17.63,;13.93,-17.23,;14.7,-15.89,;16.03,-16.66,;15.26,-18,;17.52,-16.26,;18.61,-17.35,;20.1,-16.95,;20.5,-15.47,;21.98,-15.07,;23.07,-16.16,;22.83,-17.68,;24.2,-18.38,;25.29,-17.29,;24.59,-15.92,;19.41,-14.38,;17.92,-14.78,;11.35,-16.54,;11.75,-15.05,;10.66,-13.96,;9.18,-14.36,;8.78,-15.85,;9.87,-16.93,)|
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
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