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TargetHistamine H3 receptor
LigandBDBM50206218
Substrate/Competitorn/a
Meas. Tech.ChEMBL_454704 (CHEMBL886726)
Ki 0.800±n/a nM
Citation Keith, JMGomez, LAWolin, RLBarbier, AJWilson, SJBoggs, JDMazur, CFraser, ICLord, BAluisio, LLovenberg, TWCarruthers, NI Pyrrolidino-tetrahydroisoquinolines as potent dual H3 antagonist and serotonin transporter inhibitors. Bioorg Med Chem Lett17:2603-7 (2007) [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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50206218
n/a
NameBDBM50206218
Synonyms:6-(4-methoxyphenyl)-9-(3-(piperidin-1-yl)propoxy)-1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]isoquinoline | CHEMBL393516
TypeSmall organic molecule
Emp. Form.C27H36N2O2
Mol. Mass.420.5869
SMILESCOc1ccc(cc1)C1CN2CCCC2c2cc(OCCCN3CCCCC3)ccc12 |w:14.14,8.8|
Structure
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